Journal articles: 'Lipid formulations'

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Shrestha, Hina, Rajni Bala, and Sandeep Arora. "Lipid-Based Drug Delivery Systems." Journal of Pharmaceutics 2014 (May 19, 2014): 1–10. http://dx.doi.org/10.1155/2014/801820.

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The principle objective of formulation of lipid-based drugs is to enhance their bioavailability. The use of lipids in drug delivery is no more a new trend now but is still the promising concept. Lipid-based drug delivery systems (LBDDS) are one of the emerging technologies designed to address challenges like the solubility and bioavailability of poorly water-soluble drugs. Lipid-based formulations can be tailored to meet a wide range of product requirements dictated by disease indication, route of administration, cost consideration, product stability, toxicity, and efficacy. These formulations are also a commercially viable strategy to formulate pharmaceuticals, for topical, oral, pulmonary, or parenteral delivery. In addition, lipid-based formulations have been shown to reduce the toxicity of various drugs by changing the biodistribution of the drug away from sensitive organs. However, the number of applications for lipid-based formulations has expanded as the nature and type of active drugs under investigation have become more varied. This paper mainly focuses on novel lipid-based formulations, namely, emulsions, vesicular systems, and lipid particulate systems and their subcategories as well as on their prominent applications in pharmaceutical drug delivery.

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S., Nikam Supriya, Phadatare Priya P., Watode Ankita B., and Kalyani Kayande. "NANOSTRUCTURED LIPID CARRIERS: A PROMISING APPROACH FOR TOPICAL DRUG DELIVERY SYSTEM." International Journal of Pharmaceutical Sciences and Medicine 6, no. 7 (July 30, 2021): 81–101. http://dx.doi.org/10.47760/ijpsm.2021.v06i07.007.

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Nanostructured lipid carriers (NLCs) are innovative pharmaceutical formulations made up of physiological and biocompatible lipids, as well as surfactants and co-surfactant. The initial generation of lipid nanoparticles was Solid Lipid Nanoparticles (SLN), which had a longer-lasting activity and was better, suited to drug penetration. The NLC is a second-generation lipid nanoparticle designed to alleviate the limitations of SLN, such as limited drug loading capacity and solid lipid polymorphism. Many benefits of topical medication delivery include avoiding first-pass metabolism, focusing active components for a local effect, and patient compliance. When compared to typical topical dose forms, nanoparticles have a greater effect in transporting medications through the skin. The structure, composition, many formulation methods, and characterization of NLCs are all important aspects in formulating a stable drug delivery system, as discussed in this review paper. A variety of approaches are used to make solid lipid nanoparticles and nanostructured lipid carriers, which are discussed in this paper. Lipid nanoparticles have a variety of features that make them suitable for topical usage in cosmetics and medicinal formulations. Because of extensive positive benefits such as skin hydration, skin occlusion, and skin targeting, NLCs have a significant potential in the pharmaceutical market. Skin hydration is important for API topical distribution because it hydrates the skin, which causes the pores to open. Trans epidermal water loss decreases due to the occlusion nature of lipid nanoparticles, softening the skin. It is more suited since it uses biodegradable grade lipid, which does not cause toxicity like polymeric Nano formulations. Actually, because of their biodegradable composition, NLCs are a “Nano safe” carrier that has a lot of potential for overcoming the obstacles of topical distribution.

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Peddappi Reddigari, Jayachandra Reddy, Yerikala Ramesh, and Chandrasekhar B. Kothapalli. "Formulation and evaluation of in-situ gels enriched with Tropicamide loaded solid lipid nanoparticles." International Journal of Research in Pharmaceutical Sciences 9, no. 1 (March 12, 2018): 216. http://dx.doi.org/10.26452/ijrps.v9i1.1250.

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The present research work “Formulation and Evaluation of In-situ gels enriched with Tropicamide loaded solid lipid nanoparticles”. To overcome the problems of side effects and to increase the bioavailability of tropicamide loaded solid lipid nanoparticles are containing with suitable lipids (glycerin trimyristate, Tristearin, Phosphatidylcholine & soyabean lecithin) with stabilizers (poloxamer 188) and surfactant like polysorbate 80. The interaction between drug, lipids & polymer by performing with FTIR no incompatibility with each other. The particle morphology was carried out by SEM & AFM in solid lipid nanoparticle formulation. The particle size was ranges from 213.6 ± 2.16nm to 538.0 ± 6.53 nm. The zeta potential ranges form -18.3mV to 25.6mV. The entrapment efficiency of free tropicamide was ranges from 74.13 % to 90.17%. The drug content was ranges from 0.212mg/ml to 0.912mg/ml. The SLN formulations must be transparent white colour and semi solid consistency. The pH 7.0 to 8.0 in all formulation. The gelling strength of gels TSLNGF1 to TSLNGF12 was ranges from 72 ± 1 sec to 117 ± 2 sec. The bio adhesive force was ranges from 10.12 ±1.01 dynes/cm2 to 23.12 ± 1.91 dynes/cm2. The viscosity of prepared formulation ranges from 415 ± 1.94 cps to 652 ± 1.41 cps. The spread ability studies of all formulation were ranges from 09 gms/sec to 18 gms/sec. The Accelerated stability the formulations does not undergo any chemical Changes. In vitro Franz’s diffusion studies of SLN enriched in gels TSLNGF1 to TSLNGF12 among the various formulation best formulations was TSLNGF6; its follows first order kinetics. Keywords: Solid Lipid Nanoparticles; Tropicamide; In- situ gels; In vitro diffusion studies

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Singh, Sukhwinder, Sukhmeet Singh Kamal, Amit Sharma, Daljit Kaur, Manoj Kumar Katual, and Rajesh Kumar. "Formulation and In-Vitro Evaluation of Solid Lipid Nanoparticles Containing Levosulpiride." Open Nanomedicine Journal 4, no. 1 (October 31, 2017): 17–29. http://dx.doi.org/10.2174/1875933501704010017.

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Objectives: The present study aims on preparing Levosulpiride loaded solid lipid nanoparticles (SLNs) to reduce the dose, frequency of dosing, reduce side effects and to increase the bioavailable fraction of drug (<30% orally in general). Methods: Levosulpiride was characterized by preformulation studies like physical appearance, melting point, assay, calibration curve, FTIR analysis and DSC analysis. The calibration curve of the drug was prepared in pH 6.8 phosphate buffer. Two lipids (Stearic acid and Palmitic acid) were used as lipid phase to prepare SLNs. Factorial design (23) was applied to formulate 16 formulations (8 for each lipid i.e. SF1-SF8 and PF1-PF8). Levosulpiride SLNs were prepared by solvent evaporation method followed by homogenization. Results: The optimized formulations were characterized by particle size analysis, zeta potential analysis, in vitro drug release and drug release kinetics. Drug-excipient interaction in optimized formulation was characterized by FTIR, DSC and TEM analysis. Conclusion: On the basis of evaluation parameters, the formulation SF1 (containing Stearic acid) and PF1 (containing Palimitic acid) found to be better formulations amongst their groups with a controlled drug release after a period of 24 hrs.

