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1

Sivathanu, Dr S. Bhagavathy, Shivapriya G, and Shivapriya G. "Formulation, Characterization and In vitro Drug Delivery of Vitexin Loaded Liposomes." International Journal of Pharmaceutical Sciences and Nanotechnology 14, no. 2 (April 30, 2021): 5364–71. http://dx.doi.org/10.37285/ijpsn.2021.14.2.2.

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Liposome is a spherical vesicle which contains atleast one lipid bilayer. Liposomes are used as a novel drug carriers because of its hydrophobic and hydrophilic nature, it has many advantages in the field of medical sciences. There are some other drug carriers like dendrimers, micelles, niosomes. Out of all, liposomes are considered to be the most promising agent for drug delivery. The uniqueness of liposome is when it is used as a pharmaceutical drug, it acts as a natural receptor. Thus it acts as an antigen and binds with the antibody (cancer cell) without causing any damage to the adjacent cells. For the synthesis of liposomes, a phospholipid is required. The liposomes can be synthesized using egg yolk and chloroform. So the basic phospholipid is obtained from egg yolk. For more stability, the liposomes are prepared using popc. The present work discuss about the effective preparation of drug loaded liposomes using popc (1- palmitoyl-2-oleoyl-sn-glycero-3- phosphocholine). POPC is an important phospholipid for biophysical experiments. Additionally chloroform is used as the solvent for the liposome preparation. The drug chosen for liposome loading is vitexin (vxn), which is an effective therapeutic agent against inflammation and cancer. The vesicular size, shape, drug entrapment efficacy, stability, electrochemical property and drug releasing property of the formulated liposomes were characterized. The results showed that the formulated liposomes are considered as the better drug carrier system and good choice for biotransformation within the cell to reach the target site such as cancer cells. Even though available treatments like chemotherapy and radiation therapy, causes damage to the surrounding cells, the alternative drug transferring system such as liposomal mediated drug transfer within the cell is considered as good choice of treatment to avoid such complications. The aim of liposome mediated drug carrier system is to develop a method to reach the drug to the target site. After drug delivery at the target site, the liposomes are fused within the surface of the body. This is because of the pH of liposomes, which is at 7.4 and temperature is maintained at 37 oC. So, the vxn loaded liposomes are considered as the novel drug carriers for the successful targetted drug delivery.
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2

Cattel, Luigi, Maurizio Ceruti, and Franco Dosio. "From Conventional to Stealth Liposomes a new Frontier in Cancer Chemotherapy." Tumori Journal 89, no. 3 (May 2003): 237–49. http://dx.doi.org/10.1177/030089160308900302.

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Many attempts have been made to achieve good selectivity to targeted tumor cells by preparing specialized carrier agents that are therapeutically profitable for anticancer therapy. Among these, liposomes are the most studied colloidal particles thus far applied in medicine and in particular in antitumor therapy. Although they were first described in the 1960s, only at the beginning of 1990s did the first therapeutic liposomes appear on the market. The first-generation liposomes (conventional liposomes) comprised a liposome-containing amphotericin B, Ambisome (Nexstar, Boulder, CO, USA), used as an antifungal drug, and Myocet (Elan Pharma Int, Princeton, NJ, USA), a doxorubicin-containing liposome, used in clinical trials to treat metastatic breast cancer. The second-generation liposomes (“pure lipid approach”) were long-circulating liposomes, such as Daunoxome, a daunorubicin-containing liposome approved in the US and Europe to treat AIDS-related Kaposi's sarcoma. The third-generation liposomes were surface-modified liposomes with gangliosides or sialic acid, which can evade the immune system responsible for removing liposomes from circulation. The fourth-generation liposomes, pegylated liposomal doxorubicin, were called “stealth liposomes” because of their ability to evade interception by the immune system, in the same way as the stealth bomber was able to evade radar. Actually, the only stealth liposome on the market is Caelyx/Doxil (Schering-Plough, Madison NJ, USA), used to cure AIDS-related Kaposi's sarcoma, resistant ovarian cancer and metastatic breast cancer. Pegylated liposomal doxorubicin is characterized by a very long-circulation half-life, favorable pharmacokinetic behavior and specific accumulation in tumor tissues. These features account for the much lower toxicity shown by Caelyx in comparison to free doxorubicin, in terms of cardiotoxicity, vesicant effects, nausea, vomiting and alopecia. Pegylated liposomal doxorubicin also appeared to be less myelotoxic than doxorubicin. Typical forms of toxicity associated to it are acute infusion reaction, mucositis and palmar plantar erythrodysesthesia, which occur especially at high doses or short dosing intervals. Active and cell targeted liposomes can be obtained by attaching some antigen-directed monoclonal antibodies (Moab or Moab fragments) or small proteins and molecules (folate, epidermal growth factor, transferrin) to the distal end of polyethylene glycol in pegylated liposomal doxorubicin. The most promising therapeutic application of liposomes is as non-viral vector agents in gene therapy, characterized by the use of cationic phospholipids complexed with the negatively charged DNA plasmid. The use of liposome formulations in local-regional anticancer therapy is also discussed. Finally, pegylated liposomal doxorubicin containing radionuclides are used in clinical trials as tumor-imaging agents or in positron emission tomography.
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3

Gorbik, V. S., Z. S. Shprakh, Z. M. Kozlova, and V. G. Salova. "LIPOSOMES AS A TARGETED DELIVERY SYSTEM OF DRUGS (REVIEW)." Russian Journal of Biotherapy 20, no. 1 (April 8, 2021): 33–41. http://dx.doi.org/10.17650/1726-9784-2021-20-1-33-41.

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Liposomal targeted drug delivery makes it possible to achieve effective concentration in the target cell under various pathological conditions. The main advantage of liposomal particles is their biodegradability and immunological neutrality, which improves the safety profile of drugs. The review provides information on the composition of liposomes: the main component of the liposomal membrane is phospholipids, which provide its strength and protect from mechanical impacts. Liposomal particles are distinguished by the size and number of bilayer membranes, also secreted liposomes with a non‑lamellar organization. The composition and size of liposomes are selected depending on the purpose, including excipients in the membrane that affect the properties and functions of liposomes, including the rate of release of the components, the affinity of liposomes for the target tissue, etc. The review considers the main methods for obtaining liposomes and the features of their use, advantages and disadvantages. The creation of liposomes that are sensitive to various external or internal physicochemical factors makes it possible to realize drugs effects, localize the site of its action and reduce the number and severity of side effects. Currently, liposome‑based drugs are successfully used in various fields of medicine – dermatology, cardiology, oncology, neurology, etc. The most active condact preclinical and clinical studies of liposomal drugs for the treatment of malignant neoplasms. Particular attention is paid to the work of Russian researchers in the field of targeted drug delivery. It is shown that today liposomes are an open for study and improvement system for targeted drug delivery.
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4

Medina, Oula Peñate, Tuula Peñate Medina, Jana Humbert, Bao Qi, Wolfgang Baum, Olga Will, Timo Damm, and Claus Glüer. "Using Alendronic Acid Coupled Fluorescently Labelled SM Liposomes as a Vehicle for Bone Targeting." Current Pharmaceutical Design 26, no. 46 (December 30, 2020): 6021–27. http://dx.doi.org/10.2174/1381612826666200614175905.

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Background: We recently developed a liposomal nanoparticle system that can be used for drug delivery and simultaneously be monitored by optical or photoacoustic imaging devices. Here we tested the efficacy of alendronate as a homing molecule in SM-liposomes for bone targeting. Methods: Alendronate was immobilized covalently on the liposomal surface and the fluorescent dye indocyanine green was used as a payload in the liposomes. The indocyanine green delivery was analyzed by 3D optical tomography, optical fluorescence scanner, photoacoustic imaging, and by ex-vivo biodistribution studies. Results: The results show that the alendronate, coupled to the liposomal surface, increases sphingomyelin containing liposome targeting up to several-folds. Conclusion: The alendronate targeted liposomes open possibilities for an application in active bone targeting.
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5

Tansi, Felista L., Ronny Rüger, Ansgar M. Kollmeier, Markus Rabenhold, Frank Steiniger, Roland E. Kontermann, Ulf K. Teichgräber, Alfred Fahr, and Ingrid Hilger. "Targeting the Tumor Microenvironment with Fluorescence-Activatable Bispecific Endoglin/Fibroblast Activation Protein Targeting Liposomes." Pharmaceutics 12, no. 4 (April 17, 2020): 370. http://dx.doi.org/10.3390/pharmaceutics12040370.

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Liposomes are biocompatible nanocarriers with promising features for targeted delivery of contrast agents and drugs into the tumor microenvironment, for imaging and therapy purposes. Liposome-based simultaneous targeting of tumor associated fibroblast and the vasculature is promising, but the heterogeneity of tumors entails a thorough validation of suitable markers for targeted delivery. Thus, we elucidated the potential of bispecific liposomes targeting the fibroblast activation protein (FAP) on tumor stromal fibroblasts, together with endoglin which is overexpressed on tumor neovascular cells and some neoplastic cells. Fluorescence-quenched liposomes were prepared by hydrating a lipid film with a high concentration of the self-quenching near-infrared fluorescent dye, DY-676-COOH, to enable fluorescence detection exclusively upon liposomal degradation and subsequent activation. A non-quenched green fluorescent phospholipid was embedded in the liposomal surface to fluorescence-track intact liposomes. FAP- and murine endoglin-specific single chain antibody fragments were coupled to the liposomal surface, and the liposomal potentials validated in tumor cells and mice models. The bispecific liposomes revealed strong fluorescence quenching, activatability, and selectivity for target cells and delivered the encapsulated dye selectively into tumor vessels and tumor associated fibroblasts in xenografted mice models and enabled their fluorescence imaging. Furthermore, detection of swollen lymph nodes during intra-operative simulations was possible. Thus, the bispecific liposomes have potentials for targeted delivery into the tumor microenvironment and for image-guided surgery.
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6

Peñate-Medina, Tuula, Christabel Damoah, Miriam Benezra, Olga Will, Kalevi Kairemo, Jana Humbert, Susanne Sebens, and Oula Peñate-Medina. "Alpha-MSH Targeted Liposomal Nanoparticle for Imaging in Inflammatory Bowel Disease (IBD)." Current Pharmaceutical Design 26, no. 31 (September 17, 2020): 3840–46. http://dx.doi.org/10.2174/1381612826666200727002716.

