Development and characterization of oleic acid vesicles for the topical delivery of fluconazole (original) (raw)
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Novel vesicular carriers for topical drug delivery and their applications
International Journal of Pharmaceutical Sciences Review and Research
Delivery of drug through topical route represents a most convenient and novel approach. The major difficulty arises while delivering a drug through skin is its action as a natural barrier nature which makes it difficult for most drugs to penetrate into and permeate through it. Conventional topical formulations have not proved to be effective in dermal delivery of drug. Novel drug delivery systems bear great potential for dermal delivery. Among them lipidic and non-lipidic vesicular systems like liposome, noisome, transfersome and ethosome have been suggested to overcome the problems associated with conventional topical formulations. These vesicular systems were found to be more effective as they render controlled release of drug due to depot formation in skin and some were more effective in transdermal delivery. This article summarizes the potential of novel vesicular drug delivery carrier based dermal applications of the drug.
Keywords: liposomes nanoparticles drug delivery systems transdermal drug delivery permeability percutaneous controlled release colloid skin lipids a b s t r a c t In the recent decade, skin delivery (topical and transdermal) has gained an unprecedented popularity, especially due to increased incidences of chronic skin diseases, demand for targeted and patient compliant delivery, and interest in life cycle management strategies among pharmaceutical companies. Literature review of recent publications indicates that among various skin delivery systems, lipid-based delivery systems (vesicular carriers and lipid particulate systems) have been the most successful. Ve-sicular carriers consist of liposomes, ultradeformable liposomes, and ethosomes, while lipid particulate systems consist of lipospheres, solid lipid nanoparticles, and nanostructured lipid carriers. These systems can increase the skin drug transport by improving drug solubilization in the formulation, drug partitioning into the skin, and fluidizing skin lipids. Considering that lipid-based delivery systems are regarded as safe and efficient, they are proving to be an attractive delivery strategy for the pharmaceutical as well as cosmeceutical drug substances. However, development of these delivery systems requires comprehensive understanding of physicochemical characteristics of drug and delivery carriers, formulation and process variables, mechanism of skin delivery, recent technological advancements, specific limitations, and regulatory considerations. Therefore, this review article encompasses recent research advances addressing the aforementioned issues.
Pharmaceutics
10-hydroxy decanoic acid (HDA), a naturally derived fatty acid, was used for the preparation of novel fatty acid vesicles for comparison with oleic acid (OA) ufasomes. The vesicles were loaded with magnolol (Mag), a potential natural drug for skin cancer. Different formulations were prepared using the thin film hydration method and were statistically evaluated according to a Box–Behnken design in terms of particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE). The ex vivo skin permeation and deposition were assessed for Mag skin delivery. In vivo, an assessment of the optimized formulae using 7,12-dimethylbenz[a]anthracene (DMBA)-induced skin cancer in mice was also conducted. The PS and ZP of the optimized OA vesicles were 358.9 ± 3.2 nm and −82.50 ± 7.13 mV compared to 191.9 ± 6.28 nm and −59.60 ± 3.07 mV for HDA vesicles, respectively. The EE was high (>78%) for both types of vesicles. Ex vivo permeation studies revealed enhanced Ma...
Vesicular drug delivery for the treatment of topical disorders: current and future perspectives
Journal of Pharmacy and Pharmacology, 2021
ObjectivesVesicular drug delivery has become a useful approach for therapeutic administration of pharmaceutical compounds. Lipid vesicles have found application in membrane biology, immunology, genetic engineering and theragnostics. This review summarizes topical delivery, specifically dermal/transdermal, ocular and transungual, via these vesicles, including future formulation perspectives.Key findingsLiposomes and their subsequent derivatives, viz. niosomes, transferosomes, pharmacososmes and ethosomes, form a significant part of vesicular systems that have been successfully utilized in treating an array of topical disorders. These vesicles are thought to be a safe and effective mode of improving the delivery of lipophilic and hydrophilic drugs.SummarySeveral drug molecules are available for topical disorders. However, physicochemical properties and undesirable toxicity have limited their efficacy. Vesicular delivery systems have the potential to overcome these shortcomings due to ...
Dermal delivery of drugs using different vesicular carriers: A comparative review
Asian Journal of Pharmaceutics, 2012
Many skin diseases are based in the dermal layer of the skin like-acne, alopecia, psoriasis, herpes zoster, etc. Conventional topical formulations have not proved to be effective in managing these conditions because of poor retention in the skin. Some formulations do not penetrate through the stratum corneum and some pass through the skin very quickly.Therefore, there is need to develop a strategy to deliver drugs to the dermis for better management of these conditions. Vesicular systems like liposomes, niosomes, ethosomes and transfersomes have been used by many researchers to localize drugs in the dermal layer and have been fairly successful. Some vesicles were found to be more effective in retaining drug to the skin and some were more effective in transdermal delivery. This article summarizes and compares the work done in the last decade on this topic and provides a conclusion.