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Hiemenz, John W., and Thomas J. Walsh. "Lipid Formulations of Amphotericin." Journal of Liposome Research 8, no. 4 (January 1998): 443–67. http://dx.doi.org/10.3109/08982109809039931.

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Hauss, David J. "Oral lipid-based formulations." Advanced Drug Delivery Reviews 59, no. 7 (July 2007): 667–76. http://dx.doi.org/10.1016/j.addr.2007.05.006.

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Alvebratt, Caroline, Tahnee J. Dening, Michelle Åhlén, Ocean Cheung, Maria Strømme, Adolf Gogoll, Clive A. Prestidge, and Christel A. S. Bergström. "In Vitro Performance and Chemical Stability of Lipid-Based Formulations Encapsulated in a Mesoporous Magnesium Carbonate Carrier." Pharmaceutics 12, no. 5 (May 6, 2020): 426. http://dx.doi.org/10.3390/pharmaceutics12050426.

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Lipid-based formulations can circumvent the low aqueous solubility of problematic drug compounds and increase their oral absorption. As these formulations are often physically unstable and costly to manufacture, solidification has been suggested as a way to minimize these issues. This study evaluated the physicochemical stability and in vitro performance of lipid-loaded mesoporous magnesium carbonate (MMC) particles with an average pore size of 20 nm. A medium chain lipid was loaded onto the MMC carrier via physical adsorption. A modified in vitro lipolysis setup was then used to study lipid release and digestion with 1H nuclear magnetic resonance spectroscopy. The lipid loading efficiency with different solidification techniques was also evaluated. The MMC, unlike more commonly used porous silicate carriers, dissolved during the lipolysis assay, providing a rapid release of encapsulated lipids into solution. The digestion of the dispersed lipid-loaded MMC therefore resembled that of a coarse dispersion of the lipid. The stability data demonstrated minor degradation of the lipid within the pores of the MMC particles, but storage for three months did not reveal extensive degradation. To conclude, lipids can be adsorbed onto MMC, creating a solid powder from which the lipid is readily released into the solution during in vitro digestion. The chemical stability of the formulation does however merit further attention.

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Brajtburg, J., and J. Bolard. "Carrier effects on biological activity of amphotericin B." Clinical Microbiology Reviews 9, no. 4 (October 1996): 512–31. http://dx.doi.org/10.1128/cmr.9.4.512.

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Amphotericin B (AmB), the drug of choice for the treatment of most systemic fungal infections, is marketed under the trademark Fungizone, as an AmB-deoxycholate complex suitable for intravenous administration. The association between AmB and deoxycholate is relatively weak; therefore, dissociation occurs in the blood. The drug itself interacts with both mammalian and fungal cell membranes to damage cells, but the greater susceptibility of fungal cells to its effects forms the basis for its clinical usefulness. The ability of the drug to form stable complexes with lipids has allowed the development of new formulations of AmB based on this property. Several lipid-based formulations of the drug which are more selective in damaging fungal or parasitic cells than mammalian cells and some of which also have a better therapeutic index than Fungizone have been developed. In vitro investigations have led to the conclusion that the increase in selectivity observed is due to the selective transfer of AmB from lipid complexes to fungal cells or to the higher thermodynamic stability of lipid formulations. Association with lipids modulates AmB binding to lipoproteins in vivo, thus influencing tissue distribution and toxicity. For example, lipid complexes of AmB can be internalized by macrophages, and the macrophages then serve as a reservoir for the drug. Furthermore, stable AmB-lipid complexes are much less toxic to the host than Fungizone and can therefore be administered in higher doses. Experimentally, the efficacy of AmB-lipid formulations compared with Fungizone depends on the animal model used. Improved therapeutic indices for AmB-lipid formations have been demonstrated in clinical trials, but the definitive trials leading to the selection of an optimal formulation and therapeutic regimen have not been done.

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Boyd, Ben J., and Andrew J. Clulow. "The influence of lipid digestion on the fate of orally administered drug delivery vehicles." Biochemical Society Transactions 49, no. 4 (August 25, 2021): 1749–61. http://dx.doi.org/10.1042/bst20210168.

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This review will focus on orally administered lipid-based drug delivery vehicles and specifically the influence of lipid digestion on the structure of the carrier lipids and their entrained drug cargoes. Digestion of the formulation lipids, which are typically apolar triglycerides, generates amphiphilic monoglycerides and fatty acids that can self-assemble into a diverse array of liquid crystalline structures. Tracking the dynamic changes in self-assembly of the lipid digestion products during digestion has recently been made possible using synchrotron-based small angle X-ray scattering. The influence of lipid chain length and degree of unsaturation on the resulting lipid structuring will be described in the context of the critical packing parameter theory. The chemical and structural transformation of the formulation lipids can also have a dramatic impact on the physical state of drugs co-administered with the formulation. It is often assumed that the best strategy for drug development is to maximise drug solubility in the undigested formulation lipids and to incorporate additives to maintain drug solubility during digestion. However, it is possible to improve drug absorption using lipid digestion in cases where the solubility of the dosed drug or one of its polymorphic forms is greater in the digested lipids. Three different fates for drugs administered with digestible lipid-based formulations will be discussed: (1) where the drug is more soluble in the undigested formulation lipids; (2) where the drug undergoes a polymorphic transformation during lipid digestion; and (3) where the drug is more soluble in the digested formulation lipids.

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Contini, Gisele, Fabielli de Oliveira, Alana Martins, and Katielle Córdova. "Partial Replacement of Maltodextrin by Sweet Potato Flour (Ipomoea Batatas L. Lamarck) in the Development of a Shake Beverage." Beverages 5, no. 1 (March 1, 2019): 18. http://dx.doi.org/10.3390/beverages5010018.

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Sweet potato flour contains low-glycemic complex carbohydrates and, when it is ingested, prevents insulin spikes and prolongs the feeling of satiety. The aim of this study was to elaborate and to verify the acceptability of the shake with the total or partial substitution of maltodextrin for sweet potato flour. To elaborate the shake beverage, we used a 22 factorial design, with three central points, thus generating seven formulations. For the taste, color, texture, appearance, acceptance and attitude of purchase properties, sensory tests were conducted using a nine-point hedonic scale and panelists (n = 50). The highest acceptability formulations, formulations 3 (10% sweet potato flour; 25% maltodextrin) and 7 (0% sweet potato flour; 25% maltodextrin), were submitted to pH, moisture, ash, protein, lipid, crude fiber and total carbohydrate analyses. The statistical difference between the formulations from the T test (p < 0.05) was verified for the moisture, ash and lipid parameters. Formulation 3 presented higher values of moisture (93.26 ± 0.57) and lipids (1.91 ± 0.01), and formulation 7 had higher values of ash (0.39 ± 0.01). The results of the sensorial and physicochemical analyses of the shake indicate that sweet potato flour shows potential for the elaboration of this drink.

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Dutta, Sandeep, and William F. Ebling. "Formulation-dependent Brain and Lung Distribution Kinetics of Propofol in Rats." Anesthesiology 89, no. 3 (September 1, 1998): 678–85. http://dx.doi.org/10.1097/00000542-199809000-00018.