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Background: The purpose of our study was to find a novel targeted imaging and drug delivery vehicle for inflammatory bowel disease (IBD). IBD is a common and troublesome disease that still lacks effective therapy and imaging options. As an attempt to improve the disease treatment, we tested αMSH for the targeting of nanoliposomes to IBD sites. αMSH, an endogenous tridecapeptide, binds to the melanocortin-1 receptor (MC1-R) and has anti-inflammatory and immunomodulating effects. MC1-R is found on macrophages, neutrophils and the renal tubule system. We formulated and tested a liposomal nanoparticle involving αMSH in order to achieve a specific targeting to the inflamed intestines. Methods: NDP-αMSH peptide conjugated to Alexa Fluor™ 680 was linked to the liposomal membrane via NSuccinyl PE and additionally loaded into the lumen of the liposomes. Liposomes without the αMSH-conjugate and free NDP-αMSH were used as a control. The liposomes were also loaded with ICG to track them. The liposomes were tested in DSS treated mice, which had received DSS via drinking water order to develop a model IBD. Inflammation severity was assessed by the Disease Activity Index (DAI) score and ex vivo histological CD68 staining of samples taken from different parts of the intestine. The liposome targeting was analyzed by analyzing the ICG and ALEXA 680 fluorescence in the intestine compared to the biodistribution. Results: NPD-αMSH was successfully labeled with Alexa and retained its biological activity. Liposomes were identified in expected regions in the inflamed bowel regions and in the kidneys, where MC1-R is abundant. In vivo liposome targeting correlated with the macrophage concentration at the site of the inflammation supporting the active targeting of the liposomes through αMSH. The liposomal αMSH was well tolerated by animals. Conclusions: This study opens up the possibility to further develop an αMSH targeted theranostic delivery to different clinically relevant applications in IBD inflammation but also opens possibilities for use in other inflammations like lung inflammation in Covid 19.
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7

Nijen Twilhaar, Maarten K., Lucas Czentner, Joanna Grabowska, Alsya J. Affandi, Chun Yin Jerry Lau, Katarzyna Olesek, Hakan Kalay, et al. "Optimization of Liposomes for Antigen Targeting to Splenic CD169+ Macrophages." Pharmaceutics 12, no. 12 (November 25, 2020): 1138. http://dx.doi.org/10.3390/pharmaceutics12121138.

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Despite promising progress in cancer vaccination, therapeutic effectiveness is often insufficient. Cancer vaccine effectiveness could be enhanced by targeting vaccine antigens to antigen-presenting cells, thereby increasing T-cell activation. CD169-expressing splenic macrophages efficiently capture particulate antigens from the blood and transfer these antigens to dendritic cells for the activation of CD8+ T cells. In this study, we incorporated a physiological ligand for CD169, the ganglioside GM3, into liposomes to enhance liposome uptake by CD169+ macrophages. We assessed how variation in the amount of GM3, surface-attached PEG and liposomal size affected the binding to, and uptake by, CD169+ macrophages in vitro and in vivo. As a proof of concept, we prepared GM3-targeted liposomes containing a long synthetic ovalbumin peptide and tested the capacity of these liposomes to induce CD8+ and CD4+ T-cell responses compared to control liposomes or soluble peptide. The data indicate that the delivery of liposomes to splenic CD169+ macrophages can be optimized by the selection of liposomal constituents and liposomal size. Moreover, optimized GM3-mediated liposomal targeting to CD169+ macrophages induces potent immune responses and therefore presents as an interesting delivery strategy for cancer vaccination.
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8

Naik, Himgauri, Jafrin Jobayer Sonju, Sitanshu Singh, Ioulia Chatzistamou, Leeza Shrestha, Ted Gauthier, and Seetharama Jois. "Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy." Pharmaceuticals 14, no. 3 (March 6, 2021): 221. http://dx.doi.org/10.3390/ph14030221.

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The therapeutic index of chemotherapeutic agents can be improved by the use of nano-carrier-mediated chemotherapeutic delivery. Ligand-targeted drug delivery can be used to achieve selective and specific delivery of chemotherapeutic agents to cancer cells. In this study, we prepared a peptidomimetic conjugate (SA-5)-tagged doxorubicin (Dox) incorporated liposome (LP) formulation (SA-5-Dox-LP) to evaluate the targeted delivery potential of SA-5 in human epidermal growth factor receptor-2 (HER2) overexpressed non-small-cell lung cancer (NSCLC) and breast cancer cell lines. The liposome was prepared using thin lipid film hydration and was characterized for particle size, encapsulation efficiency, cell viability, and targeted cellular uptake. In vivo evaluation of the liposomal formulation was performed in a mice model of NSCLC. The cell viability studies revealed that targeted SA-5-Dox-LP showed better antiproliferative activity than non-targeted Dox liposomes (Dox-LP). HER2-targeted liposome delivery showed selective cellular uptake compared to non-targeted liposomes on cancer cells. In vitro drug release studies indicated that Dox was released slowly from the formulations over 24 h, and there was no difference in Dox release between Dox-LP formulation and SA-5-Dox-LP formulation. In vivo studies in an NSCLC model of mice indicated that SA-5-Dox-LP could reduce the lung tumors significantly compared to vehicle control and Dox. In conclusion, this study demonstrated that the SA-5-Dox-LP liposome has the potential to increase therapeutic efficiency and targeted delivery of Dox in HER2 overexpressing cancer.
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9

Harokopakis, Evlambia, George Hajishengallis, and Suzanne M. Michalek. "Effectiveness of Liposomes Possessing Surface-Linked Recombinant B Subunit of Cholera Toxin as an Oral Antigen Delivery System." Infection and Immunity 66, no. 9 (September 1, 1998): 4299–304. http://dx.doi.org/10.1128/iai.66.9.4299-4304.1998.

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ABSTRACT Liposomes appear to be a promising oral antigen delivery system for the development of vaccines against infectious diseases, although their uptake efficiency by Peyer’s patches in the gut and the subsequent induction of mucosal immunoglobulin A (IgA) responses remain a major concern. Aiming at targeted delivery of liposomal immunogens, we have previously reported the conjugation via a thioether bond of the GM1 ganglioside-binding subunit of cholera toxin (CTB) to the liposomal outer surface. In the present study, we have investigated the effectiveness of liposomes containing the saliva-binding region (SBR) of Streptococcus mutans AgI/II adhesin and possessing surface-linked recombinant CTB (rCTB) in generating mucosal (salivary, vaginal, and intestinal) IgA as well as serum IgG responses to the parent molecule, AgI/II. Responses in mice given a single oral dose of the rCTB-conjugated liposomes were compared to those in mice given one of the following unconjugated liposome preparations: (i) empty liposomes, (ii) liposomes containing SBR, (iii) liposomes containing SBR and coadministered with rCTB, and (iv) liposomes containing SBR plus rCTB. Three weeks after the primary immunization, significantly higher levels of mucosal IgA and serum IgG antibodies to AgI/II were observed in the rCTB-conjugated group than in mice given the unconjugated liposome preparations, although the latter mice received a booster dose at week 9. The antibody responses in mice immunized with rCTB-conjugated liposomes persisted at high levels for at least 6 months, at which time (week 26) a recall immunization significantly augmented the responses. In general, mice given unconjugated liposome preparations required one or two booster immunizations to develop a substantial anti-AgI/II antibody response, which was more prominent in the group given coencapsulated SBR and rCTB. These data indicate that conjugation of rCTB to liposomes greatly enhances their effectiveness as an antigen delivery system. This oral immunization strategy should be applicable for the development of vaccines against oral, intestinal, or sexually transmitted diseases.
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10

Nosova, A. S., O. O. Koloskova, I. P. Shilovskiy, Yu L. Sebyakin, and M. R. Khaitov. "Lactose-based glycoconjugates with variable spacers for design of liver-targeted liposomes." Biomeditsinskaya Khimiya 63, no. 5 (2017): 467–71. http://dx.doi.org/10.18097/pbmc20176305467.

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Asialoglycoprotein receptors are highly abundant on the hepatocyte surface and have specific binding sites for blood serum glycoproteins. Such discovery resulted in development of liver-targeted drug delivery systems because modification of the liposomal surface by carbohydrate derivatives results in an increase of endocytosis, which facilitates selective uptake of such systems by hepatocytes. In this study we have synthesized novel lactose derivatives containing a palmitic hydrophobic domain. They were used for modification of the liposome surface. Transfection activity of modified liposomes was analyzed on the HepG2 cell line (hepatocytes) and showed an increase in the transfection efficiency as compared to the non-modified liposomes. At the same time transfection activities of modified and non-modified liposomes were similar in the case of a non-hepatocyte cell line (293T). The novel lactose-based glycoconjugates may be a promising tool for developing efficient vectors for delivery of nucleic acids to hepatocytes.
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11

Khan, David R., Maggie N. Webb, Thomas H. Cadotte, and Madison N. Gavette. "Use of Targeted Liposome-based Chemotherapeutics to Treat Breast Cancer." Breast Cancer: Basic and Clinical Research 9s2 (January 2015): BCBCR.S29421. http://dx.doi.org/10.4137/bcbcr.s29421.

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The use of nanocarriers such as liposomes to deliver anticancer drugs to tumors can significantly enhance the therapeutic index of otherwise unencapsulated cytotoxic agents. This is in part because of the fact that the phospholipid bilayer can protect healthy sensitive tissue from the damaging effects of these types of drugs. Furthermore, the ease with which the phospholipid bilayer surface can be modified to allow for polyethylene glycol incorporation resulting in pegylated liposomes allow for increased circulation times in vivo, and thus an overall increase in the concentration of the drug delivered to the tumor site. This explains the clinical success of the liposomal-based drug Doxil, which has proven to be quite efficacious in the treatment of breast cancer. However, significant challenges remain involving poor drug transfer between the liposome and tumor cells with this type of nontargeted drug delivery system. Thus, future work involves the development of “smart” drugs, or targeted drug delivery intended for improved colocalization between the drug and cancerous cells. While it is not possible to entirely discuss such a rapidly growing field of study involving many different types of chemotherapeutics here, in this review, we discuss some of the recent advancements involving the development of targeted liposome-based chemotherapeutics to treat breast cancer.
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12

Arigita, Carmen, Lisette Bevaart, Linda A. Everse, Gerben A. Koning, Wim E. Hennink, Daan J. A. Crommelin, Jan G. J. van de Winkel, Martine J. van Vugt, Gideon F. A. Kersten, and Wim Jiskoot. "Liposomal Meningococcal B Vaccination: Role of Dendritic Cell Targeting in the Development of a Protective Immune Response." Infection and Immunity 71, no. 9 (September 2003): 5210–18. http://dx.doi.org/10.1128/iai.71.9.5210-5218.2003.

