Journal articles: 'Lipid nanoparticles loaded with drugs'

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Severino, Patrícia, Tatiana Andreani, Ana Sofia Macedo, Joana F. Fangueiro, Maria Helena A. Santana, Amélia M. Silva, and Eliana B. Souto. "Current State-of-Art and New Trends on Lipid Nanoparticles (SLN and NLC) for Oral Drug Delivery." Journal of Drug Delivery 2012 (November 24, 2012): 1–10. http://dx.doi.org/10.1155/2012/750891.

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Lipids and lipid nanoparticles are extensively employed as oral-delivery systems for drugs and other active ingredients. These have been exploited for many features in the field of pharmaceutical technology. Lipids usually enhance drug absorption in the gastrointestinal tract (GIT), and when formulated as nanoparticles, these molecules improve mucosal adhesion due to small particle size and increasing their GIT residence time. In addition, lipid nanoparticles may also protect the loaded drugs from chemical and enzymatic degradation and gradually release drug molecules from the lipid matrix into blood, resulting in improved therapeutic profiles compared to free drug. Therefore, due to their physiological and biodegradable properties, lipid molecules may decrease adverse side effects and chronic toxicity of the drug-delivery systems when compared to other of polymeric nature. This paper highlights the importance of lipid nanoparticles to modify the release profile and the pharmacokinetic parameters of drugs when administrated through oral route.

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Gallarate, Marina, Luigi Battaglia, E. Peira, and Michele Trotta. "Peptide-Loaded Solid Lipid Nanoparticles Prepared through Coacervation Technique." International Journal of Chemical Engineering 2011 (2011): 1–6. http://dx.doi.org/10.1155/2011/132435.

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Stearic acid solid lipid nanoparticles were prepared according to a new technique, called coacervation. The main goal of this experimental work was the entrapment of peptide drugs into SLN, which is a difficult task, since their chemical characteristics (molecular weight, hydrophilicity, and stability) hamper peptide-containing formulations. Insulin and leuprolide, chosen as model peptide drugs, were encapsulated within nanoparticles after hydrophobic ion pairing with anionic surfactants. Peptide integrity was maintained after encapsulation, and nanoparticles can actin vitroas a sustained release system for peptide.

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Bandgar, Sandip Akaram, Pranali Dhavale, Pravin Patil, Sardar Shelake, and Shitalkumar Patil. "Formulation and evaluation of prazosin hydrochloride loaded solid lipid nanoparticles." Journal of Drug Delivery and Therapeutics 8, no. 6-s (December 15, 2018): 63–69. http://dx.doi.org/10.22270/jddt.v8i6-s.2170.

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Solid Lipid Nanoparticles (SLN) are rapidly developing field of nanotechnology with several potential application in drug delivery and research. Drugs having low aqueous solubility not only give low oral bioavailability but provide high inter-and intra subject variability. The purpose of the present study was to investigate the bioavailability enhancement of Prazosin Hydrochloride drug by formulating solid lipid nanoparticle. Prazosin Hydrochloride Drug is an antihypertensive drug with limited bioavailability so that solid lipid nanoparticle (SLN) is one of the approaches to improve bioavailability. SLN were prepared using glyceryl monostearate by hot homogenization followed by Solvent emulsification-ultrasonication. Prazosin Hydrochloride loaded SLN were characterized and optimized by parameters like particle size, zeta potential, XRD, DSC. Proposing Hydrochloride loaded SLN having the particle size 263.8±1.88 and entrapment efficiency 89.29±0.65% shows better bioavailability and optimum stability in studies. The SLN studies prepared using glyceryl mono stearate as a lipid and Polaxamer 407 as a polymer leads to improve bioavailability of the drug. Keywords: Prazosin Hydrochloride, Solid Lipid Nanoparticles, Entrapment efficiency, DSC

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P, Ashok Kumar, Mancy S.P., Manjunath K, Suresh V. Kulkarni, and Jagadeesh R. "Formulation and Evaluation of Fluvoxamine Maleate Loaded Lipid Nanoparticle." International Journal of Pharmaceutical Sciences and Nanotechnology 12, no. 4 (July 31, 2019): 4593–600. http://dx.doi.org/10.37285/ijpsn.2019.12.4.5.

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Recently solid lipid nanoparticles (SLN's) have been received much attention by the researchers owing to its biodegradability, bioavailability and the ability to deliver wide range of drugs to the targeted site of action. The purpose of the present study is to develop and evaluate the fluvoxamine maleate loaded lipid nanoparticles. The fluvoxamine maleate lipid nanoparticles (LN’s) were prepared by the hot melt homogenization followed by the sonication by using different combination of lipids like tristearin, compritol, olive oil, coconut oil, sesame oil. Compatibility study was confirmed by FTIR and DSC. The LN’s were evaluated for particle size, PDI, zeta potential, entrapment efficiency and in-vitro drug release. For the Fluvoxamine maleate LN’s prepared using the solid lipids, the particle size ranged from 98.58 to 152.43 nm. PDI of all formulations were good within the range of 0.239 to 0.456 with zeta potential from - 6.52 to -18.6 mV. Entrapment efficiency observed was in the range of 64.56 to 84.23 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 46.14 to 81.48%. For the formulations prepared using the combination of solid lipids and liquid lipids, Fluvoxamine maleate LN’s the particle size ranged from 63.22 to 263.8 nm. With good PDI range from 0.229 to 0.514 Zeta potential of all formulation is from - 5.01 to -9.30 mV. Entrapment efficiency observed was in the range of 71.02 to 90.51 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 63.71 to 85.41% depending upon the drug lipid ratio, the type of lipid used. The release kinetic studies showed that the release was first order, diffusion controlled, and the ‘n’ values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Anomalous (non-Fickian) diffusion type.

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Nithya, R., K. Siram, R. Hariprasad, and H. Rahman. "Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles." Current Nanomedicine 9, no. 1 (March 15, 2019): 76–85. http://dx.doi.org/10.2174/2405461503666180518093824.

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Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations. Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells. Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line. Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

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Borderwala, Kruti, Ganesh Swain, Namrata Mange, Jaimini Gandhi, Manisha Lalan, Gautam Singhvi, and Pranav Shah. "Optimization of Solid Lipid Nanoparticles of Ezetimibe in Combination with Simvastatin Using Quality by Design (QbD)." Nanoscience & Nanotechnology-Asia 10, no. 4 (August 26, 2020): 404–18. http://dx.doi.org/10.2174/2210681209666190218143736.

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Background: The objective of this study was to develop solid lipid nanoparticles (SLNs) of poorly water soluble anti-hyperlipidemic drugs-Ezetimibe in combination with Simvastatin. Methods: This study describes a 32 full factorial experimental design to optimize the formulation of drug loaded lipid nanoparticles (SLN) by the high speed homogenization technique. The independent variables amount of lipid (GMS) and amount of surfactant (Poloxamer 188) were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables- particle size, % entrapment efficiency (%EE) and cumulative drug release (% CDR) at 24 h. Results: The particle size, % EE and % CDR at 24 h for the 9 batches (B1 to B9) showed a wide variation of 104.6-496.6 nm, 47.80-82.05% (Simvastatin); 48.60-84.23% (Ezetimibe) and 54.64-92.27% (Simvastatin); 43.8-97.1% (Ezetimibe), respectively. The responses of the design were analysed using Design Expert 10.0.2. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw response surface plots. From the statistical analysis of data, polynomial equations were generated. Optimized formulation showed particle size of 169.5 nm, % EE of 75.43% (Simvastatin); 79.10% (Ezetimibe) and 74.13% (Simvastatin); 77.11% (Ezetimibe) %CDR after 24 h. Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilisation of drugs within lipid matrix. Conclusion: Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size approximately around 100 nm.

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Yu, Huang-Ping, Ibrahim A. Aljuffali, and Jia-You Fang. "Injectable Drug-Loaded Nanocarriers for Lung Cancer Treatments." Current Pharmaceutical Design 23, no. 3 (February 20, 2017): 481–94. http://dx.doi.org/10.2174/1381612822666161027113654.