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Background Propofol when administered by brief infusion in a lipid-free formulation has a slower onset, prolonged offset and greater potency compared with an emulsion formulation. To understand these findings the authors examined propofol brain and lung distribution kinetics in rats. Methods Rats were infused with equieffective doses of propofol in emulsion (n = 21) or lipid-free formulation (n = 21). Animals were sacrificed at various times to harvest brain and lung. Arterial blood was sampled repeatedly from each animal until sacrifice. Deconvolution and moment analysis were used to calculate the half-life for propofol brain turnover (BT) and brain:plasma partition coefficient (Kp). Lung concentration-time profiles were compared for the two formulations. Results Peak propofol plasma concentrations for the lipid-free formulation were 50% of that observed for emulsion formulation, whereas peak lung concentrations for lipid-free formulation were 300-fold higher than emulsion formulation. Brain Kp calculated from tissue disposition curve and ratio of brain:plasma area under the curves were 8.8 and 13, and 7.2 and 9.1 for emulsion and lipid-free formulations, respectively. BT were 2.4 and 2.5 min for emulsion and lipid-free formulations, respectively. Conclusions Significant pulmonary sequestration and slow release of propofol into arterial circulation when administered in lipid-free vehicle accounts for the lower peak arterial concentration and sluggish arterial kinetics relative to that observed with the emulsion formulation. Higher Kp for the lipid-free formulation could explain the higher potency associated with this formulation. BT were independent of formulation and correlated with values reported for effect-site equilibration half-time consistent with a distribution mechanism for pharmacologic hysteresis.

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Chauhan, Iti, Mohd Yasir, Madhu Verma, and Alok Pratap Singh. "Nanostructured Lipid Carriers: A Groundbreaking Approach for Transdermal Drug Delivery." Advanced Pharmaceutical Bulletin 10, no. 2 (February 18, 2020): 150–65. http://dx.doi.org/10.34172/apb.2020.021.

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Nanostructured lipid carriers (NLCs) are novel pharmaceutical formulations which are composed of physiological and biocompatible lipids, surfactants and co-surfactants. Over time, as a second generation lipid nanocarrier NLC has emerged as an alternative to first generation nanoparticles. This review article highlights the structure, composition, various formulation methodologies, and characterization of NLCs which are prerequisites in formulating a stable drug delivery system. NLCs hold an eminent potential in pharmaceuticals and cosmetics market because of extensive beneficial effects like skin hydration, occlusion, enhanced bioavailability, and skin targeting. This article aims to evoke an interest in the current state of art NLC by discussing their promising assistance in topical drug delivery system. The key attributes of NLC that make them a promising drug delivery system are ease of preparation, biocompatibility, the feasibility of scale up, non-toxicity, improved drug loading, and stability.

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Efendy Goon, Danial, Siti Hamimah Sheikh Abdul Kadir, Normala Ab Latip, Sharaniza Ab. Rahim, and Musalmah Mazlan. "Palm Oil in Lipid-Based Formulations and Drug Delivery Systems." Biomolecules 9, no. 2 (February 13, 2019): 64. http://dx.doi.org/10.3390/biom9020064.

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Palm oil is natural oil packed with important compounds and fatty acids ready to be exploited in lipid-based formulations and drug delivery. Palm oil and palm kernel oil contain long-chain and medium-chain triglycerides, respectively, including phytonutrients such as tocotrienol, tocopherol and carotenes. The exploitation of these compounds in a lipid-based formulation would be able to address hydrophobicity, lipophilicity, poor bioavailability and low water-solubility of many current drugs. The utilisation of palm oil as part of the drug delivery system seemed to improve the bioavailability and solubility of the drug, stabilising emulsification of formulation between emulsifier and surfactant, promoting enhanced drug permeability and performance, as well as extending the shelf-life of the drug. Despite the complexity in designing lipid-based formulations, palm oil has proven to offer dynamic behaviour in providing versatility in drug design, form and delivery. However, the knowledge and application of palm oil and its fractions in lipid-based formulation are scarce and interspersed. Therefore, this study aims to focus on the research and outcomes of using palm oil in lipid-based formulations and drug delivery systems, due to the importance of establishing its capabilities and benefits.

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Kim, Min-Hwan, Yae-Eun Jeon, Soobeen Kang, Jae-Young Lee, Ki Won Lee, Ki-Taek Kim, and Dae-Duk Kim. "Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol." Pharmaceutics 12, no. 9 (September 3, 2020): 845. http://dx.doi.org/10.3390/pharmaceutics12090845.

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Orobol is one of the major soy isoflavones, and has been reported to have various pharmacological activities, including an anti-skin-aging effect. However, since it has low solubility in water and physicochemical instability, the formulation of orobol for delivery into the dermal layer of the skin could be challenging. The objective of this study was to prepare lipid nanoparticles formulations of orobol to enhance its stability as well as its deposition into the skin. Formulations of orobol-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were characterized in terms of their mean particle size, entrapment efficiency, and morphology. The nano-sized spherical NLCs formulations maintained the stability of orobol for up to 28 days. Moreover, the NLCs formulation significantly increased the in vitro deposition of orobol into both Strat-M membranes and human cadaver skin compared with the other formulations. Additionally, the NLCs formulation did not cause significant skin irritation in clinical study. These results demonstrate that a shea butter-based NLC formulation could be a promising and safe carrier system for improving the stability of orobol and enhancing its topical skin delivery.

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Gómez-Aguado, Itziar, Julen Rodríguez-Castejón, Mónica Vicente-Pascual, Alicia Rodríguez-Gascón, Ana del Pozo-Rodríguez, and María Ángeles Solinís Aspiazu. "Nucleic Acid Delivery by Solid Lipid Nanoparticles Containing Switchable Lipids: Plasmid DNA vs. Messenger RNA." Molecules 25, no. 24 (December 18, 2020): 5995. http://dx.doi.org/10.3390/molecules25245995.

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The development of safe and effective nucleic acid delivery systems remains a challenge, with solid lipid nanoparticle (SLN)-based vectors as one of the most studied systems. In this work, different SLNs were developed, by combination of cationic and ionizable lipids, for delivery of mRNA and pDNA. The influence of formulation factors on transfection efficacy, protein expression and intracellular disposition of the nucleic acid was evaluated in human retinal pigment epithelial cells (ARPE-19) and human embryonic kidney cells (HEK-293). A long-term stability study of the vectors was also performed. The mRNA formulations induced a higher percentage of transfected cells than those containing pDNA, mainly in ARPE-19 cells; however, the pDNA formulations induced a greater protein production per cell in this cell line. Protein production was conditioned by energy-dependent or independent entry mechanisms, depending on the cell line, SLN composition and kind of nucleic acid delivered. Vectors containing 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) as unique cationic lipid showed better stability after seven months, which improved with the addition of a polysaccharide to the vectors. Transfection efficacy and long-term stability of mRNA vectors were more influenced by formulation-related factors than those containing pDNA; in particular, the SLNs containing only DOTAP were the most promising formulations for nucleic acid delivery.