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ABSTRACT The effect of targeting strategies for improving the interaction of liposomal PorA with dendritic cells (DC) on the immunogenicity of PorA was investigated. PorA, a major antigen of Neisseria meningitidis, was purified and reconstituted in different types of (targeted) liposomes, i.e., by using mannose or phosphatidylserine as targeting moieties, or with positively charged liposomes. We studied the efficiency of liposome uptake and its effect on the maturation of and interleukin 12 (IL-12) production by murine DC. Moreover, mice were immunized subcutaneously to study the localization and immunogenicity of PorA liposomes. Uptake of liposomes by DC was significantly increased for targeted liposomes and resulted in the maturation of DC, but to various degrees. Maturation markers (i.e., CD80, CD86, major histocompatibility complex class II, and CD40) showed enhanced expression on DC incubated with targeted PorA liposomes relative to those incubated with nontargeted PorA liposomes. Moreover, only the uptake of targeted PorA liposomes induced production of IL-12 by DC, with levels similar to those produced by lipopolysaccharide (LPS)-pulsed DC. Mannose-targeted PorA liposomes administered subcutaneously had an increased localization in draining lymph nodes compared to nontargeted PorA liposomes. Liposomes in draining lymph nodes interacted preferentially with antigen-presenting cells, an effect that was enhanced with targeted PorA liposomes. Immunization studies showed an improvement of the bactericidal antibody response (i.e., increased number of responders) generated by targeted PorA liposomes compared to that generated by nontargeted ones or LPS-containing outer membrane vesicles. In conclusion, the use of targeted PorA liposomes results in an improved uptake by and activation of DC and an increased localization in draining lymph nodes. These effects correlate with an enhanced immune response toward the vaccine.
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13

Palchetti, Sara, Damiano Caputo, Luca Digiacomo, Anna Capriotti, Roberto Coppola, Daniela Pozzi, and Giulio Caracciolo. "Protein Corona Fingerprints of Liposomes: New Opportunities for Targeted Drug Delivery and Early Detection in Pancreatic Cancer." Pharmaceutics 11, no. 1 (January 15, 2019): 31. http://dx.doi.org/10.3390/pharmaceutics11010031.

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Pancreatic ductal adenocarcinoma (PDAC) is the fourth cause of cancer-related mortality in the Western world and is envisaged to become the second cause by 2030. Although our knowledge about the molecular biology of PDAC is continuously increasing, this progress has not been translated into better patients’ outcome. Liposomes have been used to circumvent concerns associated with the low efficiency of anticancer drugs such as severe side effects and damage of healthy tissues, but they have not resulted in improved efficacy as yet. Recently, the concept is emerging that the limited success of liposomal drugs in clinical practice is due to our poor knowledge of the nano–bio interactions experienced by liposomes in vivo. After systemic administration, lipid vesicles are covered by plasma proteins forming a biomolecular coating, referred to as the protein corona (PC). Recent studies have clarified that just a minor fraction of the hundreds of bound plasma proteins, referred to as “PC fingerprints” (PCFs), enhance liposome association with cancer cells, triggering efficient particle internalization. In this study, we synthesized a library of 10 liposomal formulations with systematic changes in lipid composition and exposed them to human plasma (HP). Size, zeta-potential, and corona composition of the resulting liposome–protein complexes were thoroughly characterized by dynamic light scattering (DLS), micro-electrophoresis, and nano-liquid chromatography tandem mass spectrometry (nano-LC MS/MS). According to the recent literature, enrichment in PCFs was used to predict the targeting ability of synthesized liposomal formulations. Here we show that the predicted targeting capability of liposome–protein complexes clearly correlate with cellular uptake in pancreatic adenocarcinoma (PANC-1) and insulinoma (INS-1) cells as quantified by flow-assisted cell sorting (FACS). Of note, cellular uptake of the liposomal formulation with the highest abundance of PCFs was much larger than that of Onivyde®, an Irinotecan liposomal drug approved by the Food and Drug Administration in 2015 for the treatment of metastatic PDAC. Given the urgent need of efficient nanocarriers for the treatment of PDAC, we envision that our results will pave the way for the development of more efficient PC-based targeted nanomaterials. Here we also show that some BCs are enriched with plasma proteins that are associated with the onset and progression of PDAC (e.g., sex hormone-binding globulin, Ficolin-3, plasma protease C1 inhibitor, etc.). This could open the intriguing possibility to identify novel biomarkers.
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Sebaaly, Carine, Adriana Trifan, Elwira Sieniawska, and Hélène Greige-Gerges. "Chitosan-Coating Effect on the Characteristics of Liposomes: A Focus on Bioactive Compounds and Essential Oils: A Review." Processes 9, no. 3 (March 1, 2021): 445. http://dx.doi.org/10.3390/pr9030445.

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In recent years, liposomes have gained increasing attention for their potential applications as drug delivery systems in the pharmaceutic, cosmetic and food industries. However, they have a tendency to aggregate and are sensitive to degradation caused by several factors, which may limit their effectiveness. A promising approach to improve liposomal stability is to modify liposomal surfaces by forming polymeric layers. Among natural polymers, chitosan has received great interest due to its biocompatibility and biodegradability. This review discussed the characteristics of this combined system, called chitosomes, in comparison to those of conventional liposomes. The coating of liposomes with chitosan or its derivatives improved liposome stability, provided sustained drug release and increased drug penetration across mucus layers. The mechanisms behind these results are highlighted in this paper. Alternative assembly of polyelectrolytes using alginate, sodium hyaluronate, or pectin with chitosan could further improve the liposomal characteristics. Chitosomal encapsulation could also ensure targeted delivery and boost the antimicrobial efficacy of essential oils (EOs). Moreover, chitosomes could be an efficient tool to overcome the major drawbacks related to the chemical properties of EOs (low water solubility, sensitivity to oxygen, light, heat, and humidity) and their poor bioavailability. Overall, chitosomes could be considered as a promising strategy to enlarge the use of liposomes.
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Škorpilová, Ludmila, Silvie Rimpelová, Michal Jurášek, Miloš Buděšínský, Jana Lokajová, Roman Effenberg, Petr Slepička, et al. "BODIPY-based fluorescent liposomes with sesquiterpene lactone trilobolide." Beilstein Journal of Organic Chemistry 13 (July 4, 2017): 1316–24. http://dx.doi.org/10.3762/bjoc.13.128.

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Like thapsigargin, which is undergoing clinical trials, trilobolide is a natural product with promising anticancer and anti-inflammatory properties. Similar to thapsigargin, it has limited aqueous solubility that strongly reduces its potential medicinal applications. The targeted delivery of hydrophobic drugs can be achieved using liposome-based carriers. Therefore, we designed a traceable liposomal drug delivery system for trilobolide. The fluorescent green-emitting dye BODIPY, cholesterol and trilobolide were used to create construct 6. The liposomes were composed of dipalmitoyl-3-trimethylammoniumpropane and phosphatidylethanolamine. The whole system was characterized by atomic force microscopy, the average size of the liposomes was 150 nm in width and 30 nm in height. We evaluated the biological activity of construct 6 and its liposomal formulation, both of which showed immunomodulatory properties in primary rat macrophages. The uptake and intracellular distribution of construct 6 and its liposomal formulation was monitored by means of live-cell fluorescence microscopy in two cancer cell lines. The encapsulation of construct 6 into the liposomes improved the drug distribution in cancer cells and was followed by cell death. This new liposomal trilobolide derivative not only retains the biological properties of pure trilobolide, but also enhances the bioavailability, and thus has potential for the use in theranostic applications.
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Al-Mahmood, Sumayah. "Targeting Breast Cancer Stem Cells (BCSCs) with Liposomal Formulations." Clinical Cancer Drugs 6, no. 1 (September 27, 2019): 3–7. http://dx.doi.org/10.2174/2212697x06666190318150757.

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Breast cancer stem cells (BCSCs) are a small proportion of cells that may be responsible for improving the resistance of cancer cells to the treatment and metastasis of breast cancer (MBC). Nanovehicles such as liposomes are extensively explored for diagnosis, treatment, and imaging of cancer. Targeted therapy with nanoparticles can be used to overcome the chemoresistance problem of cancer stem cells. Liposomes are lipid bilayer nanocarriers that have the ability to inhibit Pglycoprotein to overcome multidrug resistance that makes liposome ideal choice for using in BCSCs therapy. The main objective of this review is to describe novel liposomal formulations that are used in targeting BCSCs, which help in improving breast cancer treatment.
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Pandya, Tosha, Kaushika Kaushika Patel, Rudree Pathak, and Shreeraj Shah. "Liposomal Formulations In Cancer Therapy: Passive Versus Active Targeting." Asian Journal of Pharmaceutical Research and Development 7, no. 2 (April 14, 2019): 35–38. http://dx.doi.org/10.22270/ajprd.v7i2.489.

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In Cancer therapy, Nano drug delivery system comprising of Liposomes, are the most successful mode of treatment in present scenario which also has real time clinical application. Recently it is found that the closed bilayer phospholipid vesicles have many technical advantages over the initially used liposomal formulations. The delivery of therapeutics encapsulated in liposomes changes the biological distribution profile and improves the drug therapeutic indices of various drugs. This review article throws light onto many clinical liposomal drug delivery products. The liposome Nano drug delivery by the active and passive targeting is a boon as it can reduce the off-targeting effects. The current development is more focused on the diagnostic and clinical applications. Receptor targeted delivery systems are extensively explored for active targeting. However, these delivery systems are rarely seen in the clinical application because of conjugation chemistry and other implicit hurdles to develop this system.The development of nanocarriers in the cancer treatment have enormous potential in the medical field. Moreover, Immuno liposomes have been used in cancer treatment as attractive drug targeting vehicles. On the other hand, there are many other liposomal drug delivery systems having passive targeting mechanism for cancer treatment which are widely used due to enhanced retention and permeability of formulation. This review majorly focuses on the current challenges encountered in development of liposomal Nano drug delivery systems and its effective development for cancer treatment.
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Yan, Wei, Sharon SY Leung, and Kenneth KW To. "Updates on the use of liposomes for active tumor targeting in cancer therapy." Nanomedicine 15, no. 3 (February 2020): 303–18. http://dx.doi.org/10.2217/nnm-2019-0308.