Lipid vesicles: A versatile drug delivery platform for dermal and transdermal applications
Colloids and Surfaces B: Biointerfaces, 2020
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Vesicles: Potential nano carriers for the delivery of skin cosmetics
Journal of cosmetic and laser therapy : official publication of the European Society for Laser Dermatology, 2017
In the present scenario, consumers are searching for personal care products that supply multiple benefits with minimal efforts. The outcome has been the introduction of nanotechnology-based cosmetic products that are safe to use and results driven. Some topical cosmetics can act efficaciously when they reach their target sites present in the deeper layers of the skin. The main problem with delivering active ingredients across the skin is the barrier function of the skin. Therefore, to get the maximum benefit from cosmetic products and to overcome the problems associated with their skin penetration, scientists are investigating various strategies to overcome these barrier properties. Vesicular carriers have been claimed to improve the topical delivery of active ingredients. This review offers a brief overview of current approaches in the research and development of vesicular carriers to improve the delivery and performance of active ingredients present in the cosmetics.
Pharmaceutics
Opportunistic fungal infections are responsible for over 1.5 million deaths per year. This has created a need for highly effective antifungal medication to be as potent as possible. In this study, we improved the efficacy of a common over the counter (OTC) antifungal skin medication, miconazole, by encapsulating nano-molecules of the drug in cholesterol/sodium oleate nano-vesicles. These nano-vesicles were characterized to optimize their size, zeta potential, polydispersity index and encapsulation efficiency. Furthermore, these nano-vesicles were compared to a conventional miconazole-based commercially available cream to determine potential improvements via permeation through the stratum corneum, cytotoxicity, and antifungal capabilities. Our results found that the vesicle size was within the nano range (~300 nm), with moderate polydispersity and stability. When compared with the commercially available cream, Actavis, as well as free miconazole, the miconazole nano-vesicle formulati...
International Journal of Applied Pharmaceutics, 2024
Objective: Terbinafine is a poorly water-soluble and highly permeable allylamine antifungal (BCS-II) drug. In this study, we looked at the possibility of using ethosomes as vesicular lipid nanocarriers to enhance the transdermal delivery of terbinafine. Methods: Using a 3 2 full factorial design, the ethosomal formulation with different soya lecithin and cholesterol concentrations was improved and optimized. The influence of independent variables, namely soya lecithin and cholesterol concentration in ethosomes was determined by estimating dependent variable including the particle size, polydispersity index, zeta potential, entrapment efficiency, and in vitro drug release. To improve the residence time of ethosomes on the topical application, the ethosomes were incorporated into the carbopol gel. 1% w/v of Carbopol 934 P gelembedded Terbinafine ethosomes were used to study medication release and skin interactions. Results: Optimized ratios of soya lecithin and cholestrol was used to prepare vesicles. Formulation had a particle size of 1207.39±2.71 nm, entrapment efficiency of 94.46±0.47%, and in vitro diffusion of 51.27±0.16%. It was found that the growth of fungus Aspergillus niger and Candida albicans were inhibited by Ethosomal Gel. However, ethosomal gel had more inhibitory activity on Apergillus niger compared to positive control. Conclusion: The current study suggests that ethosomal vesicles may improve transdermal dispersion without causing skin irritation. Terbinafineloaded ethosomes have the potential to be one of the most important transdermal application techniques for the treatment of fungi-related disorders.
Vitamin A-loaded solid lipid nanoparticles for topical use: drug release properties
Journal of Controlled Release, 2000
Burst release as well as sustained release has been reported for SLN suspensions. For dermal application, both features are of interest. Burst release can be useful to improve the penetration of a drug. Sustained release becomes important with active ingredients that are irritating at high concentrations or to supply the skin over a prolonged period of time with a drug. Glyceryl behenate SLN were loaded with vitamin A and the release profiles were studied. Franz diffusion cells were used to assess the release kinetic over a period of 24 h. Within the first 6 h retinol SLN displayed controlled release. After longer periods (12-24 h) the release rate increased and even exceeded the release rate of comparable nanoemulsions. Pure SLN dispersions are characterised by low viscosity. In contrast to membranous vesicles, SLN can also be stably incorporated in convenient topical dosage forms like hydrogels or creams. In the Franz diffusion cell these preparations showed a controlled release over 12-18 h. Similar to SLN dispersions an increase in release rate over a 24-h period was found. A good correlation between polymorphic transitions and increased drug release was observed in this study. Sustained release was often related to the metastable b9 polymorph. Drug expulsion is explained by a reduction of amorphous regions in the carrier lattice due to a b9→b polymorphic transition. This transformation can be controlled with surfactant mixtures or, in the case i of the hydrogel and oil / water cream, with humectants or gelling agents. Thus, the release rate for the topical route of application is adjustable.