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Parks, Colby L., William Tucker, Corey A. Amlong, Sandro Mecozzi, and Robert A. Pearce. "Lipid-free Fluoropolymer-based Propofol Emulsions and Lipid Reversal of Propofol Anesthesia in Rats." Anesthesiology 124, no. 6 (June 1, 2016): 1328–37. http://dx.doi.org/10.1097/aln.0000000000001080.

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Abstract Background Propofol, as a lipid-based emulsion, is effective at inducing anesthesia. It does, however, suffer from several drawbacks, including microbial growth, hyperlipidemia, and pain on injection. In this study, the authors examined the ability of four lipid-free propofol nanoemulsions to induce anesthesia in rats and tested whether a subsequent lipid bolus would accelerate emergence from anesthesia. Methods The authors administered five formulations of propofol intravenously to six rats, delivering five different doses five times each, in a repeated-measures randomized crossover design and measured time to loss and recovery of righting reflex. The formulations included (1) Diprivan (AstraZeneca, United Kingdom); (2) L3, incorporating a semifluorinated surfactant plus egg lecithin; (3) B8, incorporating a semifluorinated surfactant only; (4) F8, incorporating a semifluorinated surfactant plus perfluorooctyl bromide; and (5) L80, incorporating egg lecithin only. In a second phase of the study, the authors administered a lipid bolus immediately after a dose of B8 or Diprivan. Results All formulations except L80 impaired the righting reflex without apparent toxic effects. The authors estimated the threshold dose for induction by determining the x-intercept of the linear regression between time to recovery versus log dose. Threshold doses ranged from 5.8 (95% CI, 5.5 to 6.2) to 8.6 (95% CI, 7.2 to 10.2) mg/kg. A 15 ml/kg lipid bolus resulted in an accelerated clearance. Conclusions Three of the four novel lipid-free fluoropolymer-based formulations showed efficacy in producing anesthesia, which was comparable to that of Diprivan, and a lipid bolus hastened recovery. These novel propofol formulations have the potential to avoid complications seen with the existing lipid-based formulation.

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Tollemar, Jan, and Olle Ringdén. "Lipid Formulations of Amphotericin B." Drug Safety 13, no. 4 (October 1995): 207–18. http://dx.doi.org/10.2165/00002018-199513040-00001.

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Janknegt, Robert, Els WM van Etten, and Simon de Marie. "Lipid formulations of amphotericin B." Current Opinion in Infectious Diseases 9, no. 6 (December 1996): 403–6. http://dx.doi.org/10.1097/00001432-199612000-00008.

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Foubert, Imogen, and Fernando Leal-Calderon. "Lipid formulations, structuring, and crystallization." European Journal of Lipid Science and Technology 117, no. 11 (November 2015): 1681–83. http://dx.doi.org/10.1002/ejlt.201500428.

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VIDT, D. G., E. JONES, and M. GOLDMAN. "Lipid formulations of amphotericin B." Cleveland Clinic Journal of Medicine 65, no. 8 (September 1, 1998): 423–27. http://dx.doi.org/10.3949/ccjm.65.8.423.

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Walsh, Thomas J., and John Hiemenz. "LIPID FORMULATIONS OF AMPHOTERICIN B." Infectious Diseases in Clinical Practice 7, no. 1 (March 1998): S16–27. http://dx.doi.org/10.1097/00019048-199803000-00004.

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Al-Abdely, Hail, Sanjay Revankar, and John Graybill. "Lipid Formulations of Amphotericin B." Seminars in Respiratory and Critical Care Medicine 18, no. 03 (May 1997): 289–99. http://dx.doi.org/10.1055/s-2008-1070998.

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Pamornpathomkul, Boonnada, Worranan Rangsimawong, Theerasak Rojanarata, Praneet Opanasopit, Chuleerath Chaiyodsilp, and Tanasait Ngawhirunpat. "Lipid-based nanocarriers to enhance skin permeation and antioxidant activity of Centella asiatica extract." MATEC Web of Conferences 192 (2018): 01016. http://dx.doi.org/10.1051/matecconf/201819201016.

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The purpose of this study was to evaluate the use of different formulations, including solution, gel, liposome and niosome for in vitro skin permeation and antioxidant activity of Centella asiatica (CA) extract. The liposomes and niosomes loaded with CA were characterized to observe the physicochemical properties i.e., particle size, zeta potential, percentage of entrapment efficiency (%EE) and percentage of loading efficiency (%LE). In vitro skin permeation studies revealed that liposome formulations had a superior enhancing effect on skin permeation compared to niosome, gel and solution formulation. Upon applied niosome formulations for the delivery of CA extract at 24 hours (h), the antioxidant activity was higher than liposome, gel and solution formulation, as evidenced by the increased in percent inhibition using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. However, there was no significant difference in antioxidant activity between niosome and liposome formulations. Accordingly, both the liposome and noisome formulations are promising approaches for transdermal delivery of CA extract for promoting successful antioxidant activity.

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Dobreva, Mirena, Stefan Stefanov, and Velichka Andonova. "Natural Lipids as Structural Components of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Topical Delivery." Current Pharmaceutical Design 26, no. 36 (October 23, 2020): 4524–35. http://dx.doi.org/10.2174/1381612826666200514221649.

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Background: Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) are useful drug delivery systems for dermal application. Thanks to their biocompatible and biodegradable profile, these carriers offer many advantages such as enhanced bioavailability, low toxicity, viable drug targeting and controlled release. SLN and NLC are composed of well-tolerated lipids, including natural fats and oils that are successfully used in the pharmaceutical and cosmetic dermal formulation. Objective: This article presents an overview of the benefits of selecting natural fats and oils as structural components of SLN and NLC for topical application. Methods: This review is based on data published over the past 20 years about the development of stable and nontoxic lipid nanoparticles with natural lipids. We shed light on the role of natural fats in skin restoration, as well as on the contributed penetration and occlusive properties of SLN and NLC. Results: The deliberate selection of excipients (type and lipid ratio) influences the quality of the final dermal formulation. Natural lipids show good compatibility with different active molecules and are able to create stable lipid matrices that facilitate the biopharmaceutical properties of lipid nanoparticles. Patents involving natural fats and oils in SLN and NLC composition are listed, yet it is important to note that the approved marketed formulations are mainly cosmetic, not pharmaceutical, products. Conclusion: Natural lipids can enhance topical drug delivery by adding their ability of improving skin penetration and hydration to the permeation and occlusion properties of SLN and NLC.

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Omer, Mustafa E., Majed Halwani, Rayan M. Alenazi, Omar Alharbi, Shokran Aljihani, Salam Massadeh, Majed Al Ghoribi, Manal Al Aamery, and Alaa Eldeen Yassin. "Novel Self-Assembled Polycaprolactone–Lipid Hybrid Nanoparticles Enhance the Antibacterial Activity of Ciprofloxacin." SLAS TECHNOLOGY: Translating Life Sciences Innovation 25, no. 6 (July 31, 2020): 598–607. http://dx.doi.org/10.1177/2472630320943126.

