Luliconazole bilosomal gel for treating fungal infection: development, optimization and antifungal activity

用于治疗真菌感染的卢立康唑双分子凝胶:开发、优化和抗真菌活性

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Abstract

AIMS: Luliconazole is a class of imidazole that exhibits high antifungal activity. Luliconazole has drawbacks, such as low aqueous solubility and poor skin penetration. METHODS: To overcome these limitations, luliconazole-loaded bilosomes (LZBSs) were developed via ethanol injection, using soy lecithin, cholesterol, Span 60, and bile salt. A 2(3) factorial design was employed to optimize the formulation. RESULTS: The optimized batch of LZBS resulted in a vesicle size of 177.3 ± 0.00 nm with an entrapment efficacy of 90.0 ± 2.5 % and zeta potential of -54.8 ± 3.15 mV. TEM analysis confirmed the spherical shape of bilosome vesicles and ATR-FTIR results supported the formation of bilosomes without any interaction. LZBS was loaded into Carbopol gel (LZBS gel) and evaluated for in vitro and ex vivo drug release study; results showed extended release of 90.53 ± 7.89 % and 84.97 ± 5.58 %, respectively, up to 24 h. Antifungal study for LZBS gel demonstrated superior activity against Candida albicans as compared to marketed and pure drug. CONCLUSION: Thus, luliconazole-loaded bilosome gel proved to be effective against fungal infections.

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