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Different types of injectable nanoparticles, including metallic nanoparticles, polymeric nanocarriers, dendrimers, liposomes, niosomes, and lipid nanoparticles, have been employed to load drugs for lung delivery. Nanoparticles used for lung delivery offer some benefits over conventional formulations, including increased solubility, enhanced stability, improved epithelium permeability and bioavailability, prolonged half-life, tumor targeting, and minimal side effects. In recent years, the concept of using injectable nanocarriers as vehicles for drug delivery has attracted increasing attention. This review highlights recent developments using nanomedical approaches for drug targeting to the lungs. We systematically introduce the concepts and amelioration mechanisms of the nanomedical techniques for lung cancer therapy. Passive targeting by modulating the nanoparticulate structure and the physicochemical properties is an option for efficient drug delivery to the lungs. In addition, active targeting such as antibody or peptide conjugation to nanoparticles is another efficient way to deliver the drugs to the targeted site. This review describes various nanocarriers loaded with anticancer drugs for passive or active targeting of lung malignancy. In this review, we principally focus on the nanomedical application in animal studies. The article excludes investigations limited to cell-based experiments. The review ends by anticipating future developments and trends.

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Pan, Bin, Peipei Li, Jing Chen, Jian Sun, and Na Huang. "Study on the Effect and Mechanism of Paclitaxel-Succinic Acid Drug-Loaded Nanofibers in Treating Lung Cancer." Journal of Nanoscience and Nanotechnology 21, no. 2 (February 1, 2021): 909–13. http://dx.doi.org/10.1166/jnn.2021.18649.

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In recent years, nanotechnology has made great progress in the development and application of tumor detection, diagnosis, and treatment, and eventually formed a “tumor nanomedicine.” The emerging field of “materials.” Nanoparticles have attracted much attention because they can overcome physiological barriers, effectively deliver hydrophobic drugs, and specifically target tumor tissues. At present, nanomedicines mainly include lipid nanoparticles, polymer nanoparticles granules, gold nanoparticles, magnetic nanoparticles, mesoporous silica, and other dosage forms. The use of nanomaterials as carriers in the treatment of lung cancer has unique advantages in achieving targeted drug delivery, slow-release drugs, and improvement of poorly soluble drugs and peptide drugs show obvious advantages in terms of bioavailability and reduction of adverse reactions, and have broad research and development prospects. This paper reports a new type of self-assembled Ptx-SA drug-loaded nanometers based on the carrier-free concept fiber, and it was found that the drug-loaded fiber has better cellophilicity, anti-tumor effect in vitro and in vivo than naked drug, and may be mediated by regulating the expression of related proteins. Therefore, the paclitaxel-loaded nano drug delivery system serves as a new type of nano preparation for treating lung cancer is worth further research.

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Snipstad, Sofie, Sigurd Hanstad, Astrid Bjørkøy, Ýrr Mørch, and Catharina de Lange Davies. "Sonoporation Using Nanoparticle-Loaded Microbubbles Increases Cellular Uptake of Nanoparticles Compared to Co-Incubation of Nanoparticles and Microbubbles." Pharmaceutics 13, no. 5 (April 30, 2021): 640. http://dx.doi.org/10.3390/pharmaceutics13050640.

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Therapeutic agents can benefit from encapsulation in nanoparticles, due to improved pharmacokinetics and biodistribution, protection from degradation, increased cellular uptake and sustained release. Microbubbles in combination with ultrasound have been shown to improve the delivery of nanoparticles and drugs to tumors and across the blood-brain barrier. Here, we evaluate two different microbubbles for enhancing the delivery of polymeric nanoparticles to cells in vitro: a commercially available lipid microbubble (Sonazoid) and a microbubble with a shell composed of protein and nanoparticles. Various ultrasound parameters are applied and confocal microscopy is employed to image cellular uptake. Ultrasound enhanced cellular uptake depending on the pressure and duty cycle. The responsible mechanisms are probably sonoporation and sonoprinting, followed by uptake, and to a smaller degree enhanced endocytosis. The use of commercial Sonazoid microbubbles leads to significantly lower uptake than when using nanoparticle-loaded microbubbles, suggesting that proximity between cells, nanoparticles and microbubbles is important, and that mainly nanoparticles in the shell are taken up, rather than free nanoparticles in solution.

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Ruckmani, K., M. Sivakumar, and P. A. Ganeshkumar. "Methotrexate Loaded Solid Lipid Nanoparticles (SLN) for Effective Treatment of Carcinoma." Journal of Nanoscience and Nanotechnology 6, no. 9 (September 1, 2006): 2991–95. http://dx.doi.org/10.1166/jnn.2006.457.

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Solid Lipid Nanoparticles (SLN) containing Methotrexate (MTX), an anticancer drug for intravenous administration was formulated and characterized. The SLN dispersions with MTX, stearic acid, and soya lecithin in the ratio of 1:4:1, 1:4:1.5, and 1:4:2, sodium taurodeoxycholate and distilled water were prepared by micro emulsification solidification method. The results show that the prepared MTX-SLN particles (with MTX–Stearic acid–Soya lecithin—1:4:2) have an average size of 270 nm with 51.3% drug entrapment. The in vitro-release was attained up to 15th h. The pharmacokinetic studyreveals that the half-life and MRT of SLNs were higher than MTX solution. The life span of EAC (Ehrlich Ascite Carcinoma) bearing mice was increased when treated with MTX-SLNs (Methotrexate nanoparticles). These results clearly indicate that SLNs are a promising sustained release drug targeting system for lipophilic antitumour drugs.

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Amekyeh, Hilda, and Nashiru Billa. "Lyophilized Drug-Loaded Solid Lipid Nanoparticles Formulated with Beeswax and Theobroma Oil." Molecules 26, no. 4 (February 9, 2021): 908. http://dx.doi.org/10.3390/molecules26040908.

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Solid lipid nanoparticles (SLNs) have the potential to enhance the systemic availability of an active pharmaceutical ingredient (API) or reduce its toxicity through uptake of the SLNs from the gastrointestinal tract or controlled release of the API, respectively. In both aspects, the responses of the lipid matrix to external challenges is crucial. Here, we evaluate the effects of lyophilization on key responses of 1:1 beeswax–theobroma oil matrix SLNs using three model drugs: amphotericin B (AMB), paracetamol (PAR), and sulfasalazine (SSZ). Fresh SLNs were stable with sizes ranging between 206.5–236.9 nm. Lyophilization and storage for 24 months (4–8 °C) caused a 1.6- and 1.5-fold increase in size, respectively, in all three SLNs. Zeta potential was >60 mV in fresh, stored, and lyophilized SLNs, indicating good colloidal stability. Drug release was not significantly affected by lyophilization up to 8 h. Drug release percentages at end time were 11.8 ± 0.4, 65.9 ± 0.04, and 31.4 ± 1.95% from fresh AMB-SLNs, PAR-SLNs, and SSZ-SLNs, respectively, and 11.4 ± 0.4, 76.04 ± 0.21, and 31.6 ± 0.33% from lyophilized SLNs, respectively. Thus, rate of release is dependent on API solubility (AMB < SSZ < PAR). Drug release from each matrix followed the Higuchi model and was not affected by lyophilization. The above SLNs show potential for use in delivering hydrophilic and lipophilic drugs.

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Kaur, Harjeet, Baldeep Kumar, Amitava Chakrabarti, Bikash Medhi, Manish Modi, Bishan Dass Radotra, Ritu Aggarwal, and Vivek Ranjan Sinha. "A New Therapeutic Approach for Brain Delivery of Epigallocatechin Gallate: Development and Characterization Studies." Current Drug Delivery 16, no. 1 (November 27, 2018): 59–65. http://dx.doi.org/10.2174/1567201815666180926121104.

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Background: Blood-brain permeability is the primary concern when dealing with the biodistribution of drugs to the brain in neurological diseases. Objective: The purpose of the study is to develop the nanoformulation of Epigallocatechin gallate (EGCG) in order to improve its bioavailability and penetration into the brain. Methods: EGCG loaded Solid Lipid Nanoparticles (SLNs) have been developed using microemulsification method and pharmacological assessments were performed. Results: Surface morphology and micromeritics analysis showed the successful development of EGCG loaded solid lipid nanoparticles with an average size of 162.4 nm and spherical in shape. In vitro release studies indicated a consistent and slow drug release. Pharmacological evaluation of SLN-EGCG demonstrated a significant improvement in cerebral ischemia-induced memory impairment. Conclusion: The results indicate that the EGCG loaded SLNs provide a potential drug delivery system for improved delivery of EGCG to the brain, hence, enhancing its brain bioavailability.

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Pavaloiu, Ramona-Daniela, Fawzia Sha’at, Georgeta Neagu, Radu Albulescu, Mousa Sha’at, Cristina Hlevca, Gheorghe Nechifor, and Daniela Berger. "In Vitro Cytotoxicity of Polymeric Nanoparticles Coated with Lipid Layer Loaded with Cardiovascular Drugs." Proceedings 57, no. 1 (November 9, 2020): 9. http://dx.doi.org/10.3390/proceedings2020057009.