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Ciprofloxacin (CIP), a widely used antibiotic, is a poor biopharmaceutical resulting in low bioavailability. We optimized a CIP polymer–lipid hybrid nanoparticle (CIP-PLN) delivery system to enhance its biopharmaceutical attributes and the overall therapeutic performance. CIP-PLN formulations were prepared by a direct emulsification–solvent–evaporation method. Varying the type and ratio of lipid was tried to optimize a CIP-PLN formulation. All the prepared formulations were evaluated for their particle size, polydispersity index, zeta potential, physical stability, and drug entrapment efficiency. The drug in vitro release profile was also studied. Antibacterial activities were tested by the agar diffusion method for all CIP-PLN formulations against an Escherichia coli clinical bacterial isolate (EC04). CIP-PLN formulations showed average sizes in the range of 133.9 ± 1.7 nm to 217.1 ± 0.8 nm, exhibiting high size uniformity as indicated by polydispersity indices lower than 0.25. The entrapment efficiency was close to 80% for all formulations. The differential scanning calorimetry (DSC) thermograms indicated the existence of CIP in the amorphous state in all PLN formulations. Fourier transform infrared spectra indicated deep incorporation of molecular CIP within the polymer matrix. The release profile of CIP from PLN formulas showed a uniform prolonged drug profile, extended for a week from most formulations with a zero-order kinetics. The antibacterial activity of CIP-PLN formulations showed significantly higher antibacterial activity only with F4 containing lecithin as the lipid component. In conclusion, we successfully optimized a CIP-PLN formulation with a low nanoparticle size in a close range, high percentage of entrapment efficiency and drug loading, uniform prolonged release rate, and higher antibacterial activity against the EC04 clinical isolate.

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Tay, Erin, Tri-Hung Nguyen, Leigh Ford, Hywel D. Williams, Hassan Benameur, Peter J. Scammells, and Christopher J. H. Porter. "Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure." Pharmaceutics 12, no. 1 (December 22, 2019): 17. http://dx.doi.org/10.3390/pharmaceutics12010017.

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Lipid based formulations (LBFs) are commonly employed to enhance the absorption of highly lipophilic, poorly water-soluble drugs. However, the utility of LBFs can be limited by low drug solubility in the formulation. Isolation of ionizable drugs as low melting, lipophilic salts or ionic liquids (ILs) provides one means to enhance drug solubility in LBFs. However, whether different ILs benefit from formulation in different LBFs is largely unknown. In the current studies, lumefantrine was isolated as a number of different lipophilic salt/ionic liquid forms and performance was assessed after formulation in a range of LBFs. The solubility of lumefantrine in LBF was enhanced 2- to 80-fold by isolation as the lumefantrine docusate IL when compared to lumefantrine free base. The increase in drug loading subsequently enhanced concentrations in the aqueous phase of model intestinal fluids during in vitro dispersion and digestion testing of the LBF. To assess in vivo performance, the systemic exposure of lumefantrine docusate after administration in Type II-MCF, IIIB-MCF, IIIB-LCF, and IV formulations was evaluated after oral administration to rats. In vivo exposure was compared to control lipid and aqueous suspension formulations of lumefantrine free base. Lumefantrine docusate in the Type IIIB-LCF showed significantly higher plasma exposure compared to all other formulations (up to 35-fold higher). The data suggest that isolation of a lipid-soluble IL, coupled with an appropriate formulation, is a viable means to increase drug dose in an oral formulation and to enhance exposure of lumefantrine in vivo.

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Söderberg, Lars, Henrik Dyhre, Bodil Roth, and Sven Björkman. "Ultralong Peripheral Nerve Block by Lidocaine:Prilocaine 1:1 Mixture in a Lipid Depot Formulation." Anesthesiology 104, no. 1 (January 1, 2006): 110–21. http://dx.doi.org/10.1097/00000542-200601000-00017.

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Background The aim of this study was to develop stable and easily injectable lipid depot preparations of local anesthetics in which the drug concentration can be varied according to desired duration of action. Methods The formulations contained a 2.0, 5.0, 10, 20, 40, 60, 80, or 100% eutectic mixture of lidocaine and prilocaine base in medium-chain triglyceride. Duration of sciatic nerve block and local neurotoxicity was investigated in rats with 2.0% lidocaine:prilocaine HCl solution and 99.5% ethanol as controls. The rate of release of local anesthetic from the site of administration and the possibility to predict in vivo depot characteristics from in vitro release data were investigated for the 20 and 60% formulations. Results The duration of sensory sciatic block was prolonged 3 times with the 20% formulation and approximately 180 times with the 60% formulation, in comparison with the 2% aqueous solution. With the 80 and 100% formulations, all animals still showed nerve block after 2 weeks. The in vivo release of local anesthetic could be approximately predicted from in vitro data for the 20% but not for the 60% formulation. The formulations of 60% or greater and ethanol showed neurotoxic effects. Conclusions The pharmaceutical properties of these formulations compare favorably with those of other depot preparations. The high-percentage ones showed the longest duration of action yet reported for sciatic nerve block in rats. The possibility of using a high-concentration local anesthetic depot formulation as an alternative to ethanol or phenol for long-term nerve blocks in chronic pain merits further investigation.

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Dupont, Bertrand. "Overview of the lipid formulations of amphotericin B." Journal of Antimicrobial Chemotherapy 49, suppl_1 (January 1, 2002): 31–36. http://dx.doi.org/10.1093/jac/49.suppl_1.31.

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Abstract Invasive fungal infections have been increasingly recognized as a major cause of morbidity and mortality in the immunocompromised host. Amphotericin B has a broad spectrum and has remained the drug of choice for life-threatening invasive fungal infections. However, adverse events, particularly renal insufficiency, are limiting factors in achieving an effective dose: the prescription of amphotericin B is a compromise between toxicity and efficacy. Lipid formulations offer a better therapeutic index by circumscribing amphotericin B toxicity. Three lipid formulations are available in most countries: AmBisome, the only true liposome; Abelcet, with a ribbon-like structure; and Amphocil/Amphotec, composed of disc-like structures. All these formulations contain amphotericin B, but they differ in shape, size, reticuloendothelial clearance, Cmax, AUC and visceral diffusion. The impact of these differences in pharmacokinetics and pharmacodynamics on clinical efficacy is still unclear. Efficacy has been shown in neutropenic patients with fever of unknown origin, systemic candidosis, invasive aspergillosis, cryptococcal meningitis and a variety of other difficult-to-treat mycoses, such as Fusarium or Zygomycetes infections. The effective dose may vary from one formulation to the other and is c. 3–5 mg/kg/day. All formulations are less nephrotoxic than amphotericin B. In one randomized double-blind study, AmBisome 3 or 5 mg/kg/day was less nephrotoxic and gave fewer infusion-related events than Abelcet 5 mg/kg/day. Abelcet induces fewer infusion-related side effects than Amphocil. All formulations seem at least as effective as amphotericin B. In some patients with life-threatening mycosis who failed treatment with, or were intolerant to, amphotericin B, the lipid formulations were effective. Further studies with comparable selected high-risk patients are warranted to clarify the usefulness and the indications of each of the formulations. Cost is a factor limiting prescription in many institutions, where use is often restricted to patients intolerant of, or refractory to, amphotericin B.