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In the development of cancer chemotherapy, besides the discovery of new anticancer drugs, a variety of nanocarrier systems for the delivery of previously developed and new chemotherapeutic drugs have currently been explored. Liposome is one of the most studied nanocarrier systems because of its biodegradability, simple preparation method, high efficacy and low toxicity. To make the best use of this vehicle, a number of multifunctionalized liposomal formulations have been investigated. The objective of this review is to summarize the current development of novel active targeting liposomal formulations, and to give insight into the challenges and future direction of the field. The recent studies in active targeting liposomes suggest the great potential of precise targeted anticancer drug delivery in cancer therapeutics.
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19

Melnikova, E. V., D. V. Goryachev, A. A. Chaplenko, M. A. Vodyakova, A. R. Sayfutdinova, and V. A. Merkulov. "Development of liposomal drug formulations: quality attributes and methods for quality control." NANOMEDICINE, no. 6 (December 31, 2018): 33–39. http://dx.doi.org/10.24075/brsmu.2018.092.

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The use of nanostructured components in drug manufacturing and, more specifically, targeted drug delivery has recently become a major trend in the pharmaceutical industry. Nanodrugs encompass a wide range of pharmaceutical agents containing dendrimers, nanocrystals, micelles, liposomes, and polymer nanoparticles. Liposomes are the most well-studied nanoparticles and effective drug carriers. However, the more complex their structure is, the more process controls are needed and the more quality attributes have to be monitored, including the chemical properties of the liposomal fraction such as the shape, size and charge of the nanoparticle, conjugation efficacy, and distribution of the active ingredient. We believe that quality control of key liposome characteristics should rely on dynamic and laser light scattering coupled with electrophoresis, differential scanning calorimetry, cryo-electron microscopy, nuclear magnetic resonance, laser diffraction analysis, and gel filtration chromatography.
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20

Tanashyan, M. M., R. B. Medvedev, O. V. Lagoda, E. S. Berdnikovich, S. I. Skrylev, E. G. Gemdzhian, and M. V. Krotenkova. "The state of cognitive functions after angioreconstructive operations on the carotid arteries." IMMUNO-ONCOLOGY, no. 5 (September 16, 2019): 65–71. http://dx.doi.org/10.24075/brsmu.2019.059.

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The use of nanostructured components in drug manufacturing and, more specifically, targeted drug delivery has recently become a major trend in the pharmaceutical industry. Nanodrugs encompass a wide range of pharmaceutical agents containing dendrimers, nanocrystals, micelles, liposomes, and polymer nanoparticles. Liposomes are the most well-studied nanoparticles and effective drug carriers. However, the more complex their structure is, the more process controls are needed and the more quality attributes have to be monitored, including the chemical properties of the liposomal fraction such as the shape, size and charge of the nanoparticle, conjugation efficacy, and distribution of the active ingredient. We believe that quality control of key liposome characteristics should rely on dynamic and laser light scattering coupled with electrophoresis, differential scanning calorimetry, cryo-electron microscopy, nuclear magnetic resonance, laser diffraction analysis, and gel filtration chromatography.
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21

Gew, Lai Ti, Vicit Rizal Eh Suk, and Misni Misran. "Preparation and Characterization of PEGylated C18 Fatty Acids/Anti-SNAP25 Antibody-Targeted Liposomes." Current Chemical Biology 13, no. 2 (July 12, 2019): 129–39. http://dx.doi.org/10.2174/2212796812666180912113156.

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Background: Unsaturated C18 fatty acids, such as oleic acid (L1), linoleic acid (L2), and linolenic acid (L3), are a good choice of lipids to prepare liposomes. They are inexpensive, biocompatible, nontoxic, and readily available compared with phospholipids. Moreover, cis-double bonds of unsaturated fatty acids prevent the packing of molecules which increases membrane fluidity in liposomes making them a good choice of starting materials to prepare liposomes. Objective: Unsaturated C18 fatty acid liposomes, as well as their PEGylated and non- PEGylated antibody-targeted liposomes, were prepared and characterized. Methods: The particle size and zeta potential of the prepared liposomes (1 mM, pH = 7.4) for 28 and 14 days, respectively, were monitored and characterized. Membrane-bound antibodies Anti-SNAP25 (AS25) and DOPE PEG2000 (DP) were conjugated to pure C18 fatty acid liposomes to achieve stable fatty acid formulations. Results: The mean particle sizes of pure L1, L2, and L3 liposome solutions were 125, 129, and 122 nm respectively, while their polydispersity index values were 0.28, 0.21, and 0.40 respectively. A large negative zeta potential value of 45 mV was observed due to anionic carboxylate head-group of pure liposomes. The incorporation of AS25 into L1/DP, L2/DP, and L3/DP liposome solutions stabilized their mean particle size and zeta potential measurements over 28 and 14 days, respectively. Conclusion: L1/DP/AS25 was found to be the most stable PEGylated antibody-targeted liposome system because its particle size remained between 90 and 125 nm in 28 days. Transmission electron microscopy observations also supported the incorporation of AS25 and DP on the membrane surface as predicted.
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22

Lee, Robert J., Susan Wang, Mary Jo Turk, and Philip S. Low. "The Effects of pH and Intraliposomal Buffer Strength on the Rate of Liposome Content Release and Intracellular Drug Delivery." Bioscience Reports 18, no. 2 (April 1, 1998): 69–78. http://dx.doi.org/10.1023/a:1020132226113.

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Targeted liposomal drug formulations may enter cells by receptor-mediated endocytosis and then traffick by membrane flow into acidic intracellular compartments. In order to understand the impact of these intracellular pH changes on liposomal drug unloading, the effect of pH on the release from folate-targeted liposomes of three model compounds with distinct pH dependencies was examined. 5(6)-carboxyfluorescein, which titrates from its anionic to uncharged form following internalization by KB cells, displays strong endocytosis-dependent release, since only its uncharged (endosomal) form is membrane permeable. Endocytosis-triggered unloading of drugs of this sort is enhanced by encapsulating the drug in a weak buffer at neutral pH, so that acidification of the intraliposomal compartment following cellular uptake can occur rapidly. Sulforhodamine B, in contrast, retains both anionic and cationic charges at endosomal pH (∼pH 5), and consequently, escapes the endosomes only very slowly. Doxorubicin, which is commonly loaded into liposomes in its membrane-impermeable (cationic) form using an acidic buffer, still displays endocytosis-triggered unloading, since sufficient uncharged doxorubicin remains at endosomal pHs to allow rapid re-equilibration of the drug according to the new proton gradient across the membrane. In this case, when the extraliposomal [H+] increases 250-fold from 4 × 10−8 M (pH 7.4, outside the cell) to 10−5 M (pH 5, inside the endosome), the ratio of doxorubicin inside to outside the liposome must decrease by a factor of 250. Therefore, the collapse of the transliposomal pH gradient indirectly drives an efflux of the drug molecule from the liposome. Since a change in intraliposomal pH is not required to unload drugs of this type, the intraliposomal compartment can be buffered strongly at acidic pH to prevent premature release of the drug outside the cell. In summary, pH triggered release of liposome-encapsulated drugs can be achieved both with drugs that increase as well as decrease their membrane permeabilities upon acidification, as long as the intraliposomal buffer strength and pH is rationally selected.
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23

Walther, F. J., R. David-Cu, M. C. Supnet, M. L. Longo, B. R. Fan, and R. Bruni. "Uptake of antioxidants in surfactant liposomes by cultured alveolar type II cells is enhanced by SP-A." American Journal of Physiology-Lung Cellular and Molecular Physiology 265, no. 4 (October 1, 1993): L330—L339. http://dx.doi.org/10.1152/ajplung.1993.265.4.l330.

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Antioxidant delivery may be targeted toward the alveolar epithelium by encapsulating superoxide dismutase (SOD) and catalase in liposomes made from pulmonary surfactant. We studied whether antioxidant-surfactant liposomes increase cellular antioxidant activity in alveolar type II cells and whether this effect is influenced by the presence of surfactant protein A (SP-A). Cu,Zn SOD and catalase were encapsulated in liposomes made from synthetic phospholipids with or without 5% SP-A or from natural cow surfactant. Alveolar type II cells from adult rats were preincubated for 20 h, and liposome mixtures were added for 24 h, followed by measurement of cellular SOD and catalase activities (U/mg DNA). Antioxidant-surfactant liposomes increased alveolar type II cell antioxidant activity sharply. Uptake of SOD/catalase from liposomes with synthetic phospholipids and SP-A was twice that from liposomes without SP-A and did not further improve in the presence of SP-B and -C. Encapsulation of antioxidants diminished the surface activity of the surfactant liposomes, but this feature was absent in the presence of SP-A. These data suggest that: 1) antioxidant-surfactant liposomes augment alveolar type II cell antioxidant activity, 2) liposomal uptake is facilitated by the presence of SP-A, and 3) inhibition of surface activity of surfactant by encapsulated antioxidants can be reversed by SP-A.
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Liu, Si-Yen, Sheng-Nan Lo, Wan-Chi Lee, Wei-Chuan Hsu, Te-Wei Lee, and Chih-Hsien Chang. "Evaluation of Nanotargeted 111In-Cyclic RGDfK-Liposome in a Human Melanoma Xenotransplantation Model." International Journal of Molecular Sciences 22, no. 3 (January 22, 2021): 1099. http://dx.doi.org/10.3390/ijms22031099.

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Nanotargeted liposomes may be modified with targeting peptide on the surface of a prepared liposome to endow specificity and elevate targeting efficiency. The aim of this study was to develop a radioactive targeted nanoparticle, the 111In-cyclic RGDfK-liposome, and its advantage of recognizing the αVβ3 integrin was examined. The cyclic RGDfK modified liposomes were demonstrated the ability to bind the αVβ3 integrin expressed on the surface of human melanoma cell in vitro and in vivo. The effects of the cyclic RGDfK-liposome on the functioning of phagocytes was also examined, showing no considerable negative effects on the engulfment of bacteria and the generation of reactive oxygen species. Based upon these findings, the cyclic RGDfK- liposome is said to be a promising agent for tumor imaging.
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25

Cadinoiu, Anca N., Delia M. Rata, Leonard I. Atanase, Oana M. Daraba, Daniela Gherghel, Gabriela Vochita, and Marcel Popa. "Aptamer-Functionalized Liposomes as a Potential Treatment for Basal Cell Carcinoma." Polymers 11, no. 9 (September 18, 2019): 1515. http://dx.doi.org/10.3390/polym11091515.