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Shah, Rohan M., Daniel S. Eldridge, Enzo A. Palombo, and Ian H. Harding. "Microwave-assisted formulation of solid lipid nanoparticles loaded with non-steroidal anti-inflammatory drugs." International Journal of Pharmaceutics 515, no. 1-2 (December 2016): 543–54. http://dx.doi.org/10.1016/j.ijpharm.2016.10.054.

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Sonawane, Rahul, Harshad Harde, Mahesh Katariya, Satyam Agrawal, and Sanyog Jain. "Solid lipid nanoparticles-loaded topical gel containing combination drugs: an approach to offset psoriasis." Expert Opinion on Drug Delivery 11, no. 12 (July 31, 2014): 1833–47. http://dx.doi.org/10.1517/17425247.2014.938634.

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Cervantes, Blanca, Lide Arana, Silvia Murillo-Cuesta, Marina Bruno, Itziar Alkorta, and Isabel Varela-Nieto. "Solid Lipid Nanoparticles Loaded with Glucocorticoids Protect Auditory Cells from Cisplatin-Induced Ototoxicity." Journal of Clinical Medicine 8, no. 9 (September 14, 2019): 1464. http://dx.doi.org/10.3390/jcm8091464.

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Cisplatin is a chemotherapeutic agent that causes the irreversible death of auditory sensory cells, leading to hearing loss. Local administration of cytoprotective drugs is a potentially better option co-therapy for cisplatin, but there are strong limitations due to the difficulty of accessing the inner ear. The use of nanocarriers for the efficient delivery of drugs to auditory cells is a novel approach for this problem. Solid lipid nanoparticles (SLNs) are biodegradable and biocompatible nanocarriers with low solubility in aqueous media. We show here that stearic acid-based SLNs have the adequate particle size, polydispersity index and ζ-potential, to be considered optimal nanocarriers for drug delivery. Stearic acid-based SLNs were loaded with the fluorescent probe rhodamine to show that they are efficiently incorporated by auditory HEI-OC1 (House Ear Institute-Organ of Corti 1) cells. SLNs were not ototoxic over a wide dose range. Glucocorticoids are used to decrease cisplatin-induced ototoxicity. Therefore, to test SLNs’ drug delivery efficiency, dexamethasone and hydrocortisone were tested either alone or loaded into SLNs and tested in a cisplatin-induced ototoxicity in vitro assay. Our results indicate that the encapsulation in SLNs increases the protective effect of low doses of hydrocortisone and lengthens the survival of HEI-OC1 cells treated with cisplatin.

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Maretti, Rustichelli, Lassinantti Gualtieri, Costantino, Siligardi, Miselli, Buttini, et al. "The Impact of Lipid Corona on Rifampicin Intramacrophagic Transport Using Inhaled Solid Lipid Nanoparticles Surface-Decorated with a Mannosylated Surfactant." Pharmaceutics 11, no. 10 (October 1, 2019): 508. http://dx.doi.org/10.3390/pharmaceutics11100508.

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The mimicking of physiological conditions is crucial for the success of accurate in vitro studies. For inhaled nanoparticles, which are designed for being deposited on alveolar epithelium and taken up by macrophages, it is relevant to investigate the interactions with pulmonary surfactant lining alveoli. As a matter of fact, the formation of a lipid corona layer around the nanoparticles could modulate the cell internalization and the fate of the transported drugs. Based on this concept, the present research focused on the interactions between pulmonary surfactant and Solid Lipid Nanoparticle assemblies (SLNas), loaded with rifampicin, an anti-tuberculosis drug. SLNas were functionalized with a synthesized mannosylated surfactant, both alone and in a blend with sodium taurocholate, to achieve an active targeting to mannose receptors present on alveolar macrophages (AM). Physico-chemical properties of the mannosylated SLNas satisfied the requirements relative to suitable respirability, drug payload, and AM active targeting. Our studies have shown that a lipid corona is formed around SLNas in the presence of Curosurf, a commercial substitute of the natural pulmonary surfactant. The lipid corona promoted an additional resistance to the drug diffusion for SLNas functionalized with the mannosylated surfactant and this improved drug retention within SLNas before AM phagocytosis takes place. Moreover, lipid corona formation did not modify the role of nanoparticle mannosylation towards the specific receptors on MH-S cell membrane.

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Saporito, Francesca, Giuseppina Sandri, Maria Cristina Bonferoni, Silvia Rossi, Cinzia Boselli, Antonia Icaro Cornaglia, Barbara Mannucci, Pietro Grisoli, Barbara Vigani, and Franca Ferrari. "Essential oil-loaded lipid nanoparticles for wound healing." International Journal of Nanomedicine Volume 13 (December 2017): 175–86. http://dx.doi.org/10.2147/ijn.s152529.

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Sha, Huizi, Hong Chen, and Baorui Liu. "Lipid-insertion to enable targeting functionalization of paclitaxel loaded erythrocyte membrane nanoparticle by tumor-penetrating bispecific recombinant protein." Journal of Clinical Oncology 35, no. 15_suppl (May 20, 2017): e14047-e14047. http://dx.doi.org/10.1200/jco.2017.35.15_suppl.e14047.

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e14047 Background: There is a great interest in targeting and penetrating of cancer cells for research or therapeutic purposes. Red blood cells (RBCs) are readily available and fully biocompatible long-circulating intravascular carriers that are amenable to chemical modifications, drug loading and reinjection. The purpose of this study was to design a tumor-targeting biocompatible drug delivery system for delivery of antitumor drugs. Methods: DSPE-PEG-MAL, phospholipid derivatives was used to insert into erythrocyte membrane nanoparticles. To make nanoparticles active targeting to the tumor site, a tumor-penetrating bispecific recombinant protein named anti-EGFR-iRGD was used. The characterization, bio-distribution, tumor targeting ability and antitumor activity of paclitaxel loaded anti-EGFR-iRGD modified erythrocyte membrane nanoparticle were evaluated. Results: In this study, anti-EGFR-iRGD-RBC-PTX nanoparticles was successfully constructed with a size of around 100 nm. A lipid-insertion method is employed to functionalize these nanoparticles without the need for direct chemical conjugation. It showed signifcantly targeted skill and increased cytotoxic effect toward both nontargeted RBC-PTX and combination of anti-EGFR-iRGD and RBC-PTX. The tissue distribution and antitumor assays in mice bearing gastric cancer xenograft confrmed the superior penetration tumor effcacy and antitumor activity of anti-EGFR-iRGD-RBC-PTX. Conclusions: We designed and successfully prepared a novel anti-EGFR-iRGD decorated, erythrocyte membrane sourced nanoparticle for targeted drug delivery, with enhanced tumor targeting and anti-tumor effect. Anti-EGFR-iRGD-RBC-PTX represents a potential effective nanomedicine against gastric cancer.

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Arana, Lide, Laura Bayón-Cordero, Laura Sarasola, Miren Berasategi, Sandra Ruiz, and Itziar Alkorta. "Solid Lipid Nanoparticles Surface Modification Modulates Cell Internalization and Improves Chemotoxic Treatment in an Oral Carcinoma Cell Line." Nanomaterials 9, no. 3 (March 20, 2019): 464. http://dx.doi.org/10.3390/nano9030464.

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Solid lipid nanoparticles (SLN) present low toxicity, versatility to incorporate both lipophilic and hydrophilic drugs, controlled drug release and they are easy to scale-up. It is well known that the endocytosis pathway by which SLN are taken up and the subsequent subcellular distribution are crucial for the biological effect of the incorporated drug. In addition, interactions between SLN and cells depend on many factors, such as, the composition of nanoparticle surface. In this work different amounts of phosphatidylethanolamine polyethylene glycol (PE–PEG) were added to SLN composed of stearic acid, Epikuron 200 and sodium taurodeoxycholate. Characterization of obtained nanoparticle suspensions were performed by the analysis of particle size, polydispersity index, ζ-potential, cell toxicity and cell internalization pathway. We have observed that the presence of PE–PEG improves active cell internalization of the nanoparticles in an oral adenocarcinoma cell line, reducing non-specific internalization mechanisms. Finally, we have tested the effect of surface coating on the efficiency of incorporated drugs using all-trans retinoic acid as a model drug. We have observed that delivery of this drug into PE–PEG coated SLN increases its chemotoxic effect compared to non-coated SLN. Therefore, it can be concluded that surface modification with PE–PEG improves the efficiency and the specificity of the SLN-loaded drug.

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Krishnam Raju, Kovoru, Beeravelli Sudhakar, and Kolapalli Venkata Ramana Murthy. "Factorial Design Studies and Biopharmaceutical Evaluation of Simvastatin Loaded Solid Lipid Nanoparticles for Improving the Oral Bioavailability." ISRN Nanotechnology 2014 (February 13, 2014): 1–8. http://dx.doi.org/10.1155/2014/951016.