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Guo, Wenjin, and Robert J. Lee. "Efficient Gene Delivery Using Anionic Liposome-Complexed Polyplexes (LPDII)." Bioscience Reports 20, no. 5 (October 1, 2000): 419–32. http://dx.doi.org/10.1023/a:1010338219401.

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Synthetic gene transfer vectors based on polyplexes complexed to anionic liposomes (LPDII vectors) were characterized for their transfection efficiency in cultured mammalian cells. The effects of polycation to DNA ratio, lipid to DNA ratio, choice of polycation and lipid composition were systematically evaluated in human oral carcinoma KB cells, using a luciferase reporter gene. For LPDII formulations containing poly-L-lysine and dioeoylphosphatidylethanolamine/cholesteryl hemisuccinate (DOPE/CHEMS) anionic liposomes, at a constant lipid to DNA ratio, an increase in the polycation/DNA (N/P) ratio resulted in an increase in transfection activity. Meanwhile, the optimal lipid to DNA ratio for efficient gene delivery was influenced by the N/P ratio used, and was increased at higher N/P ratios. For the DNA condensing agent, poly-L-lysine could be replaced by polyethylenimine (PEI) as the DNA condensing agent in the formulations. For the lipidic components, CHEMS could be replaced by other anioniclipids including oleic acid, dicetylphosphate and phosphatidylserine, but DOPE, a fusogenic helper lipid, could not be replaced by dioleolyphosphatidylcholine. LPDII formulation showed significantly less cytotoxicity compared to the commonly used cationic lipsomes or PEI mediated transfection and several cell lines were transfected with high efficiency. LPDII vectors avoid the use of toxic cationic lipids and may have potential application in gene therapy.

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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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Rahnfeld, Lisa, and Paola Luciani. "Injectable Lipid-Based Depot Formulations: Where Do We Stand?" Pharmaceutics 12, no. 6 (June 19, 2020): 567. http://dx.doi.org/10.3390/pharmaceutics12060567.

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The remarkable number of new molecular entities approved per year as parenteral drugs, such as biologics and complex active pharmaceutical ingredients, calls for innovative and tunable drug delivery systems. Besides making these classes of drugs available in the body, injectable depot formulations offer the unique advantage in the parenteral world of reducing the number of required injections, thus increasing effectiveness as well as patient compliance. To date, a plethora of excipients has been proposed to formulate depot systems, and among those, lipids stand out due to their unique biocompatibility properties and safety profile. Looking at the several long-acting drug delivery systems based on lipids designed so far, a legitimate question may arise: How far away are we from an ideal depot formulation? Here, we review sustained release lipid-based platforms developed in the last 5 years, namely oil-based solutions, liposomal systems, in situ forming systems, solid particles, and implants, and we critically discuss the requirements for an ideal depot formulation with respect to the used excipients, biocompatibility, and the challenges presented by the manufacturing process. Finally, we delve into lights and shadows originating from the current setups of in vitro release assays developed with the aim of assessing the translational potential of depot injectables.

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&NA;. "Lipid-based formulations of amphotericin B." Drugs & Therapy Perspectives 13, no. 11 (June 1999): 1–5. http://dx.doi.org/10.2165/00042310-199913110-00001.

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Herbrecht, Raoul, Shanti Natarajan-Amé, Yasmine Nivoix, and Valérie Letscher-Bru. "The lipid formulations of amphotericin B." Expert Opinion on Pharmacotherapy 4, no. 8 (August 2003): 1277–87. http://dx.doi.org/10.1517/14656566.4.8.1277.

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SWENSON, C. E., L. E. BOLCSAK, W. R. PERKINS, and A. S. JANOFF. "Lipid-based formulations of amphotericin B." Journal of Antimicrobial Chemotherapy 35, no. 5 (1995): 709–11. http://dx.doi.org/10.1093/jac/35.5.709.

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MOREAU, P. "Lipid-based formulations of amphotericin B." Journal of Antimicrobial Chemotherapy 35, no. 5 (1995): 711. http://dx.doi.org/10.1093/jac/35.5.711.

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CHAVANET, P., and D. CAILLOT. "Lipid-based formulations of amphotericin B." Journal of Antimicrobial Chemotherapy 35, no. 5 (1995): 711–13. http://dx.doi.org/10.1093/jac/35.5.711-a.

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O'Marcaigh, Aengus S., and Donna L. Betcher. "Amphotericin B and Its Lipid Formulations." Journal of Pediatric Oncology Nursing 11, no. 3 (January 1994): 125–27. http://dx.doi.org/10.1177/104345429401100308.

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Plotnick, Arnold N. "Lipid-based formulations of amphotericin B." Journal of the American Veterinary Medical Association 216, no. 6 (March 2000): 838–41. http://dx.doi.org/10.2460/javma.2000.216.838.

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Veerareddy, P. R., and V. Vobalaboina. "Lipid-based formulations of amphotericin B." Drugs of Today 40, no. 2 (2004): 133. http://dx.doi.org/10.1358/dot.2004.40.2.799425.

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Malisiova, Fotini, Sophia Hatziantoniou, Kostas Dimas, Dimitrios Kletstas, and Costas Demetzos. "Liposomal Formulations from Phospholipids of Greek Almond Oil. Properties and Biological Activity." Zeitschrift für Naturforschung C 59, no. 5-6 (June 1, 2004): 330–34. http://dx.doi.org/10.1515/znc-2004-5-607.

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The seeds of the almond tree [(Prunus dulcis (Mill.) D. A. Webb. (syn. Prunus amygdalus)] were collected in two different periods of maturity and were studied for their lipid content. The total lipids (TL) were extracted by the Bligh-Dyer method and the lipid classes have been isolated by chromatographic techniques and were analyzed by HPTLC coupled with a flame ionization detector (HPTLC/FID) and GC-MS. The oils were found to be rich in neutral lipids (89.9% and 96.3% of total lipids) and low in polar lipids (10.1% and 3.7% of total lipids) for the immature and mature seed oils, respectively. The neutral lipid fraction consisted mainly of triacylglycerides whereas the polar lipids mainly consisted of phospholipids. GC-MS data showed that the main fatty acid for both oils was 9-octadecenoic acid (oleic acid). The unsaturated fatty acids were found as high as 89.4% and 89.7%, while the percentage of the saturated fatty acids was found 10.6% and 10.3% for the immature and mature seed oils, respectively. Liposomes were prepared from the isolated phospholipids using the thin lipid film methodology, and their physical properties were characterized. Cytotoxicity was found absent when assayed against normal and cancerous cell lines. These new formulations may have future applications for encapsulation and delivery of drugs and cosmetically active ingredients.

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Xiao, Lu, Tao Yi, Ying Liu, and Hua Zhou. "TheIn VitroLipolysis of Lipid-Based Drug Delivery Systems: A Newly Identified Relationship between Drug Release and Liquid Crystalline Phase." BioMed Research International 2016 (2016): 1–9. http://dx.doi.org/10.1155/2016/2364317.

