Oleic acid vesicles: a new approach for topical delivery of antifungal agent

Abstract

The occurrence of topical fungal infections is increasing nowadays. Cutaneous fungal infections like cutaneous candidiasis are more prominent in patients associated with AIDS. Current available strategies for the treatment of cutaneous fungal infections are creams or gels which show various adverse effects on skin along with systemic absorption. These drawbacks can be overcome by using various novel drug delivery systems. So, the present investigation aims at exploring the potential of fatty acid vesicles (ufasomes) for the topical delivery of clotrimazole. Oleic acid was employed as a fatty material for the preparation of vesicles. Clotrimazole-loaded oleic acid vesicles were prepared using a thin film hydration method. Prepared vesicles were characterized for size, size distribution, shape, thermal behaviour (differential scanning calorimetry), in vitro release, in vitro antifungal activity, in vitro skin permeation and retention studies and for in vivo antifungal activity. Transmission electron microscopic (TEM) images confirmed the formation of vesicular dispersion (ufasomes) of clotrimazole. Oleic acid vesicles possessed high drug entrapment (49.5 ± 1.0%) and optimum size (455 ± 22 nm) along with good colloidal characteristics (polydispersity index = 0.210 ± 0.035 & zeta potential = - 22.45 ± 0.25 mV) at 4:6 drug-to-oleic acid ratio. In vitro drug release study showed sustained release of drug from the vesicular dispersion. Skin permeation and skin retention studies suggested accumulation of drug in the epidermal part of the skin. In vivo study confirmed prolonged release of drug from oleic acid vesicle up to five days indicating its usefulness for long-term therapy. So, it can be concluded from the present study that fatty acid vesicle may be a good approach to treat topical fungal infections.

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“…Penetration enhancer vesicles: Oleic acid induces penetration into skin due to subcutaneous lipid fluidization and phase separation. Oleic acid vesicles have been used to deliver clotrimazole with enhanced penetration as well as sustained release of upto five days after application [57].…”

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