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Statins are HMG-CoA reductase inhibitors, which lower the cholesterol level through reversible and competitive inhibition; they are involved in the biosynthesis of cholesterol and other sterols. Simvastatin exhibits poor oral bioavailability (<5%) and undergoes extensive microsomal metabolism by CYP enzymes. CYP3A4 is the major metabolizing enzyme that metabolizes lactone form of simvastatin and significantly lowers intestinal uptake. The hydrophobic properties of simvastatin prevent complete dissolution of the drug in the intestinal fluid which also contributes to its lower bioavailability. SLNs are alternative carrier system to polymeric nanoparticles. SLNs are in submicron size range (1–1000 nm). To overcome the hepatic first pass metabolism and to enhance the bioavailability, intestinal lymphatic transport of drugs can be exploited. In the present study, attempt has been made to prepare solid lipid nanoparticles of simvastatin to improve the bioavailability. SLNs of simvastatin were prepared with Trimyristin by hot homogenization followed by ultrasonication method. The SLNs were characterized for various physicochemical properties and analytical techniques like PXRD, DSC to study thermal nature and morphology of formulation and excipients. Promising results of the study indicated the applicability of simvastatin solid lipid nanoparticles as potential tools for improvement of bioavailability of poorly soluble drugs.

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Musika, Jidapa, and Nuannoi Chudapongse. "Development of Lipid-Based Nanocarriers for Increasing Gastrointestinal Absorption of Lupinifolin." Planta Medica 86, no. 05 (January 31, 2020): 364–72. http://dx.doi.org/10.1055/a-1095-1129.

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AbstractLupinifolin, a plant flavonoid, has been reported to possess various pharmacological effects. It most likely exerts low oral bioavailability because of poor water solubility. The objective of this study was to develop lipid nanocarriers as drug delivery systems to increase the gastrointestinal absorption of lupinifolin extracted from Albizia myriophylla. Three types of nanocarriers, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were prepared by an emulsification-sonication technique. All three types of nanocarriers loaded with lupinifolin, lupinifolin-loaded solid lipid nanoparticles, lupinifolin-loaded nanostructured lipid carriers, and lupinifolin-loaded nanoemulsions, were successfully synthesized. The lipid components chosen to formulate nanocarriers were tripalmitin and/or medium chain triglyceride. Physicochemical characterizations along with releasing profiles of lupinifolin-loaded lipid nanocarriers were compared. It was found that the best lipid nanocarrier for lupinifolin was lupinifolin-loaded nanostructured lipid carriers, which demonstrated the particle size of 151.5 ± 0.1 nm, monodispersity distribution with a polydispersity index of 0.24, negative surface charge at − 41.2 ± 0.7 mV, high encapsulation (99.3%), and high loading capacity (5.0%). The obtained lupinifolin-loaded nanostructured lipid carriers exhibited prolonged release in a simulated circulatory system but produced a low release in gastrointestinal conditions (3.7%). Intestinal permeability of the nanocarriers was further evaluated in everted intestinal sacs. The results from the ex vivo study indicated that lupinifolin-loaded nanostructured lipid carriers significantly increased the absorption of lupinifolin compared to the native form. In conclusion, lupinifolin-loaded lipid nanocarriers were successfully formulated as delivery systems to enhance its oral bioavailability. Further in vivo experiments are needed to validate the results from this study.

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Masiiwa, Wadzanayi L., and Louis L. Gadaga. "Intestinal Permeability of Artesunate-Loaded Solid Lipid Nanoparticles Using the Everted Gut Method." Journal of Drug Delivery 2018 (April 30, 2018): 1–9. http://dx.doi.org/10.1155/2018/3021738.

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Background. Artesunate is one of the most potent, rapidly acting and therapeutically versatile antimalarial drugs. Its efficacy is hampered by poor aqueous solubility and stability resulting in low oral bioavailability. Recent efforts to nanoformulate artesunate have shown great potential of improving its dissolution profile and bioavailability. However, no study has yet been done to investigate the intestinal permeability of these nanoformulations, which is a critical determinant of systemic absorption. Objective of the Study. The main aim of the study was to determine the intestinal permeability of artesunate-loaded solid lipid nanoparticles (SLN). Method. The microemulsion dilution technique was used to fabricate artesunate-loaded solid lipid nanoparticles. In vitro drug release studies were performed at pH 1.2 and 6.8 using the dialysis membrane method. The everted gut sac method was used to assess the intestinal permeability of the prepared nanoparticles. Results. The average particle size was 1109 nm and the polydispersity index (PDI) was 0.082. The zeta potential was found to be −20.7 mV. The encapsulation efficiency of the solid lipid nanoparticles obtained was 51.7%. At both pH 1.2 and 6.8, pure artesunate was rapidly released within the first 30 mins while the SLN showed a biphasic release pattern with an initial burst release during the first hour followed by a prolonged release over time. The rate of drug release increased with increasing pH. The apparent permeability (Papp) of SLN was found to be greater (0.169 mg/cm2) as compared to that of pure artesunate (0.117 mg/cm2) at the end of the experiment. Conclusion. The results obtained in this study showed that the microemulsion dilution technique can be used to formulate artesunate solid lipid nanoparticles. The formulation exhibited a sustained drug release profile. The intestinal permeability of artesunate could be enhanced by the nanoformulation.

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Chareanputtakhun, P., Theerasak Rojanarata, Praneet Opanasopit, and Tanasait Ngawhirunpat. "Development of NLCs for Topical ATRAs Applications." Advanced Materials Research 506 (April 2012): 162–65. http://dx.doi.org/10.4028/www.scientific.net/amr.506.162.

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NLCs are second generation of lipid nanoparticles which have many advantages that make them interesting for topical drugs delivery systems. All-trans retinoic acids (ATRAs) are highly lipophilic and instable in the presence of air, light and heat. In this study, 0.3% ATRAs loaded NLCs were developed by de novo emulsifications, then were reduced to nanometer range by ultrasonicator. The characterizations of NLCs i.e. size and zeta potential were examined. NLCs with different solid:liquid lipids ratios (2:1, 1:1 and 1:2), were formulated in order to maximize the skin permeation. The results demonstrate the sizes of NLCs were in nanometer ranges with negative zeta potential. Moreover the results showed that the amount of solid lipids in the formulation affected the skin permeation. The highest ATRAs permeations though shed snake skin could be achieved from the NLCs which lipid matrixs were composed of 2:1 solid:liquid lipids ratios.

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Pereira, Cardoso, Rodrigues, Amorim, Amaral, Almeida, Queiroz, et al. "Magnetoliposomes Containing Calcium Ferrite Nanoparticles for Applications in Breast Cancer Therapy." Pharmaceutics 11, no. 9 (September 14, 2019): 477. http://dx.doi.org/10.3390/pharmaceutics11090477.

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Magnetoliposomes containing calcium ferrite (CaFe2O4) nanoparticles were developed and characterized for the first time. CaFe2O4 nanoparticles were covered by a lipid bilayer or entrapped in liposomes forming, respectively, solid or aqueous magnetoliposomes as nanocarriers for new antitumor drugs. The magnetic nanoparticles were characterized by UV/Visible absorption, XRD, HR-TEM, and SQUID, exhibiting sizes of 5.2 ± 1.2 nm (from TEM) and a superparamagnetic behavior. The magnetoliposomes were characterized by DLS and TEM. The incorporation of two new potential antitumor drugs (thienopyridine derivatives) specifically active against breast cancer in these nanosystems was investigated by fluorescence emission and anisotropy. Aqueous magnetoliposomes, with hydrodynamic diameters around 130 nm, and solid magnetoliposomes with sizes of ca. 170 nm, interact with biomembranes by fusion and are able to transport the antitumor drugs with generally high encapsulation efficiencies (70%). These fully biocompatible drug-loaded magnetoliposomes can be promising as therapeutic agents in future applications of combined breast cancer therapy.

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Cometa, Stefania, Maria Addolorata Bonifacio, Giuseppe Trapani, Sante Di Gioia, Laura Dazzi, Elvira De Giglio, and Adriana Trapani. "In vitro investigations on dopamine loaded Solid Lipid Nanoparticles." Journal of Pharmaceutical and Biomedical Analysis 185 (June 2020): 113257. http://dx.doi.org/10.1016/j.jpba.2020.113257.

