Abstract
Fluconazole is a triazole antifungal, widely prescribed for the treatment of vaginal Candidiasis. Topical application of FZ localizes the drug in tissue and reduces the side effects as compared to systemic administration. In contrast to the lower retention of conventional formulations in vagina, mucoadhesive formulations would prolong the retention time resulting in effective topical therapy. The aim of the present study was to develop a mucoadhesive vaginal gel of Fluconazole for treatment of Candidiasis. Various mucoadhesive polymers including, Carbopol 974, Carbopol 980, Polycarbophil, Hydroxy propyl methyl cellulose K 100 M, Hydroxyl propyl cellulose, Hydroxy ethyl cellulose (Natrosol 250) and Xanthan gum were evaluated for their potential as gel matrices in vaginal drug delivery. The gel formulations were prepared at different concentrations of polymers and evaluated for appearance, pH, spreadability, extrudability, viscosity, effect of dilution on viscosity, ex vivo mucoadhesion and in vitro drug release. The optimized formulations were evaluated for in vitro antifungal activity, in vivo vaginal irritation and stability. The gel formulations prepared using polycarbophil (2 %w/w) and hydroxyl ethyl cellulose (6 % w/w) were optimized since these formulations were found to be clear, easily spreadable and extrudable, viscous with shear thinning property, resistant to dilution by acidic pH of vagina, and revealed excellent mucoadhesive behaviour. The developed formulations exhibited sustained drug release pattern with diffusion as the mechanism of drug release. The formulations indicated in vitro antifungal activity against Candida albicance and did not show any sign of vaginal irritation, when tested in mice vagina. Thus, the study demonstrated the potential of developed mucoadhesive gel of Fluconazole in treatment of vaginal Candidiasis.