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More than one out of every three new cancers is a skin cancer, and the large majority are basal cell carcinomas (BCC). Targeted therapy targets the cancer’s specific genes, proteins, or tissue environment that contributes to cancer growth and survival and blocks the growth as well as the spread of cancer cells while limiting damage to healthy cells. Therefore, in the present study AS1411 aptamer-functionalized liposomes for the treatment of BCC were obtained and characterized. Aptamer conjugation increased liposome size, suggesting that the presence of an additional hydrophilic molecule on the liposomal surface increased the hydrodynamic diameter. As expected, the negatively charged DNA aptamer reduced the surface potential of the liposomes. Vertical Franz diffusion cells with artificial membranes were used to evaluate the in vitro release of 5-fluorouracil (5-FU). The aptamer moieties increase the stability of the liposomes and act as a supplementary steric barrier leading to a lower cumulative amount of the released 5-FU. The in vitro cell viability, targeting capability and apoptotic effects of liposomes on the human dermal fibroblasts and on the basal cell carcinoma TE 354.T cell lines were also evaluated. The results indicate that the functionalized liposomes are more efficient as nanocarriers than the non-functionalized ones.
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26

Kumbhar, M. S., and M. C. Singh. "Development and Evaluation of Dapsone Loaded Topical Liposomes." International Journal of Pharmaceutical Sciences and Nanotechnology 7, no. 2 (May 31, 2014): 2441–49. http://dx.doi.org/10.37285/ijpsn.2014.7.2.6.

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Topical liposomal drug delivery is becoming promising system with several advantages like skin deposition, controlled release, targeted action and reduced drug quantity etc. Topical treatments are used for various diseases and disorders. Acne vulgaris is a worldwide skin disease. For acne treatments oral, injectable routes are used but topical route is the better route for site delivery. Dapsone, as antibacterial and anti-inflammatory drug has been recommended in topical acne treatment. Multilamellar vesicles (MLV) of dapsone were prepared using conventional thin film hydration method. Optimization techniques were used to determine, formulation with high drug entrapment efficiency and optimum vesicle size. Soya lecithin and cholesterol were used as independent variables. The prepared liposomes were characterized for size, shape, entrapment efficiency, zeta potential, in-vitro drug release (by Franz diffusion cell) and skin deposition. Maximum entrapment was found to be 33.44%. In skin permeation study, liposomal gels resulted in significantly slower drug release than equivalent plain gels. Liposomal gels were found to have 2-3 fold increase in the skin deposition than plain gel, indicating liposome forms depots in skin layers and thus providing a better option to deal with skin-cited acne vulgaris. Amongst different storage conditions (kept for 2 months), the liposomes stored at 2 to 8 °C were found to be most stable, as compare to room temperature and 45 °C.
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Polkovnikova, Yu A. "Modeling the Formation of Liposomes with Vinpocetine from Soy Lecithin Phospholipids by Molecular Dynamics." Drug development & registration 10, no. 3 (August 28, 2021): 83–87. http://dx.doi.org/10.33380/2305-2066-2021-10-3-83-87.

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Introduction. Liposomal preparations have the following advantages: they protect body cells from the toxic effects of drugs; prolong the action of the drug introduced into the body; protect medicinal substances from degradation; promote the manifestation of targeted specificity due to selective penetration from blood into tissues; change the pharmacokinetics of drugs, increasing their pharmacological effectiveness; allow you to create a water-soluble form of a number of medicinal substances, thereby increasing their bioavailability. The development of liposomal forms of vinpocetine is highly relevant. Currently, when developing the composition of liposomal forms, molecular modeling methods are widely used, which are a convenient method for predicting both the properties of the membranes themselves and aspects of the interaction of membranes with small molecules or proteins.Aim. The aim of this study is to model the process of liposome assembly from soy lecithin phospholipids in the presence of vinpocetine by the molecular dynamics method; as well as predicting the distribution of vinpocetine between the internal cavity of the liposome, the phospholipid membrane, and the dispersion medium based on the simulation results.Materials and methods. To simulate the process of liposome formation, the method of coarse-grained molecular dynamics in a Martini 2.2 force field was used using the Gromacs 2016.4 program. The assembly of the simulated system - a solution of soy lecithin phospholipids in water was performed using the Internet service Charmm-GUI-> Inputgenerator-> Martinimaker-> Randombuilder.Results and discussion. The results of molecular modeling showed that the vinpocetine molecules did not penetrate into the liposome, but were adsorbed on its surface. This is due to the low solubility of vipocetin in the hydrophobic medium of the soy lecithin liposome membrane.Conclusion. It was shown that the minimum diameter of a liposome formed from purified soy lecithin is 15.3 nm. Vinpocetine does not penetrate into liposomes from purified soy lecithin, but is adsorbed on the outer surface of their membrane. The surface excess in this case, according to the results of modeling coarse-grained molecular dynamics at a temperature of 298 K in an alcohol-water medium, is 1.2 • 10-7 mol/m2.
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28

Mishra, Keerti, and Akhlesh K. Jain. "Liposomes: An Emerging Approach for the Treatment of Cancer." Current Pharmaceutical Design 27, no. 20 (August 4, 2021): 2398–414. http://dx.doi.org/10.2174/1381612827666210406141449.

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Background: Conventional drug delivery agents for a life-threatening disease, i.e., cancer, lack specificity towards cancer cells, producing a greater degree of side effects in the normal cells with a poor therapeutic index. These toxic side effects often limit dose escalation of anti-cancer drugs, leading to incomplete tumor suppression/ cancer eradication, early disease relapse, and ultimately, the development of drug resistance. Accordingly, targeting the tumor vasculatures is essential for the treatment of cancer. Objective: To search and describe a safer drug delivery carrier for the treatment of cancer with reduced systemic toxicities. Methods: Data were collected from Medline, PubMed, Google Scholar, Science Direct using the following keywords: ‘liposomes’, ‘nanocarriers’, ‘targeted drug delivery’, ‘ligands’, ‘liposome for anti-cancerous drugs’, ‘treatment for cancer’ and ‘receptor targeting.’ Results: Liposomes have provided a safe platform for the targeted delivery of encapsulated anti-cancer drugs for the treatment of cancer, which results in the reduction of the cytotoxic side effects of anti-cancer drugs on normal cells. Conclusion: Liposomal targeting is a better emerging approach as an advanced drug delivery carrier with targeting ligands for anti-cancer agents.
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29

Mortensen, Joachim Høg, Maria Jeppesen, Linda Pilgaard, Ralf Agger, Meg Duroux, Vladimir Zachar, and Torben Moos. "Targeted Antiepidermal Growth Factor Receptor (Cetuximab) Immunoliposomes Enhance Cellular Uptake In Vitro and Exhibit Increased Accumulation in an Intracranial Model of Glioblastoma Multiforme." Journal of Drug Delivery 2013 (September 23, 2013): 1–13. http://dx.doi.org/10.1155/2013/209205.

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Therapeutic advances do not circumvent the devastating fact that the survival rate in glioblastoma multiforme (GBM) is less than 5%. Nanoparticles consisting of liposome-based therapeutics are provided against a variety of cancer types including GBM, but available liposomal formulations are provided without targeting moieties, which increases the dosing demands to reach therapeutic concentrations with risks of side effects. We prepared PEGylated immunoliposomes (ILs) conjugated with anti-human epidermal growth factor receptor (EGFR) antibodies Cetuximab (α-hEGFR-ILs). The affinity of the α-hEGFR-ILs for the EGF receptor was evaluated in vitro using U87 mg and U251 mg cells and in vivo using an intracranial U87 mg xenograft model. The xenograft model was additionally analyzed with respect to permeability to endogenous albumin, tumor size, and vascularization. The in vitro studies revealed significantly higher binding of α-hEGFR-ILs when compared with liposomes conjugated with isotypic nonimmune immunoglobulin. The uptake and internalization of the α-hEGFR-ILs by U87 mg cells were further confirmed by 3D deconvolution analyses. In vivo, the α-hEGFR-ILs accumulated to a higher extent inside the tumor when compared to nonimmune liposomes. The data show that α-hEGFR-ILs significantly enhance the uptake and accumulation of liposomes in this experimental model of GBM suggestive of improved specific nanoparticle-based delivery.
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30

Wiedenhoeft, Tabea, Tobias Braun, Ronald Springer, Michael Teske, Erik Noetzel, Rudolf Merkel, and Agnes Csiszár. "The Basement Membrane in a 3D Breast Acini Model Modulates Delivery and Anti-Proliferative Effects of Liposomal Anthracyclines." Pharmaceuticals 13, no. 9 (September 19, 2020): 256. http://dx.doi.org/10.3390/ph13090256.

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Breast cancer progression is marked by cancer cell invasion and infiltration, which can be closely linked to sites of tumor-connected basement membrane thinning, lesion, or infiltration. Bad treatment prognosis frequently accompanies lack of markers for targeted therapy, which brings traditional chemotherapy into play, despite its adverse effects like therapy-related toxicities. In the present work, we compared different liposomal formulations for the delivery of two anthracyclines, doxorubicin and aclacinomycin A, to a 2D cell culture and a 3D breast acini model. One formulation was the classical phospholipid liposome with a polyethylene glycol (PEG) layer serving as a stealth coating. The other formulation was fusogenic liposomes, a biocompatible, cationic, three-component system of liposomes able to fuse with the plasma membrane of target cells. For the lysosome entrapment-sensitive doxorubicin, membrane fusion enabled an increased anti-proliferative effect in 2D cell culture by circumventing the endocytic route. In the 3D breast acini model, this process was found to be limited to cells beneath a thinned or compromised basement membrane. In acini with compromised basement membrane, the encapsulation of doxorubicin in fusogenic liposomes increased the anti-proliferative effect of the drug in comparison to a formulation in PEGylated liposomes, while this effect was negligible in the presence of intact basement membranes.
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31

Saito, Atsushi, Hiroaki Shimizu, Yusuke Doi, Tatsuhiro Ishida, Miki Fujimura, Takashi Inoue, Hiroshi Kiwada, and Teiji Tominaga. "Immunoliposomal drug-delivery system targeting lectin-like oxidized low-density lipoprotein receptor–1 for carotid plaque lesions in rats." Journal of Neurosurgery 115, no. 4 (October 2011): 720–27. http://dx.doi.org/10.3171/2011.5.jns10227.