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Peñate-Medina, Tuula, Eike Kraas, Kunliang Luo, Jana Humbert, Hanwen Zhu, Fabian Mertens, Mirko Gerle, et al. "Utilizing ICG Spectroscopical Properties for Real-Time Nanoparticle Release Quantification In vitro and In vivo in Imaging Setups." Current Pharmaceutical Design 26, no. 31 (September 17, 2020): 3828–33. http://dx.doi.org/10.2174/1381612826666200318170849.

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Background: Nanoparticle imaging and tracking the release of the loaded material from the nanoparticle system have attracted significant attention in recent years. If the release of the loaded molecules could be monitored reliably in vivo, it would speed up the development of drug delivery systems remarkably. Methods: Here, we test a system that uses indocyanine green (ICG) as a fluorescent agent for studying release kinetics in vitro and in vivo from the lipid iron nanoparticle delivery system. The ICG spectral properties like its concentration dependence, sensitivity and the fluctuation of the absorption and emission wavelengths can be utilized for gathering information about the change of the ICG surrounding. Results: We have found that the absorption, fluorescence, and photoacoustic spectra of ICG in lipid iron nanoparticles differ from the spectra of ICG in pure water and plasma. We followed the ICG containing liposomal nanoparticle uptake into squamous carcinoma cells (SCC) by fluorescence microscopy and the in vivo uptake into SCC tumors in an orthotopic xenograft nude mouse model under a surgical microscope. Conclusion: Absorption and emission properties of ICG in the different solvent environment, like in plasma and human serum albumin, differ from those in aqueous solution. Photoacoustic spectral imaging confirmed a peak shift towards longer wavelengths and an intensity increase of ICG when bound to the lipids. The SCC cells showed that the ICG containing liposomes bind to the cell surface but are not internalized in the SCC-9 cells after 60 minutes of incubation. We also showed here that ICG containing liposomal nanoparticles can be traced under a surgical camera in vivo in orthotopic SCC xenografts in mice.

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Carbone, Claudia, Maria do Céu Teixeira, Maria do Céu Sousa, Carlos Martins-Gomes, Amelia M. Silva, Eliana Maria Barbosa Souto, and Teresa Musumeci. "Clotrimazole-Loaded Mediterranean Essential Oils NLC: A Synergic Treatment of Candida Skin Infections." Pharmaceutics 11, no. 5 (May 13, 2019): 231. http://dx.doi.org/10.3390/pharmaceutics11050231.

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The increasing development of resistance of Candida species to traditional drugs represents a great challenge to the medical field for the treatment of skin infections. Essential oils were recently proposed to increase drug effectiveness. Herein, we developed and optimized (23 full factorial design) Mediterranean essential oil (Rosmarinus officinalis, Lavandula x intermedia “Sumian”, Origanum vulgare subsp. hirtum) lipid nanoparticles for clotrimazole delivery, exploring the potential synergistic effects against Candida spp. Small sized nanoparticles (<100 nm) with a very broad size distribution (PDI < 0.15) and long-term stability were successfully prepared. Results of the in vitro biosafety on HaCaT (normal cell line) and A431 (tumoral cell line), allowed us to select Lavandula and Rosmarinus as anti-proliferative agents with the potential to be used as co-adjuvants in the treatment of non-tumoral proliferative dermal diseases. Results of calorimetric studies on biomembrane models, confirmed the potential antimicrobial activity of the selected oils due to their interaction with membrane permeabilization. Nanoparticles provided a prolonged in vitro release of clotrimazole. In vitro studies against Candida albicans, Candida krusei and Candida parapsilosis, showed an increase of the antifungal activity of clotrimazole-loaded nanoparticles prepared with Lavandula or Rosmarinus, thus confirming nanostructured lipid carriers (NLC) containing Mediterranean essential oils represent a promising strategy to improve drug effectiveness against topical candidiasis.

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Madkour, Loutfy H. "Biotechnology of Nanostructures Micronutrients Vitamins for Human Health." Journal of Nanosciences Research & Reports 3, no. 2 (June 30, 2021): 1–13. http://dx.doi.org/10.47363/jnsrr/2021(3)119.

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Nowadays, nanotechnology is used as a way to increase bioavailability and decrease the side effects of drugs and nutrients. Micronutrients and nutraceuticals such as vitamins, carotenoids, polyunsaturated fatty acids and polyphenols are classes of food ingredients that are essential for human health and well-being. These compounds are rarely added purely to the targeted food application but rather in encapsulated, solid, dry product forms with added functionalities such as improved stability, bioavailability or handling. Development of new strategies, like nanocarriers, that help to promote the access of neuroprotective molecules to the brain, is needed for providing more effective therapies for the disorders of the central nervous system (CNS). Polymer–lipid hybrid nanoparticles, encapsulating vitamin D3 and vitamin K2, with improved features in terms of stability, loading and mucoadhesiveness were produced for potential nutraceutical and pharmaceutical applications. Recently, nanoformulations that include nanovesicles, solid-lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and polymeric nanoparticles have shown promising outcomes in improving the efficacy and bioavailability of vitamin E. Active targeting of nanoparticles loaded with vitamin D to cancer cells.

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Madhavan S, Azhagu, Priyadharshini R, Sripriya R, Uma V, and Vinotha P. "Pharmacognostical and Phytochemical Screening of GC–MS Analysis of Bioactive Compounds Present in Ethanolic Rhizome Extract of Zingiber officinale Roscoe." Journal of Biomedical Research & Environmental Sciences 2, no. 5 (May 2021): 372–77. http://dx.doi.org/10.37871/jbres1244.

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Nowadays, nanotechnology is used as a way to increase bioavailability and decrease the side effects of drugs and nutrients. Micronutrients and nutraceuticals such as vitamins, carotenoids, polyunsaturated fatty acids and polyphenols are classes of food ingredients that are essential for human health and well-being. These compounds are rarely added purely to the targeted food application but rather in encapsulated, solid, dry product forms with added functionalities such as improved stability, bioavailability or handling. Development of new strategies, like nanocarriers, that help to promote the access of neuroprotective molecules to the brain, is needed for providing more effective therapies for the disorders of the Central Nervous System (CNS). Polymer–lipid hybrid nanoparticles, encapsulating vitamin D3 and vitamin K2, with improved features in terms of stability, loading and mucoadhesiveness were produced for potential nutraceutical and pharmaceutical applications. Recently, nanoformulations that include nanovesicles, solid-lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and polymeric nanoparticles have shown promising outcomes in improving the efficacy and bioavailability of vitamin E. Active targeting of nanoparticles loaded with vitamin D to cancer cells.

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H Madkour, Loutfy. "Biotechnology of Nanostructures Micronutrients Vitamins for Human Health." Journal of Biomedical Research & Environmental Sciences 2, no. 5 (May 2021): 358–71. http://dx.doi.org/10.37871/jbres1243.

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Nowadays, nanotechnology is used as a way to increase bioavailability and decrease the side effects of drugs and nutrients. Micronutrients and nutraceuticals such as vitamins, carotenoids, polyunsaturated fatty acids and polyphenols are classes of food ingredients that are essential for human health and well-being. These compounds are rarely added purely to the targeted food application but rather in encapsulated, solid, dry product forms with added functionalities such as improved stability, bioavailability or handling. Development of new strategies, like nanocarriers, that help to promote the access of neuroprotective molecules to the brain, is needed for providing more effective therapies for the disorders of the Central Nervous System (CNS). Polymer–lipid hybrid nanoparticles, encapsulating vitamin D3 and vitamin K2, with improved features in terms of stability, loading and mucoadhesiveness were produced for potential nutraceutical and pharmaceutical applications. Recently, nanoformulations that include nanovesicles, solid-lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and polymeric nanoparticles have shown promising outcomes in improving the efficacy and bioavailability of vitamin E. Active targeting of nanoparticles loaded with vitamin D to cancer cells.

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Dureja, Harish, and Sunil Khatak. "Recent Advances in Nanotechnology based Tubercular Chemotherapy." International Journal of Pharmaceutical Sciences and Nanotechnology 8, no. 3 (November 30, 2015): 2979–94. http://dx.doi.org/10.37285/ijpsn.2015.8.3.4.