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The purpose of this study was to offer a new insight into the microstructure changes duringin vitrolipolysis of five lipid-based drug delivery formulations belonging to different lipid formulation types. Five lipid-based formulations of indomethacin were investigated using anin vitrolipolysis model. During lipolysis, microstructures of the intermediate phase formed by lipolytic products were observed. The results showed that the time of liquid crystal formation duringin vitrodigestion for these formulations was Type I > Type II > Type IIIB > Type IV > Type IIIA (p<0.05). After lipolysis, the drug releases from these formulations were determined. The results showed that the amount of drug distributed in the aqueous phase, obtained by ultracentrifuge after lipolysis, was, astonishingly, in inverse rank order of the above mentioned, that is, Type IIIA > Type IV > Type IIIB > Type II > Type I (p<0.05). These results showed that the liquid crystalline phase probably has a critical influence on the fate of the drug duringin vitrolipolysis and suggested that the liquid crystalline phase facilitated drug precipitation. These findings may improve the understanding of lipolysis of lipid-based drug delivery systems for designing better delivery system.

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Tsamouris, George, Sophia Hatziantoniou, and Costas Demetzos. "Lipid Analysis of Greek Walnut Oil (Juglans regia L.)." Zeitschrift für Naturforschung C 57, no. 1-2 (February 1, 2002): 51–56. http://dx.doi.org/10.1515/znc-2002-1-209.

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The walnut oil (Juglans regia L.) total lipids (TL) were extracted by the Bligh-Dyer method and the lipid classes have been isolated by chromatographic techniques and they were analyzed by high performance thin layer chromatography (HPTLC) /FID and GC-MS. The oil was found to be rich in neutral lipids (96.9% of total lipids) and low in polar lipids (3.1% of total lipids). The neutral lipid fraction consisted mainly of triacylglycerides whereas the polar lipids mainly consisted of sphingolipids. GC-MS data showed that the main fatty acid was linoleic acid. Unsaturated fatty acids were found as high as 85%, while the percentage of the saturated fatty acids was found 15%. Two types of liposomes were prepared from the isolated walnut oil phospholipids and characterized as new formulations. These formulations may have future applications for encapsulation and delivery of drugs and cosmetic active ingredients.

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Faustino and Pinheiro. "Lipid Systems for the Delivery of Amphotericin B in Antifungal Therapy." Pharmaceutics 12, no. 1 (January 1, 2020): 29. http://dx.doi.org/10.3390/pharmaceutics12010029.

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Amphotericin B (AmB), a broad-spectrum polyene antibiotic in the clinic for more than fifty years, remains the gold standard in the treatment of life-threatening invasive fungal infections and visceral leishmaniasis. Due to its poor water solubility and membrane permeability, AmB is conventionally formulated with deoxycholate as a micellar suspension for intravenous administration, but severe infusion-related side effects and nephrotoxicity hamper its therapeutic potential. Lipid-based formulations, such as liposomal AmB, have been developed which significantly reduce the toxic side effects of the drug. However, their high cost and the need for parenteral administration limit their widespread use. Therefore, delivery systems that can retain or even enhance antimicrobial efficacy while simultaneously reducing AmB adverse events are an active area of research. Among those, lipid systems have been extensively investigated due to the high affinity of AmB for binding lipids. The development of a safe and cost-effective oral formulation able to improve drug accessibility would be a major breakthrough, and several lipid systems for the oral delivery of AmB are currently under development. This review summarizes recent advances in lipid-based systems for targeted delivery of AmB focusing on non-parenteral nanoparticulate formulations mainly investigated over the last five years and highlighting those that are currently in clinical trials.

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Larabi, Malika, Vanessa Yardley, Philippe M. Loiseau, Martine Appel, Philippe Legrand, Annette Gulik, Christian Bories, Simon L. Croft, and Gillian Barratt. "Toxicity and Antileishmanial Activity of a New Stable Lipid Suspension of Amphotericin B." Antimicrobial Agents and Chemotherapy 47, no. 12 (December 2003): 3774–79. http://dx.doi.org/10.1128/aac.47.12.3774-3779.2003.

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ABSTRACT The aim of the present study was to evaluate the toxicity and the activity of a new lipid complex formulation of amphotericin B (AMB) (LC-AMB; dimyristoyl phosphatidylcholine, dimyristoyl phosphatidylglycerol, and AMB) that can be produced by a simple process. Like other lipid formulations, this new complex reduced both the hemolytic activity of AMB (the concentration causing 50% hemolysis of human erythrocytes, >100 μg/ml) and its toxicity toward murine peritoneal macrophages (50% inhibitory concentration, >100 μg/ml at 24 h). The in vivo toxicity of the new formulation (50% lethal dose,> 200 mg/kg of body weight for CD1 mice) was similar to those of other commercial lipid formulations of AMB. The complex was the most effective formulation against the DD8 strain of Leishmania donovani. It was unable to reverse the resistance of an AMB-resistant L. donovani strain. In vivo LC-AMB was less efficient than AmBisome against L. donovani.

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Akula, Samatha, Aravind Kumar Gurram, and Srinivas Reddy Devireddy. "Self-Microemulsifying Drug Delivery Systems: An Attractive Strategy for Enhanced Therapeutic Profile." International Scholarly Research Notices 2014 (December 8, 2014): 1–11. http://dx.doi.org/10.1155/2014/964051.

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Ease of administration and painless approach made oral route the most preferred. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of dissolution rate limited absorption. Failure to attain intended therapeutic effect of the poor water soluble drugs by this route led to development of novel drug delivery systems which will fulfill therapeutic needs with minimum dose. Although many formulation approaches like solid dispersions, complexation, pH modification, and cocrystals exist, lipid based delivery systems finding increased appliance with the apparent increase in absorption of drug. Among lipid based formulations, self-microemulsifying formulations (droplet size < 100 nm) are evident to improve the oral bioavailability of hydrophobic drugs primarily due to their efficiency in facilitating solubilization and in presenting the hydrophobic drug in solubilized form whereby dissolution process can be circumvented. Various components that are used to formulate these dosage forms like surfactants and lipids contribute to the overall improvement in oral bioavailability via promoting the lymphatic transport; thereby hepatic first pass metabolism can be surmounted. The present paper gives exhaustive information on the formulation design and characterization of SMEDDS along with the probable mechanisms by which the bioavailability can be improved with SMEDDS.

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Sánchez-López, Elena, Anna Paús, Ignacio Pérez-Pomeda, Ana Calpena, Isabel Haro, and María José Gómara. "Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide." Pharmaceutics 12, no. 6 (May 31, 2020): 502. http://dx.doi.org/10.3390/pharmaceutics12060502.