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Object Targeted drug delivery with immunoliposomes has been applied to various in vivo animal models and is newly focused as a novel therapeutic target. Lectin-like oxidized low-density lipoprotein receptor–1 (LOX1) is a potent regulator of systemic atherosclerosis, and the authors focused on its effect on carotid plaques. The authors developed a LOX1-targeted liposomal rho-kinase inhibitor and examined the therapeutic effect on carotid intimal hypertrophy in rats. Methods LOX1-targeted rho-kinase inhibitor fasudil-containing liposomes, composed of hydrogenated soy phosphatidylcholine/cholesterol/PEG2000-DSPE, were prepared by conjugating anti-LOX1 antibodies on the surface and by remote loading of fasudil. Carotid intimal hypertrophy was induced by balloon injury, and the drugs were intravenously administered on Day 3 postinjury. The rats were divided into 4 groups: nontreatment, treatment with intravenous fasudil (2 mg), treatment with liposomal fasudil (2 mg), and treatment with LOX1-targeted liposomal fasudil (2 mg). The authors compared intimal hypertrophy, atherosclerotic factor, and matrix metalloproteinase-9 expression among groups. Results DiI–labeled LOX1-targeted liposomes were prominently observed in the lesions on Day 7 after the surgery. The intimal thickness was significantly reduced in the LOX1-targeted liposomal fasudil–treated group (mean 81.6 ± 13.9 μm) compared with the other groups (no treatment 105.4 ± 16.8 μm; fasudil treatment 102.4 ± 20.0 μm; and liposomal fasudil treatment 102.8 ± 22.2 μm; p = 0.046). Matrix metalloproteinase-9 expression was also significantly reduced in the LOX1-targeted liposomal fasudil group. Conclusions Liposomes conjugated with anti-LOX1 antibody effectively reached carotid artery lesions, and liposomal rho-kinase significantly inhibited intimal hypertrophy. The new liposomal drug delivery system targeting LOX1 may become a therapeutic strategy for atherosclerotic diseases.
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32

Afrakhteh, Moslem, Alireza Kheirollah, Aminollah Pourshohod, Mohammad Ali Ghaffari, Mostafa Jamalan, and Majid Zeinali. "Cytotoxicity of Sodium Arsenite-loaded Anti-HER2 Immunoliposomes Against HER2-expressing Human Breast Cancer Cell Lines." Letters in Drug Design & Discovery 16, no. 5 (April 15, 2019): 556–62. http://dx.doi.org/10.2174/1570180815666180803120409.

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Background: Chemotherapy is a routine approach in treatment of patients with cancer, while side effects of chemotherapeutic drugs are inevitable. To minimize side effects, specific targeting of neoplastic cells is a promising strategy in cancer therapy. Sodium arsenite is a metalloid toxin with anti-neoplastic properties, but low selectivity and carcinogenic activity have limited its clinical usage. Methods: Targeting of HER2-overexpressing (SK-BR-3) and HER2-low expressing (MCF-7) cancerous breast cell lines by two different liposomal forms of sodium arsenite (bare liposome and trastuzumab-conjugated liposome) was investigated in the current study. Levels of HER2 expression in the above mentioned cell lines were confirmed by western blotting. Size and morphology of the constructed liposomes were characterized by atomic force microscopy (AFM) and dynamic light scattering (DLS). Viability of the cells after treatment was assessed using MTT assay. Results: Sodium arsenite in the free and liposomal forms showed growth inhibitory effects against both SK-BR-3 and MCF-7 cell lines in an examined concentration range of 1-20 µM, although this effect was more significant in SK-BR-3 cell line. Loading of sodium arsenite in anti-HER2 immunoliposomes significantly enhanced its cytotoxicity while the specificity was also improved. By encapsulation of sodium arsenite in anti-HER2 immunoliposomes, its efficacy in ablation of SKBR- 3 cells was increased about 1.4-fold compared to the free or liposomal forms. Conclusion: In conclusion, targeted delivery of sodium arsenite using anti-HER2 immunoliposomes can be considered as an alternative strategy for specific treatment of HER2-positive breast cancers.
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33

Shmeeda, H., D. Tzemach, L. Mac, A. Najafi, K. Hjortsvang, and A. Gabizon. "Her2-targeted pegylated stealth liposomal doxorubicin (PLD) retains its specific targeting ability to Her2-expressing tumor cells after in vivo circulation and extravasation to mouse malignant ascites." Journal of Clinical Oncology 24, no. 18_suppl (June 20, 2006): 13097. http://dx.doi.org/10.1200/jco.2006.24.18_suppl.13097.

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13097 Background: Receptor-directed targeting of ligand-bearing liposomes to tumor cells may enhance therapeutic efficacy by intracellular delivery of a concentrated payload of liposomal drug. The goal of this study was to assess whether Her2-targeted PLD retains its binding ability to Her2-expressing target cells through circulation in the blood and extravasation to the ascitic fluid of mice with malignant ascites. Methods: PLD was grafted with a pegylated lipophilic conjugate of an anti-Her2 scFv antibody fragment (F5) at a ratio of 15 ligands per liposome. BALB/c mice were injected with J6456 lymphoma cells into the peritoneal cavity to generate malignant ascites. When abdominal swelling developed, Her2-targeted PLD and nontargeted PLD were injected into the mice i.v. at a dose of 15 mg/kg. The ascitic fluid was collected 48 hr later, ascitic tumor cells were removed, and the doxorubicin levels in the cell-free ascitic fluid and plasma were determined. Binding of the liposome-containing ascitic fluid was tested in vitro against Her2-expressing human tumor cell lines (N87, SKBR-3) and compared to the binding of shelf formulations (not passaged in vivo) of Her2-PLD and PLD, using as parameter the amount of cell-associated doxorubicin. Results: Plasma and ascitic fluid levels of Her2-PLD were only slightly below those of PLD indicating that the Her2 ligand did not cause any significant change in the clearance rate of PLD. Her2-PLD and PLD bound to an equal extent to J6456 cells in vivo. The in vitro binding of Her2-PLD from ascites to Her2- expressing cells was increased 10 to 20-fold above that of PLD from ascites, similarly to the 20-fold difference in binding between shelf Her2-PLD and PLD. Conclusions: Her2-targeted PLD demonstrates similar circulation time to that of nontargeted PLD. After in vivo passage, the targeted liposome retains most of its original binding capacity to Her2 expressing cells indicating that the ligand is stably maintained in association with the doxorubicin liposomal carrier. Targeting of PLD using this Her2 antibody fragment should provide an important means of selective drug delivery to tumors expressing the Her2 receptor. [Table: see text]
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Kelly, Ciara, Caroline Jefferies, and Sally-Ann Cryan. "Targeted Liposomal Drug Delivery to Monocytes and Macrophages." Journal of Drug Delivery 2011 (October 26, 2011): 1–11. http://dx.doi.org/10.1155/2011/727241.

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As the role of monocytes and macrophages in a range of diseases is better understood, strategies to target these cell types are of growing importance both scientifically and therapeutically. As particulate carriers, liposomes naturally target cells of the mononuclear phagocytic system (MPS), particularly macrophages. Loading drugs into liposomes can therefore offer an efficient means of drug targeting to MPS cells. Physicochemical properties including size, charge and lipid composition can have a very significant effect on the efficiency with which liposomes target MPS cells. MPS cells express a range of receptors including scavenger receptors, integrins, mannose receptors and Fc-receptors that can be targeted by the addition of ligands to liposome surfaces. These ligands include peptides, antibodies and lectins and have the advantages of increasing target specificity and avoiding the need for cationic lipids to trigger intracellular delivery. The goal for targeting monocytes/macrophages using liposomes includes not only drug delivery but also potentially a role in cell ablation and cell activation for the treatment of conditions including cancer, atherosclerosis, HIV, and chronic inflammation.
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35

Arroyo-Ariza, Daniel, Elizabeth Suesca, Chad Leidy, and John M. Gonzalez. "Sulfatide-Rich Liposome Uptake by a Human-Derived Neuroblastoma Cell Line." Processes 8, no. 12 (December 8, 2020): 1615. http://dx.doi.org/10.3390/pr8121615.

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Liposomes are bilayer membrane vesicles that can serve as vehicles for drug delivery. They are a good alternative to free drug administration that provides cell-targeted delivery into tumors, limiting the systemic toxicity of chemotherapeutic agents. Previous results from our group showed that an astrocytoma cell line exhibits selective uptake of sulfatide-rich (SCB) liposomes, mediated by the low-density lipoprotein receptor (LDL-R). The goal of this study was to assess the uptake of liposomes in a neuroblastoma cell line. For this purpose, we used two types of liposomes, one representing a regular cell membrane (DOPC) and another rich in myelin components (SCB). An astrocytoma cell line was used as a control. Characterization of liposome uptake and distribution was conducted by flow cytometry and fluorescence microscopy. Similar levels of LDL-R expression were found in both cell lines. The uptake of SCB liposomes was higher than that of DOPC liposomes. No alterations in cell viability were found. SCB liposomes were located near the cell membrane and did not colocalize within the acidic cellular compartments. Two endocytic pathway inhibitors did not affect the liposome uptake. Neuroblastoma cells exhibited a similar uptake of SCB liposomes as astrocytoma cells; however, the pathway involved appeared to be different than the hypothesized pathway of LDL-R clathrin-mediated endocytosis.
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36

Cho, Hea-Young, Chong Ki Lee, and Yong-Bok Lee. "Preparation and Evaluation of PEGylated and Folate-PEGylated Liposomes Containing Paclitaxel for Lymphatic Delivery." Journal of Nanomaterials 2015 (2015): 1–10. http://dx.doi.org/10.1155/2015/471283.