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Tuberculosis (TB) is a more prevalent granulomatos bacterial infection, which remains the world’s second most common cause of death due to infections of Mycobacterium tuberculosis (M.Tuberculosis). A number of characteristics of mycobacterium makes there disease chronic and necessitate prolonged treatment. The emergence of multi-drug-resistance (MDR) stains of M.Tuberculosis makes its necessary for the development of effective combinations of either first-line or second-line drugs or discovery of new safe and effective drug molecules and also implements other modalities of treatment. A number of novel carrier-based drug delivery systems incorporating the traditional and newer anti-tubercular agents have been shown incredible promise to target the site of action, reduce dosing frequency and enhance drug bioavailability with the objective of improving patient compliance. Nanoparticulate system have unique and comparatively more effective drug delivery carriers, including liposomal-mediated drug delivery, polymeric nanoparticles/microparticles, solid lipid nanoparticles, nanosuspensions, nanoemulsions, niosomes, dendrimers, Metal/cyclodextrin inclusion complexes and other nanosystems exploiting the extraordinary properties of matter at the nanoscale. Nanoparticles shown significant improvements in diagnosis, treatment and prevention and provide the flexibility of selecting the invasive and non-invasive route of delivery for chemotherapy of tuberculosis. This manuscript have been made to highlight and overviews the present WHO estimated burden of tuberculosis globally, recent discovery of safe and effective newer anti-tubercular drug moleculesfor MDR and XDR tuberculosis, first and second line anti-tubercular drugs loaded novel nanoparticle carriers for chemotherapy and development of solid lipid nanoparticles as an alternative drug carriers for tubercular chemotherapy.

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Shi, Sanjun, Lu Han, Li Deng, Yanling Zhang, Hongxin Shen, Tao Gong, Zhirong Zhang, and Xun Sun. "Dual drugs (microRNA-34a and paclitaxel)-loaded functional solid lipid nanoparticles for synergistic cancer cell suppression." Journal of Controlled Release 194 (November 2014): 228–37. http://dx.doi.org/10.1016/j.jconrel.2014.09.005.

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Wen, Jia, Xiuge Gao, Qian Zhang, Benazir Sahito, Hongbin Si, Gonghe Li, Qi Ding, et al. "Optimization of Tilmicosin-Loaded Nanostructured Lipid Carriers Using Orthogonal Design for Overcoming Oral Administration Obstacle." Pharmaceutics 13, no. 3 (February 25, 2021): 303. http://dx.doi.org/10.3390/pharmaceutics13030303.

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Tilmicosin (TMS) is widely used to treat bacterial infections in veterinary medicine, but the clinical effect is limited by its poor solubility, bitterness, gastric instability, and intestinal efflux transport. Nanostructured lipid carriers (NLCs) are nowadays considered to be a promising vector of therapeutic drugs for oral administration. In this study, an orthogonal experimental design was applied for optimizing TMS-loaded NLCs (TMS-NLCs). The ratios of emulsifier to mixed lipids, stearic acid to oleic acid, drugs to mixed lipids, and cold water to hot emulsion were selected as the independent variables, while the hydrodynamic diameter (HD), drug loading (DL), and entrapment efficiency (EE) were the chosen responses. The optimized TMS-NLCs had a small HD, high DL, and EE of 276.85 ± 2.62 nm, 9.14 ± 0.04%, and 92.92 ± 0.42%, respectively. In addition, a low polydispersity index (0.231 ± 0.001) and high negative zeta potential (−31.10 ± 0.00 mV) indicated the excellent stability, which was further demonstrated by uniformly dispersed spherical nanoparticles under transmission electron microscopy. TMS-NLCs exhibited a slow and sustained release behavior in both simulated gastric juice and intestinal fluid. Furthermore, MDCK-chAbcg2/Abcb1 cell monolayers were successfully established to evaluate their absorption efficiency and potential mechanism. The results of biodirectional transport showed that TMS-NLCs could enhance the cellular uptake and inhibit the efflux function of drug transporters against TMS in MDCK-chAbcg2/Abcb1 cells. Moreover, the data revealed that TMS-NLCs could enter the cells mainly via the caveolae/lipid raft-mediated endocytosis and partially via macropinocytosis. Furthermore, TMS-NLCs showed the same antibacterial activity as free TMS. Taken together, the optimized NLCs were the promising oral delivery carrier for overcoming oral administration obstacle of TMS.

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Agrawal, Pranav, Amol Tatode, and Milind Umekar. "Solid Lipid Nanoparticle for the Delivery of Docetaxel: A Review." Journal of Drug Delivery and Therapeutics 10, no. 5-s (October 15, 2020): 224–28. http://dx.doi.org/10.22270/jddt.v10i5-s.4441.

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Solid lipid nanoparticles are the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery, clinical medicine and research. Due to its solid state it has greater stability than other nanocarrier systems. There are several other advantages like sustained release, improves bioavaibility and delivery of poorly water soluble drugs, helps in control of several pharmacokinetic parameters of drugs due to which use of SLN is increasing day by day. Various techniques can be used for the formulation of SLN i.e. solvent evaporation, microemulsification technique, high pressure homogenization and supercritical fluid method. It has several applications likes it is use in gene transfer therapy, also use in different drug delivery systmer like oral and pulmonary drug delivery system. Due to several advantages SLNs are widely used in chemotherapy for the treatment of the cancer. The use of SLN for the delivery of Docetaxel to tumor site have several benefits likes site specific delivery, less toxic effect, more cell cytotoxicity and more bioavaibility which leads to decrease in the dosing frequency. Docetaxel is an anticancer agent extracted from plant Taxus Baccata which is widely used in chemotherapy to treat cancer. This article contains the detail information of about the advantages, disadvantages, different method of preparation and several SLN loaded with Docetaxel. Keywords: Solid lipid nanoparticles, drug delivery, clinical medicine, poorly water soluble drugs

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Aldawsari, Hibah M., and Sima Singh. "Rapid Microwave-Assisted Cisplatin-Loaded Solid Lipid Nanoparticles: Synthesis, Characterization and Anticancer Study." Nanomaterials 10, no. 3 (March 11, 2020): 510. http://dx.doi.org/10.3390/nano10030510.

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Cisplatin is one of the most leading potent chemotherapy drugs prescribed for the treatment of most solid tumors. However, the induction of toxicities and the development of resistance restricts its applications. Efforts are made in the proposed study to control the delivery of cisplatin to tumor sites by incorporating it into solid lipid nanoparticle (SLNs) drug carriers. By considering this fact, in the current research work, a single-step, one-pot, microwave-assisted technology was used to produce cisplatin-loaded SLNs. The shape of the SLNs was observed to be spherical, with a uniform size distribution of 74.85 nm, polydispersity index (PDI) of 0.311, and zeta potential of −20.8 mV. The percentage of encapsulation efficiency was found to be 71.85%. In vitro drug release study was calculated to be 80% in 24 h. The formulation in blood was found to be safe; a study of hemolysis confirmed this. Breast cancer cell line MCF-7 was used to test cytotoxicity and cellular interaction of cisplatin-loaded SLNs with an IC50 value of 6.51 ± 0.39 μg/mL. Overall, the results of our findings show that the approach of SLNs-based, cisplatin-based, drug delivery has led to increased sustainability in breast cancer therapy with superior biocompatibility.

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Xiang, Qing-yu, Min-ting Wang, Fu Chen, Tao Gong, Yan-lin Jian, Zhi-rong Zhang, and Yuan Huang. "Lung-targeting delivery of dexamethasone acetate loaded solid lipid nanoparticles." Archives of Pharmacal Research 30, no. 4 (April 2007): 519–25. http://dx.doi.org/10.1007/bf02980228.

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Rukmangathen, Rajalakshmi, Indira Muzib Yallamalli, and Prasanna Raju Yalavarthi. "Biopharmaceutical Potential of Selegiline Loaded Chitosan Nanoparticles in the Management of Parkinson's Disease." Current Drug Discovery Technologies 16, no. 4 (December 11, 2019): 417–25. http://dx.doi.org/10.2174/1570163815666180418144019.

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Background: Selegiline hydrochloride, a hydrophilic anti-Parkinson’ moiety, undergoes extensive first-pass metabolism and has low bioavailability. A process to obtain of selegiline (SH) loaded chitosan nanoparticles was attempted to circumvent the above problem, through intranasal delivery. Methods: SH loaded polymeric nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate, and stabilized by tween 80/ poloxamer 188. The resulting nanoparticles (NPs) were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, particle size, zeta potential and surface morphology by scanning electron microscopy. Further, they were schematically evaluated for mucoadhesive strength, in-vitro drug release, release kinetics, pharmacokinetics, catalepsy, akinesia, in-vivo lipid peroxidation, nitrite levels, glutathione, catalase enzyme levels in brain and physicochemical stability parameters. Results: Selegiline nanoparticles (SP18) produced were in size of 63.1 nm, polydispersity index of 0.201, zeta potential of +35.2 mV, mucoadhesion of 65.4% and entrapment efficiency of 74.77%. Selegiline showed biphasic release from nanoparticles, over a period of 36 h, with Fickian diffusion controlled release profile. Maximum concentration of SH in plasma was recognized as 52.71 ng/ml at 2 h for SP18, 20.09 ng/ml at 1 h for marketed formulation, and 21.69 ng/ ml for drug solution. SH loaded NPs showed a reversive effect in catalepsy and akinesia behaviour. This effect was especially pronounced in rats receiving SH loaded CS-NPs. Significant decrease in lipid peroxidation and nitrite concentration; increase in reduced glutathione and catalase enzyme levels were obtained due to antioxidant characteristics of SH, which turned to be useful to treat Parkinson’s disease. Conclusion: Selegiline loaded chitosan nanoparticles form an effective non-invasive drug delivery system of direct nose to brain targeting in Parkinson’s disease.