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The effective use of fusion inhibitor peptides against cervical and colorectal infections requires the development of sustained release formulations. In this work we comparatively study two different formulations based on polymeric nanoparticles and lipid vesicles to propose a suitable delivery nanosystem for releasing an HIV-1 fusion inhibitor peptide in vaginal mucosa. Polymeric nanoparticles of poly-d,l-lactic-co-glycolic acid (PLGA) and lipid large unilamellar vesicles loaded with the inhibitor peptide were prepared. Both formulations showed average sizes and polydispersity index values corresponding to monodisperse systems appropriate for vaginal permeation. High entrapment efficiency of the inhibitor peptide was achieved in lipid vesicles, which was probably due to the peptide’s hydrophobic nature. In addition, both nanocarriers remained stable after two weeks stored at 4 °C. While PLGA nanoparticles (NPs) did not show any delay in peptide release, lipid vesicles demonstrated favorably prolonged release of the peptide. Lipid vesicles were shown to improve the retention of the peptide on ex vivo vaginal tissue in a concentration sufficient to exert its pharmacological effect. Thus, the small size of lipid vesicles, their lipid-based composition as well as their ability to enhance peptide penetration on vaginal tissue led us to consider this formulation as a better nanosystem than polymeric nanoparticles for the sustained delivery of the HIV-1 fusion inhibitor peptide in vaginal tissues.

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Chintamani Panda, Sachinkumar Prabhubhai Chauhan, and Krishnan Balamurugan. "Formulation and In Vitro Characterization of Raloxifene Nanostructured Lipid Carriers For Oral Delivery With Full Factorial Design-Based Studies Using Quality By Design (QbD) Approach." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (October 19, 2020): 6417–27. http://dx.doi.org/10.26452/ijrps.v11i4.3434.

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The main aim of the present study is to improve the dissolution rate of Raloxifene Hydrochloride by formulating nanostructured lipid carriers (NLC) using Quality by Design (QbD) approach. The formulations of NLC-RH were prepared by the ultrasonication method using stearic acid as solid lipid, medium-chain triglyceride as the liquid lipid and polysorbate 80 as the surface-active agent. Two most critical quality attributes (CQAs) for NLC-RH were particle size and entrapment efficiency. The other attributes of medium influence identified includes dissolution rate, zeta potential and particle size didtribution. The Critical Material Attributes (CMAs) identified were solid lipid/liquid lipid ratio and surfactant concentration. The time required for ultrasonication was selected as a Critical Process Parameter (CPP). The 23 full factorial design was used to evaluate the relationship between the CMAs and CPPs variable. Based on the experiments, the composition of the optimal formulation is achieved with solid lipid/liquid lipid ratio of 7:3 and 7 % of surfactant concentration with 15 min of ultrasonication time. The optimized formulation of NLC-RH was found to be with a mean particle size of 146 nm with narrow particle size distributions. From the above results, it is concluded that a promising Raloxifene HCl loaded NLC could give a novel and potential therapy for osteoporosis.

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Mohd Azharuddin, Theivendren Panner Selvam, Maya Sharma, and Jayesh Dwivedi. "Design development and evaluation of novel ophthalmic nano lipid in situ gel-forming solution using timolol hydrochloride." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (December 5, 2020): 6837–44. http://dx.doi.org/10.26452/ijrps.v11i4.3654.

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The present research work was aimed to design, develop and evaluate the nano lipid-based drug delivery system by incorporating timolol hydrochloride drug for ocular therapy and improve the release of the drug through the ocular route. Nanolipids in situ gels were prepared by film hydration method involving two steps. First nano lipids were formulated with the help of organic solvents, and then they were incorporated into a gel by using gelling agents. FTIR spectrum studies were carried out for drug and the formulations which reveal that there was no interaction between the drug and excipients used. The various formulations prepared were subjected for the different evaluation parameters, which showed good and effective results for visual appearance, pH, gelation study, viscosity and ocular irritation studies. It was further observed from this research work that formulation TF2 (HPMC K-15M 0.2%w/v and Carbopol 940 0.4%w/v) had a maximum entrapment efficiency of 97.30%, drug content of about 97.67% and drug release of about 84.29% for 10 hrs. Stability studies were carried out for TF2 formulation, and they found that they were stable throughout the study period. It was finally concluded from the present work that formulations prepared were more suitable and had good patient compliance compared to the eye drops.

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Šoltýsová, I., D. Toropilová, and T. de Vringer. "Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation." Folia Veterinaria 60, no. 4 (December 1, 2016): 63–69. http://dx.doi.org/10.1515/fv-2016-0040.

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Abstract Active ingredients in pharmaceuticals differ by their physico-chemical properties and their bioavailability therefore varies. The most frequently used and most convenient way of administration of medicines is oral, however many drugs are little soluble in water. Thus they are not sufficiently effective and suitable for such administration. For this reason a system of lipid based formulations (LBF) was developed. Series of formulations were prepared and tested in water and biorelevant media. On the basis of selection criteria, there were selected formulations with the best emulsification potential, good dispersion in the environment and physical stability. Samples of structurally different drugs included in the Class II of the Biopharmaceutics classification system (BCS) were obtained, namely Griseofulvin, Glibenclamide, Carbamazepine, Haloperidol, Itraconazol, Triclosan, Praziquantel and Rifaximin, for testing of maximal saturation in formulations prepared from commercially available excipients. Methods were developed for preparation of formulations, observation of emulsification and its description, determination of maximum solubility of drug samples in the respective formulation and subsequent analysis. Saturation of formulations with drugs showed that formulations 80 % XA and 20 % Xh, 35 % XF and 65 % Xh were best able to dissolve the drugs which supports the hypothesis that it is desirable to identify limited series of formulations which could be generally applied for this purpose.

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Pereira, Rayanne R., Matteo Testi, Francesca Rossi, Jose O. C. Silva Junior, Roseane M. Ribeiro-Costa, Ruggero Bettini, Patrizia Santi, Cristina Padula, and Fabio Sonvico. "Ucuùba (Virola surinamensis) Fat-Based Nanostructured Lipid Carriers for Nail Drug Delivery of Ketoconazole: Development and Optimization Using Box-Behnken Design." Pharmaceutics 11, no. 6 (June 17, 2019): 284. http://dx.doi.org/10.3390/pharmaceutics11060284.

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Ucuùba fat is fat obtained from a plant found in South America, mainly in Amazonian Brazil. Due to its biocompatibility and bioactivity, Ucuùba fat was used for the production of ketoconazole-loaded nanostructured lipid carriers (NLC) in view of an application for the treatment of onychomycosis and other persistent fungal infections. The development and optimization of Ucuùba fat-based NLC were performed using a Box-Behnken design of experiments. The independent variables were surfactant concentration (% w/v), liquid lipids concentration (% w/v), solid lipids concentration (% w/v), while the outputs of interest were particle size, polydispersity index (PDI) and drug encapsulation efficiency (EE). Ucuùba fat-based NLC were produced and the process was optimized by the development of a predictive mathematical model. Applying the model, two formulations with pre-determined particle size, i.e., 30 and 85 nm, were produced for further evaluation. The optimized formulations were characterized and showed particle size in agreement to the predicted value, i.e., 33.6 nm and 74.6 nm, respectively. The optimized formulations were also characterized using multiple techniques in order to investigate the solid state of drug and excipients (DSC and XRD), particle morphology (TEM), drug release and interactions between the formulation components (FTIR). Furthermore, particle size, surface charge and drug loading efficiency of the formulations were studied during a one-month stability study and did not show evidence of significant modification.

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Journal articles on the topic 'Lipid formulations'

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