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This study attempted to prepare polyethylene-glycol modified (PEGylated) and folate-PEGylated liposomes containing paclitaxel (Ptx) in order to reduce the toxicity and improve the bioavailability and biocompatibility by targeting drugs to the lymphatics using cancer cell specific ligand folate to prevent metastasis via the lymphatic system. Liposomes were prepared by lipid film hydration method using PEG and folate-PEG as surface modifiers. The mean particle size and encapsulation efficiency of liposomes were114±6.81 nm and81±2.3% for PEGylated liposome and122±4.87 nm and88±2.0% for folate-PEGylated liposome, respectively. According to stability test, it could be confirmed that PEGylated and folate-PEGylated liposomes were stable for at least 5 days. After intravenous administration of the PEGylated and folate-PEGylated liposomes to rats, theCLt(total clearance) andt1/2(half-life) were significantly different (P<0.05) compared with those of PADEXOL Inj. In targeting efficiency, calculated as the concentration ratio of Ptx in lymph nodes and plasma, there was significant increase in targeting efficiency at lymph nodes (P<0.05). From these results, we could conclude that the prepared Ptx-containing PEGylated and folate-PEGylated liposomes are good candidates for the targeted delivery of the drug to lymphatic system.
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37

Baryshnikov, A. Yu. "NANOSTRUCTURED LIPOSOMAL SYSTEMS AS TRANSPORT AGENTS FOR ANTICANCER DRUGS." Annals of the Russian academy of medical sciences 67, no. 3 (March 23, 2012): 23–31. http://dx.doi.org/10.15690/vramn.v67i3.181.

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Liposomes quite recently have turned from a model of biological membranes into an object of extensive research and practical use. The versatile traits of liposomal formulation allow its' universal implementation, especially in cancer chemotherapy. The advantages of liposomal use as a carrier of an anticancer drug for its targeted selective accumulation are discussed in this article. This article contains description of new types of liposomes, differing in contents and use, such as: simple, sterically stabilized, targeted (immunoliposomes),cationic, sensitive to physical and chemical stimuli. The characteristics of liposomal systems of anticancer drug delivery designed at Blokhin Russian Oncological Scientific Centre is given in the article.
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38

Di Paolo, Daniela, Fabio Pastorino, Chiara Brignole, Danilo Marimpietri, Monica Loi, Mirco Ponzoni, and Gabriella Pagnan. "Drug Delivery Systems: Application of Liposomal Anti-Tumor Agents to Neuroectodermal Cancer Treatment." Tumori Journal 94, no. 2 (March 2008): 246–53. http://dx.doi.org/10.1177/030089160809400217.

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Disseminated neuroectoderma-derived tumors, mainly neuroblastoma in childhood and melanoma in the adulthood, are refractory to most current therapeutic regimens and hence the prognosis remains very poor. Preclinical research studies have indicated several agents that show promising therapeutic potential for these neoplasms. However, there appears to be a limitation to their in vivo applicability, mainly due to unfavorable pharmacokinetic properties that lead to insufficient drug delivery to the tumor or metastatic sites or to high systemic or organ-specific toxicity. In this scenario, the focus is on targeted cancer therapy. Encapsulating anticancer drugs in liposomes enables targeted drug delivery to tumor tissue and prevents damage to the normal surrounding tissue. Indeed, sterically stabilized liposomes have been shown to enhance the selective localization of entrapped drugs to solid tumors, with improvements in therapeutic indices. The identification of tumor-associated antigens and/or genes and the relative ease of manipulating the physicochemical features of liposome hold promise for the development of novel therapeutic strategies that selectively target tumor cells. Combined targeting is still investigated, especially the availability to simultaneously target and kill both the cancer cells and the tumor vasculature. Animal models make it possible to link molecular genetics and biochemistry information to the physiological basis of disease and are important predictive tools that offer a frontline testing system for studying the involvement of specific genes and the efficacy of novel therapeutics approaches. Relevant experimental models of human neuroblastoma and melanoma, which better reflect the tumor behavior in patients, are required to evaluate the effectiveness of the various targeted liposomal formulations and their possible systemic and organ-specific toxicity. The most multifunctional targeted liposomes are herein described, with primary attention on testing their efficacy in clinically relevant animal models for the treatment of neuroblastoma and melanoma.
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39

Bonde, Smita, and Sukanya Nair. "ADVANCES IN LIPOSOMAL DRUG DELIVERY SYSTEM: FASCINATING TYPES AND POTENTIAL APPLICATIONS." International Journal of Applied Pharmaceutics 9, no. 3 (May 1, 2017): 1. http://dx.doi.org/10.22159/ijap.2017v9i3.17984.

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Liposomes are an efficient novel drug delivery system. They are used because of their structure which is stable and due to their ability to accommodate both lipophilic and hydrophilic drug. Various fascinating types of liposomes have been developed in recent past to further enhance their utility. Long-circulating liposomes or stealth liposomes are able to hide from the defence system of the body and circulate for a longer time in the blood. Targeted liposomes namely immuno- liposomes consists of antibodies conjugated on their surface to improve the specificity of the cell. Liposomes have been modified as per the conditions of pH and temperature, specifically designed to improve drug delivery to targeted tumor cells. Liposomes are being used in the treatment of various diseases and there are various liposomal drug formulations available today. Liposomes can be used as carriers for genetic materials such as antisense, DNA, RNA which are useful in the treatment of diseases. Liposomes are also efficient carriers of cytokines which further activate macrophages. This review provides the detailed insight of types and applications of liposomes and the potential challenges in the development of liposomal drug delivery systems.
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40

Rahman, Mahfoozur, Sarwar Beg, Amita Verma, Imran Kazmi, Farhan Jalees Ahmed, Vikas Kumar, Firoz Anwar, and Sohail Akhter. "Liposomes as Anticancer Therapeutic Drug Carrier’s Systems: More than a Tour de Force." Current Nanomedicine 10, no. 2 (August 13, 2020): 178–85. http://dx.doi.org/10.2174/2468187309666190618171332.

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A liposome is a spherical vesicle composed of a bilayer of lipid with central aqueous cavity. Liposomes are the first nano vesicular drug delivery carriers, which are successfully translated into real-time clinical application and gained great potential in the past 30 years. The characteristics of liposomes to encapsulate both hydrophilic and hydrophobic drugs, their biocompatibility and biodegradability make it attractive nanocarriers in drug delivery area. Apart from this, great technical advancement has been made to develops second-generation liposomes named as stealth liposomes, cationic liposomes, triggered release liposomes and ligand targeted liposomes. This led to widespread use of liposomes in various areas including anticancer therapeutics, diagnostics and imaging agents. Therefore, the presents review article made an extensive discussion of various liposomes and its applications in cancer treatment.
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41

Di Francesco, Valentina, Martina Di Francesco, Paolo Decuzzi, Roberto Palomba, and Miguel Ferreira. "Synthesis of Two Methotrexate Prodrugs for Optimizing Drug Loading into Liposomes." Pharmaceutics 13, no. 3 (March 4, 2021): 332. http://dx.doi.org/10.3390/pharmaceutics13030332.

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Methotrexate (MTX), a compound originally used as an anticancer drug, has also found applications in a broad variety of autoimmune disorders thanks to its anti-inflammation and immunomodulatory functions. The broad application of MTX is anyway limited by its poor solubility in biological fluids, its poor bioavailability and its toxicity. In addition, encapsulating its original form in nanoformulation is very arduous due to its considerable hydrophobicity. In this work, two strategies to efficiently encapsulate MTX into liposomal particles are proposed to overcome the limitations mentioned above and to improve MTX bioavailability. MTX solubility was increased by conjugating the molecule to two different compounds: DSPE and PEG. These two compounds commonly enrich liposome formulations, and their encapsulation efficiency is very high. By using these two prodrugs (DSPE-MTX and PEG-MTX), we were able to generate liposomes comprising one or both of them and characterized their physiochemical features and their toxicity in primary macrophages. These formulations represent an initial step to the development of targeted liposomes or particles, which can be tailored for the specific application MTX is used for (cancer, autoimmune disease or others).
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42

Klibanov, Alexander L., Ban An Khaw, Naseem Nossiff, Sean M. O'Donnell, Leaf Huang, Mikhail A. Slinkin, and Vladimir P. Torchilin. "Targeting of macromolecular carriers and liposomes by antibodies to myosin heavy chain." American Journal of Physiology-Lung Cellular and Molecular Physiology 261, no. 4 (October 1, 1991): L60—L65. http://dx.doi.org/10.1152/ajplung.1991.261.4.l60.

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Macromolecular carriers and liposomes were covalently coupled to monoclonal antibodies against cardiac myosin heavy chain. Deferoxamine-modified polymers bound tightly with 67Ga and68 Ga radioisotopes. Ternary deferoxamine-polylysine antibody conjugates specifically targeted the radioisotopes to a myosin-coated microplate. Scatchard analysis revealed a high affinity of the conjugate for the target with a Kas of ≈108 M-1. Liposomes that contained immobilized antimyosin antibodies were targeted specifically to the myosin-coated plate. Additional coating of these liposomes with polyethylene glycol reduced specific binding to the target in vitro. However, because of the presence of polyethylene glycol on the surface of liposomes, these liposomes had a long half-life and slowly cleared from the bloodstream after intravenous injection. These immunoliposomes showed up to 16- to 18-fold specific localization to the necrotic areas of the myocardium in rabbits with experimental infarction. antimyosin; chelating polymer; liposome; monoclonal antibody; myocardial infarction; radioimmunoimaging
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43

Klibanov, Alexander L., Ban An Khaw, Naseem Nossiff, Sean M. O'Donnell, Leaf Huang, Mikhail A. Slinkin, and Vladimir P. Torchilin. "Targeting of macromolecular carriers and liposomes by antibodies to myosin heavy chain." American Journal of Physiology-Heart and Circulatory Physiology 261, no. 4 (October 1, 1991): 60–65. http://dx.doi.org/10.1152/ajpheart.1991.261.4.60.

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Macromolecular carriers and liposomes were covalently coupled to monoclonal antibodies against cardiac myosin heavy chain. Deferoxamine-modified polymers bound tightly with 67Ga and 68Ga radioisotopes. Ternary deferoxamine-polylysine antibody conjugates specifically targeted the radioisotopes to a myosin-coated microplate. Scatchard analysis revealed a high affinity of the conjugate for the target with a Kas of ≈108 M-1. Liposomes that contained immobilized antimyosin antibodies were targeted specifically to the myosin-coated plate. Additional coating of these liposomes with polyethylene glycol reduced specific binding to the target in vitro. However, because of the presence of polyethylene glycol on the surface of liposomes, these liposomes had a long half-life and slowly cleared from the bloodstream after intravenous injection. These immunoliposomes showed up to 16- to 18-fold specific localization to the necrotic areas of the myocardium in rabbits with experimental infarction. antimyosin; chelating polymer; liposome; monoclonal antibody; myocardial infarction; radioimmunoimaging
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44

Li, Juanjuan, Mei Yue, Xiaodong Shi, Shunqiao Feng, Ruihong Tang, Xia Zhang, Rong Liu, Ziqin Liu, and Tianyou Wang. "EVALUATION OF ANTI-CANCER ACTIVITY OF SURVIVIN siRNA DELIVERED BY FOLATE RECEPTOR-TARGETED POLYETHYLENE-GLYCOL LIPOSOMES IN K562-BEARING XENOGRAFT MICE." Biomedical Engineering: Applications, Basis and Communications 26, no. 02 (March 12, 2014): 1450026. http://dx.doi.org/10.4015/s1016237214500264.