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Dąbrowska, Marta, Eliana B. Souto, and Izabela Nowak. "Lipid Nanoparticles Loaded with Iridoid Glycosides: Development and Optimization Using Experimental Factorial Design." Molecules 26, no. 11 (May 25, 2021): 3161. http://dx.doi.org/10.3390/molecules26113161.

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Lipid nanoparticles based on multiple emulsion (W/O/W) systems are suitable for incorporating hydrophilic active substances, including iridoid glycosides. This study involved optimization of composition of lipid nanoparticles, incorporation of active compounds (aucubin and catalpol), evaluation of stability of the resulting nanocarriers, and characterization of their lipid matrix. Based on 32 factorial design, an optimized dispersion of lipid nanoparticles (solid lipid:surfactant—4.5:1.0 wt.%) was developed, predisposed for the incorporation of iridoid glycosides by emulsification-sonication method. The encapsulation efficiency of the active substances was determined at nearly 90% (aucubin) and 77% (catalpol). Regarding the stability study, room temperature was found to be the most suitable for maintaining the expected physicochemical parameter values (particle size < 100 nm; polydispersity index < 0.3; zeta potential > |± 30 mV|). Characterization of the lipid matrix confirmed the nanometer size range of the resulting carriers (below 100 nm), as well as the presence of the lipid in the stable β’ form.

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Chaves, Luíse L., Sofia Lima, Alexandre C. C. Vieira, Domingos Ferreira, Bruno Sarmento, and Salette Reis. "Overcoming clofazimine intrinsic toxicity: statistical modelling and characterization of solid lipid nanoparticles." Journal of The Royal Society Interface 15, no. 139 (February 2018): 20170932. http://dx.doi.org/10.1098/rsif.2017.0932.

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The aim of this work was to develop solid lipid nanoparticles (SLNs) loaded with clofazimine (CLZ) (SLNs-CLZ) to overcome its intrinsic toxicity and low water solubility, for oral drug delivery. A Box–Behnken design was constructed to unravel the relations between the independent variables in the selected responses. The optimized SLNs-CLZ exhibited the following properties: particle size ca 230 nm, zeta potential of −34.28 mV, association efficiency of 72% and drug loading of 2.4%, which are suitable for oral delivery. Further characterization included Fourier transformed infrared spectroscopy that confirmed the presence of the drug and the absence of chemical interactions. By differential scanning calorimetry was verified the amorphous state of CLZ. The storage stability studies ensured the stability of the systems over a period of 12 weeks at 4°C. In vitro cytotoxicity studies evidenced no effect of both drug-loaded and unloaded SLNs on MKN-28 gastric cells and on intestinal cells, namely Caco-2 and HT29-MTX cells up to 25 µg ml −1 in CLZ. Free CLZ solutions exhibited IC 50 values of 16 and 20 µg ml −1 for Caco-2 and HT29-MTX cells, respectively. It can be concluded that the optimized system, designed considering important variables for the formulation of poorly soluble drugs, represents a promising platform for oral CLZ delivery.

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Du, Shufang, Hongwei Wang, Feng Jiang, and Ying Wang. "Diabetic Retinopathy Analysis—Effects of Nanoparticle-Based Triamcinolone." Journal of Nanoscience and Nanotechnology 20, no. 10 (October 1, 2020): 6111–15. http://dx.doi.org/10.1166/jnn.2020.18569.

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Triamcinolone (TA) is a hormone corticosteroid drug used to treat edema, inflammation, and angiogenic eye diseases. It can be administered by intravitreal injection at an early stage. The intraocular instillation method can improve the bioavailability of TA by loading the drug on to a nanostructured lipid carrier (NLC). The nanoparticles (20 to 200 nm) used in this experiment were previously prepared by high-pressure homogenization using a factorial optimization design method. The NLC produced contained a distinct peak with a negative charge. The nanoparticles were loaded with drugs (TA-NLC) and fluorescent Nile Red lipids. Using the treated nanoparticles, NR-NLC was dripped into the eyes of mice in an in vivo test, demonstrating the ability to deliver lipophilic active substances to the posterior ocular segment. The short- and long-term stability of TA-NLC was also evaluated using a Turbiscan® high-performance stability analysis. Results showed that backscattering in the 6-month stability test was less than 1.5%. When stored at room temperature, the possibility of the nanoparticles condensing into flocs during the storage period is very small.

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Chang, Ming-Cheng, Ping-Fang Chiang, Yu-Jen Kuo, Cheng-Liang Peng, Kuan-Yin Chen, and Ying-Cheng Chiang. "Hyaluronan-Loaded Liposomal Dexamethasone– Diclofenac Nanoparticles for Local Osteoarthritis Treatment." International Journal of Molecular Sciences 22, no. 2 (January 11, 2021): 665. http://dx.doi.org/10.3390/ijms22020665.

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Osteoarthritis (OA) remains one of the common degenerative joint diseases and a major cause of pain and disability in older adult individuals. Oral administration of non-steroidal anti-inflammatory drugs (NSAIDs) (such as diclofenac, DIC) or intra-articular injected gluco-corticosteroids (such as dexamethasone, DEX) were the conventional treatment strategies for OA to reduce joint pain. Current limitations for both drugs including severe adverse effects with risks of toxicity were noted. The aim of the present study was to generate a novel OA treatment formulation hyaluronic acid (HA)-Liposomal (Lipo)-DIC/DEX to combat joint pain. The formulation was prepared by constructing DIC with DEX-loaded nanostructured lipid carriers Lipo-DIC/DEX mixed with hyaluronic acid (HA) for prolonged OA application. The prepared Lipo-DIC/DEX nanoparticles revealed the size as 103.6 ± 0.3 nm on average, zeta potential as −22.3 ± 4.6 mV, the entrapment efficiency of 90.5 ± 5.6%, and the DIC and DEX content was 22.5 ± 4.1 and 2.5 ± 0.6%, respectively. Evidence indicated that HA-Lipo-DIC/DEX could reach the effective working concentration in 4 h and sustained the drug-releasing time for at least 168 h. No significant toxicities but increased cell numbers were observed when HA-Lipo-DIC/DEX co-cultured with articular chondrocytes cells. Using live-animal In vivo imaging system (IVIS), intra-articular injection of each HA-Lipo-DIC/DEX sufficed to reduce knee joint inflammation in OA mice over a time span of four weeks. Single-dose injection could reduce the inflammation volume down to 77.5 ± 5.1% from initial over that time span. Our results provided the novel drug-releasing formulation with safety and efficiency which could be a promising system for osteoarthritis pain control.

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Chang, Ming-Cheng, Ping-Fang Chiang, Yu-Jen Kuo, Cheng-Liang Peng, Kuan-Yin Chen, and Ying-Cheng Chiang. "Hyaluronan-Loaded Liposomal Dexamethasone–Diclofenac Nanoparticles for Local Osteoarthritis Treatment." International Journal of Molecular Sciences 22, no. 2 (January 11, 2021): 665. http://dx.doi.org/10.3390/ijms22020665.

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Osteoarthritis (OA) remains one of the common degenerative joint diseases and a major cause of pain and disability in older adult individuals. Oral administration of non-steroidal anti-inflammatory drugs (NSAIDs) (such as diclofenac, DIC) or intra-articular injected gluco-corticosteroids (such as dexamethasone, DEX) were the conventional treatment strategies for OA to reduce joint pain. Current limitations for both drugs including severe adverse effects with risks of toxicity were noted. The aim of the present study was to generate a novel OA treatment formulation hyaluronic acid (HA)-Liposomal (Lipo)-DIC/DEX to combat joint pain. The formulation was prepared by constructing DIC with DEX-loaded nanostructured lipid carriers Lipo-DIC/DEX mixed with hyaluronic acid (HA) for prolonged OA application. The prepared Lipo-DIC/DEX nanoparticles revealed the size as 103.6 ± 0.3 nm on average, zeta potential as −22.3 ± 4.6 mV, the entrapment efficiency of 90.5 ± 5.6%, and the DIC and DEX content was 22.5 ± 4.1 and 2.5 ± 0.6%, respectively. Evidence indicated that HA-Lipo-DIC/DEX could reach the effective working concentration in 4 h and sustained the drug-releasing time for at least 168 h. No significant toxicities but increased cell numbers were observed when HA-Lipo-DIC/DEX co-cultured with articular chondrocytes cells. Using live-animal In vivo imaging system (IVIS), intra-articular injection of each HA-Lipo-DIC/DEX sufficed to reduce knee joint inflammation in OA mice over a time span of four weeks. Single-dose injection could reduce the inflammation volume down to 77.5 ± 5.1% from initial over that time span. Our results provided the novel drug-releasing formulation with safety and efficiency which could be a promising system for osteoarthritis pain control.

