DEVELOPMENT OF THERMOSENSITIVE GEL OF FLUCONAZOLE FOR VAGINAL CANDIDIASIS
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2016, Vol 8, Issue 1
Abstract
Objective: The aim of the present study was to develop in-situ gelling formulations of Fluconazole (FCZ) using thermosensitive polymer for treatment of vaginal Candidiasis.Methods: In-situ gelling formulations of FCZ (1 % w/w) were prepared with different concentrations of Poloxamer 407 (P 407, 15-20% w/w) using the cold dispersion method. Similarly, Â formulations were also prepared by adding mucoadhesive polymers like hydroxyethyl cellulose, Polycarbophil, Carbopol 974 and Hydroxypropyl methylcellulose E 50 LV (0.4 % w/w) to the P 407 formulations. These formulations were evaluated for appearance, clarity, pH, gelling ability, gelling time, gelling temperature, viscosity (in sol and gel forms), spreading time, ex-vivo mucoadhesion, in-vitro dissolution, morphological characteristics by SEM and in-vitro antifungal efficacy against Candida albicance. In-vivo vaginal irritation of developed formulation was assessed in New Zealand female rabbits. Results: In-situ gelling formulation of FCZ, prepared using 18 % w/w P407 and 0.4 % hydroxyethyl cellulose, was optimized since this formulation was found to be clear, transparent, forming a quick and stable gel with shear thinning behaviour and excellent mucoadhesion. The developed formulation released 74.21% of FCZ after 8 h of dissolution in 5.2 pH citrate buffer. In-vitro antifungal activity against Candida albicance showed the stronger antifungal activity of formulation as compared to a marketed formulation. In-vivo vaginal irritation study in rabbits demonstrated no significant irritation after 10 d of exposure to the formulation. Conclusion: The study demonstrated that in-situ gelling formulation of FCZ prepared using thermosensitive polymer had improved activity against Candida albicance and would be efficacious for the treatment of vaginal Candidiasis.
Authors and Affiliations
Sanjeevani S. Deshkar, Arun T. Patil, Sushilkumar S. Poddar
Keywords
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