Preparation of luliconazole nanocrystals loaded hydrogel for improvement of dissolution and antifungal activity

制备负载卢立康唑纳米晶体的水凝胶以提高其溶解性和抗真菌活性

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Abstract

Superficial fungal infection in immunocompromised patients can lead to many disorders and complications. Currently, new topical treatment options are critically needed to treat these fungal infections. Luliconazole (LZL) is a topical antifungal medicine used for fungal infection treatment. The purpose of this paper was to develop a new topical luliconazole nanocrystal (LNC) incorporated hydrogel. This study suggested the potential benefits of LNC embedded in a gel as a drug delivery system for topical antifungal treatments. Preliminary experiments were therefore carried out to characterize the LNC in comparison with raw drug. Prepared gel was homogeneous for human use with about 88 percent trapping, non-irritant and safe. Nano-systems showed an overall 5 fold enhancement in solubility, 4 fold increase in dissolution velocity, higher skin retention and better antifungal activity. Drugs retained from LNC hydrogel (N-GEL) in different skin layers within 8 h were the highest, i.e. 62.17% compared to coarse suspension (41.87%), nanosuspension (49.77%), D-GEL (55.76%). In addition, LNC and N-GEL had higher ZOI (41.20 ± 0.61mm and 44.25 ± 0.57mm respectively) than LZL and D-GEL (35.98 ± 0.81mm and 36.83 ± 0.83mm respectively). Therefore, it was observed that LNC loaded hydrogel was more effective in killing the fungus. Consequently, hydrogel incorporated with LNC could be a new approach with improved activity and increased dermal delivery for drugs with poor aqueous solubility rather than coarse drug containing gel.

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