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Objective: To investigate anti-cancer activity of the novel survivin siRNA Folate Receptor (FR)-targeted Polyethylene-Glycol Liposomes (PEG) liposomes in K562-bearing nude mice. Methods: The leukemia cell line K562 xenograft model was established in balb/c nu/nu mice, and survivin siRNA FR-targeted PEG liposomes was administrated by intraperitoneal (i.p.). The same volume of liposomes was administrated as placebo control. The real time PCR and western blotting were used to examine the knocking down effect. The tumor weight and size in nude mice was measured to evaluate the inhibitory effect in vivo. Results: The expression ratio of survivin mRNA in siRNA group was 0.35 ± 0.1 (survivin/GAPDH) vs. 1.85 ± 0.65 in control group with significant difference (p < 0.05), as well as protein level by western blotting analysis (p < 0.05). The results also showed the novel survivin siRNA liposomes could inhibit the growth of K562 in xenograft model. Conclusion: This novel survivin siRNA FR-targeted PEG liposome delivery system may be a potential gene therapy for the treatment of leukemia.
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45

Sevastre, Ani-Simona, Stefania Carina Baloi, Catalina Elena Cioc, and Alexandu Oprita. "NEW PHARMACEUTICAL DOSAGE FORMS USED IN THE TREATMENT OF BREAST CANCER. LIPOSOMES." Medico Oncology 2, no. 1 (May 25, 2021): 10–24. http://dx.doi.org/10.52701/monc.2021.v2i1.17.

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In order to obtain antineoplastic compounds and innovative formulations, new technologies and testing methods are continuously being developed. Unfortunately, besides cancer cells, chemotherapy also affects normal cells. An option to avoid toxicity is represented by the targeted cancer treatment using novel pharmaceutical dosage forms. Liposomes represent a relatively new pharmaceutical dosage form, used for their many advantages. In this article, the methods of liposomal preparation are mentioned, along with the classification and the latest improvements involving this pharmaceutical form. The bioavailability of conventional liposomes is currently improved by developing photodynamic liposomes, pH or temperature sensitive liposomes and targeted liposomes.
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46

Sawant, Ganesh Shankar, Kiran Vilas Sutar, and Akhil S. Kanekar. "Liposome: A Novel Drug Delivery System." International Journal of Research and Review 8, no. 4 (April 21, 2021): 252–68. http://dx.doi.org/10.52403/ijrr.20210433.

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Liposome is a spherical sac phospholipid molecule. It encloses a water droplet especially as form artificially to carry drug into tissue membrane. It is spherical sac vesicle it consists at least one lipid bilayer. Liposomes are mainly development for drug delivery size and size distribution. The process of sonication (extrusion) is required to obtain small size and narrow size distribution of liposome. The main significant role in formulating of potent drug, improve therapeutic effect. Liposome formulation is mainly design in increasing accumulation at the target site, and then resulting effect is targeted to reduce toxicity. There is various method for liposome formulation depending upon lipid drug interaction liposome disposition mechanism- parameters particle size, charge and surface hydration. Liposome is a nanoparticle (size-100nm). Nanoscale drug delivery system using liposome as well as nanoparticle. This technology is for "Rational delivery of chemotherapeutic" drug treatment of cancer. Liposome is use as to study the cell membrane and cell organelles. The advantages of liposome formation using microfluidic approach for bulk-mixing approaches are discussed. Keywords: liposome, lipid bilayer, sonication, nanoparticles, particle size, toxicity.
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47

Malik, Ritu, Ketan Pancholi, and Andreas Melzer. "Microbubble–liposome conjugate." Nanobiomedicine 3 (January 1, 2016): 184954351667080. http://dx.doi.org/10.1177/1849543516670806.

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Liposome–microbubble conjugates are considered as better targeted drug delivery vehicles compared to microbubbles alone. The microbubble in the integrated drug delivery system delivers the drug intracellularly on the target, whereas the liposome component allows loading of high drug dose and extravasation through leaky vasculature. In this work, a new high yielding microbubble production method was used to prepare microbubbles for formulation of the liposome-conjugated drug delivery system. In formulation process, the prepared liposome of 200 nm diameter was attached to the microbubble surface using the avidin–biotin interaction. The analysis of the confocal scanning laser microscope images showed that approximately 8 × 108 microbubbles per millilitre (range: 2–7 μm, mean size 5 ± 0.5 μm) can be efficiently conjugated to the liposomes. The method of conjugation was found to be effective in attaching liposome to microbubbles.
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48

Banerjee, Goutam, Swapna Medda, and Mukul K. Basu. "A Novel Peptide-Grafted Liposomal Delivery System Targeted to Macrophages." Antimicrobial Agents and Chemotherapy 42, no. 2 (February 1, 1998): 348–51. http://dx.doi.org/10.1128/aac.42.2.348.

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ABSTRACT The interaction of chemotactic peptide (e.g., fMet-Leu-Phe)-grafted liposomes with macrophages is noted to be rapid and specific. At a grafted peptide concentration of 100 nmol, internalization of the peptide-grafted liposomes by the macrophages is found to reach equilibrium in 30 min. The peptide alone and the peptide-grafted empty liposomes are found to show moderate antileishmanial activity in vitro. Primaquine, which is known to generate O2 − in phagocytic cells, showed leishmanicidal properties when it was tested in vitro against parasite-infected macrophages over a certain range of concentrations. It showed much better efficacy against experimental leishmaniasis when it was used in the fMet-Leu-Phe-grafted liposomal form in comparison with its efficacy when it was either in the free form or encapsulated in ungrafted liposomes. The conventional toxicity parameters (e.g., blood pathology and tissue histology-specific enzyme levels related to normal liver function) are found to be very close to normal when fMet-Leu-Phe-grafted liposomal primaquine is used. The biodegradabilities of both the drug and the delivery systems are also found to be very satisfactory. Thus, this delivery system may have possible applications for the treatment of leishmaniasis as well as other macrophage-associated disorders.
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49

Ashrafzadeh, Maryam Sadat, Amir Heydarinasab, Azim Akbarzadeh, and Mehdi Ardjmand. "In Vitro Characteristics of Glioma Cells Targeting by OX26-modified Liposomal Cisplatin." Letters in Drug Design & Discovery 17, no. 9 (September 11, 2020): 1126–38. http://dx.doi.org/10.2174/1570180817999200330165213.

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Background: Drug delivery to the brain tumor is limited due to the presence of the blood-brain barrier (BBB). Objective: This study aimed to evaluate the therapeutic effects of cisplatin-loaded PEGylated liposomes, targeted with the OX26 antibody (targeted liposomal cisplatin) against transferrin receptor expressing rat glioma C6 cells in vitro. Method: The liposomes were synthesized using reverse phase evaporation method and were conjugated to the OX26 monoclonal antibody. They were characterized in terms of size, drug encapsulation efficiency, morphology and drug release experiments using dynamic light scattering, atomic absorption spectrometry, scanning electron microscopy, and dialysis membrane methods. Then, their biological activities were evaluated on targeting the BBB. Results: The characterization results showed that spherical nanodrug with a size of 157 nm and drug loading efficiency of 24% was synthesized, which released 64% of the loaded cisplatin after 72 h in a controlled release manner. The nanoparticles caused an increase in the cisplatin cytotoxicity effects by 1.7-, 1.8- and 1.8-fold, compared to cisplatin-loaded PEGylated liposomes (liposomal cisplatin) after 24, 48 and 72h incubation, respectively against C6 cells. Moreover, targeted liposomal cisplatin showed promising results in the transport of cisplatin across the BBB, in which it caused an increase in the cisplatin cytotoxicity on C6 cells by 2.7- and 2.4-fold, compared to cisplatin and liposomal cisplatin, respectively. Conclusion: Regarding the properties of the targeted liposomal cisplatin, it suggests that the potency of the formulation, to be evaluated, for the transport of cisplatin across the BBB, delivers it to the brain tumor in vivo.
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Yuba, Eiji, Yoshiki Fukaya, Shin Yanagihara, Nozomi Kasho, and Atsushi Harada. "Development of Mannose-Modified Carboxylated Curdlan-Coated Liposomes for Antigen Presenting Cell Targeted Antigen Delivery." Pharmaceutics 12, no. 8 (August 11, 2020): 754. http://dx.doi.org/10.3390/pharmaceutics12080754.

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Specific delivery to antigen presenting cells (APC) and precise control of the intracellular fate of antigens are crucial to induce cellular immunity that directly and specifically attacks cancer cells. We previously achieved cytoplasmic delivery of antigen and activation of APC using carboxylated curdlan-modified liposomes, which led to the induction of cellular immunity in vivo. APCs express mannose receptors on their surface to recognize pathogen specifically and promote cross-presentation of antigen. In this study, mannose-residue was additionally introduced to carboxylated curdlan as a targeting moiety to APC for further improvement of polysaccharide-based antigen carriers. Mannose-modified curdlan derivatives were synthesized by the condensation between amino group-introduced mannose and carboxy group in pH-sensitive curdlan. Mannose residue-introduced carboxylated curdlan-modified liposomes showed higher pH-sensitivity than that of liposomes modified with conventional carboxylated curdlan. The introduction of mannose-residue to the liposomes induced aggregation in the presence of Concanavalin A, indicating that mannose residues were presented onto liposome surface. Mannose residue-introduced carboxylated curdlan-modified liposomes exhibited high and selective cellular association to APC. Furthermore, mannose residue-introduced carboxylated curdlan-modified liposomes promoted cross-presentation of antigen and induced strong antitumor effects on tumor-bearing mice. Therefore, these liposomes are promising as APC-specific antigen delivery systems for the induction of antigen-specific cellular immunity.
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