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Zhang, Yake, Fangyuan Xie, You Yin, Qin Zhang, Hong Jin, Yan Wu, Liying Pang, Jun Li, and Jie Gao. "Immunotherapy of Tumor RNA-Loaded Lipid Nanoparticles Against Hepatocellular Carcinoma." International Journal of Nanomedicine Volume 16 (February 2021): 1553–64. http://dx.doi.org/10.2147/ijn.s291421.

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Murgia, Denise, Giuseppe Angellotti, Fabio D’Agostino, and Viviana De Caro. "Bioadhesive Matrix Tablets Loaded with Lipophilic Nanoparticles as Vehicles for Drugs for Periodontitis Treatment: Development and Characterization." Polymers 11, no. 11 (November 2, 2019): 1801. http://dx.doi.org/10.3390/polym11111801.

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Periodontitis treatment is usually focused on the reduction or eradication of periodontal pathogens using antibiotics against anaerobic bacteria, such as metronidazole (MTR). Moreover, recently the correlation between periodontal diseases and overexpression of reactive oxygen species (ROS) led to the introduction of antioxidant biomolecules in therapy. In this work, bioadhesive buccal tablets, consisting of a hydrophilic matrix loaded with metronidazole and lipophilic nanoparticles as a vehicle of curcumin, were developed. Curcumin (CUR)-loaded nanostructured lipid carriers (NLC) were prepared using glycyrrhetic acid, hexadecanol, isopropyl palmitate and Tween®80 as a surfactant. As method, homogenization followed by high-frequency sonication was used. After dialysis, CUR-NLC dispersion was evaluated in terms of drug loading (DL, 2.2% w/w) and drug recovery (DR, 88% w/w). NLC, characterized by dynamic light scattering and scanning electron microscopy (SEM), exhibited a spherical shape, an average particle size of 121.6 nm and PDI and PZ values considered optimal for a colloidal nanoparticle dispersion indicating good stability of the system. Subsequently, a hydrophilic sponge was obtained by lyophilization of a gel based on trehalose, Natrosol and PVP-K90, loaded with CUR-NLC and MTR. By compression of the sponge, matrix tablets were obtained and characterized in term of porosity, swelling index, mucoadhesion and drugs release. The ability of the matrix tablets to release CUR and MTR when applied on buccal mucosa and the aptitude of actives to penetrate and/or permeate the tissue were evaluated. The data demonstrate the ability of NLC to promote the penetration of CUR into the lipophilic domains of the mucosal membrane, while MTR can penetrate and permeate the mucosal tissue, where it can perform a loco-regional antibacterial activity. These results strongly support the possibility of using this novel matrix tablet for delivering MTR together with CUR for topical treatment of periodontal diseases.

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Idlas, Pierre, Elise Lepeltier, Gérard Jaouen, and Catherine Passirani. "Ferrocifen Loaded Lipid Nanocapsules: A Promising Anticancer Medication against Multidrug Resistant Tumors." Cancers 13, no. 10 (May 11, 2021): 2291. http://dx.doi.org/10.3390/cancers13102291.

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Resistance of cancer cells to current chemotherapeutic drugs has obliged the scientific community to seek innovative compounds. Ferrocifens, lipophilic organometallic compounds composed of a tamoxifen scaffold covalently bound to a ferrocene moiety, have shown very interesting antiproliferative, cytotoxic and immunologic effects. The formation of ferrocenyl quinone methide plays a crucial role in the multifaceted activity of ferrocifens. Lipid nanocapsules (LNCs), meanwhile, are nanoparticles obtained by a free organic solvent process. LNCs consist of an oily core surrounded by amphiphilic surfactants and are perfectly adapted to encapsulate these hydrophobic compounds. The different in vitro and in vivo experiments performed with this ferrocifen-loaded nanocarrier have revealed promising results in several multidrug-resistant cancer cell lines such as glioblastoma, breast cancer and metastatic melanoma, alone or in combination with other therapies. This review provides an exhaustive summary of the use of ferrocifen-loaded LNCs as a promising nanomedicine, outlining the ferrocifen mechanisms of action on cancer cells, the nanocarrier formulation process and the in vivo results obtained over the last two decades.

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De Gaetano, Federica, Maria Chiara Cristiano, Valentina Venuti, Vincenza Crupi, Domenico Majolino, Giuseppe Paladini, Giuseppe Acri, et al. "Rutin-Loaded Solid Lipid Nanoparticles: Characterization and In Vitro Evaluation." Molecules 26, no. 4 (February 16, 2021): 1039. http://dx.doi.org/10.3390/molecules26041039.

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This study was aimed at preparing and characterizing solid lipid nanoparticles loading rutin (RT-SLNs) for the treatment of oxidative stress-induced diseases. Phospholipon 80H® as a solid lipid and Polysorbate 80 as surfactant were used for the SLNs preparation, using the solvent emulsification/diffusion method. We obtained spherical RT-SLNs with low sizes, ranging from 40 to 60 nm (hydrodynamic radius) for the SLNs prepared starting from 2% and 5% (w/w) theoretical amount. All prepared formulations showed negative zeta-potential values. RT was efficiently encapsulated within SLNs, obtaining high encapsulation efficiency and drug content percentages, particularly for SLNs prepared with a 5% theoretical amount of RT. In vitro release profiles and analysis of the obtained data applying different kinetic models revealed Fickian diffusion as the main mechanism of RT release from the SLNs. The morphology of RT-SLNs was characterized by scanning electron microscopy (SEM), whereas the interactions between RT and the lipid matrix were investigated by Raman spectroscopy, evidencing spectral modifications of characteristic bands of RT due to the establishment of new interactions. Finally, antioxidant activity assay on human glioblastoma astrocytoma (U373) culture cells showed a dose-dependent activity for RT-SLNs, particularly at the highest assayed dose (50 μM), whereas the free drug showed the lesser activity.

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Arıca Yegin, Betül, Jean-Pierre Benoît, and Alf Lamprecht. "Paclitaxel-Loaded Lipid Nanoparticles Prepared by Solvent Injection or Ultrasound Emulsification." Drug Development and Industrial Pharmacy 32, no. 9 (January 2006): 1089–94. http://dx.doi.org/10.1080/03639040600683501.

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Mahmoudian, Mohammad, Hadi Valizadeh, and Parvin Zakeri-Milani. "Bortezomib-loaded solid lipid nanoparticles: preparation, characterization, and intestinal permeability investigation." Drug Development and Industrial Pharmacy 44, no. 10 (July 2, 2018): 1598–605. http://dx.doi.org/10.1080/03639045.2018.1483385.

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Yadav, Pawan, Goutam Rath, Gazal Sharma, Ranjit Singh, and Amit Kumar Goyal. "Polysorbate 80 Coated Solid Lipid Nanoparticles for the Delivery of Temozolomide Into the Brain." Open Pharmacology Journal 8, no. 1 (October 30, 2018): 21–28. http://dx.doi.org/10.2174/1874143601808010021.

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Introduction:Anti-angiogenic therapy can produce transient regression in tumor in case of Glioblastoma (GBM); however, no prolongation of patient survival rate had so far been achieved.Methodology:To address this problem, an effort was made to design and characterize a temozolomide loaded nanosystem for targeting the tumor vasculature in the brain using polymeric nanoparticles. It included the formation of Temozolomide (TMZ) loaded Solid-Lipid Nanoparticles (SLNs) and their conjugation with polysorbate-80 (P-80) which enhanced the penetration of drug to blood-brain barrier resulting in the enhancement of pro-apoptotic activity.Results:Conjugating nanoparticles with a tumor-penetrating polymer (P-80) further enhanced the therapeutic efficacy of the drug.Conclusion:The animal studies indicated the enhanced potential of the developed system in the effective treatment of glioblastoma.

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Journal articles on the topic 'Lipid nanoparticles loaded with drugs'

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