Formulation and In vitro Evaluation of Fluconazole Topical Gels

Abstract

Aims: Topical drug delivery of fluconazole, an antifungal drug, in gel form was formulated to avoid the side effect of the oral route. Study Design: In this study I prepare different formulation from different polymers and select the best formulation to undergo further antifungal and stability studies. Place and Duration of Study: Faculty of Pharmacy, Department of Pharmaceutics, Assiut University, between May 2010 and July 2011. Methodology: Different polymers; Sodium carboxymethyl cellulose, Sodium alginate, Carbopol 934P, Hydroxypropylmethyl cellulose, Pluronic F-127 and hydroxypropyl cellulose, were used. The compatibility of fluconazole and different gelling polymer was assessed through differential scanning calorimetry and infrared absorption spectroscopy. The influence of polymer type and concentration on fluconazole release from the prepared gels were studied. The prepared gel formulations were evaluated for pH, drug content, rheology, spreadability and in vitro drug release Results: The rheological behavior of all the prepared gels showed a pseudoplastic flow (shear thinning) which is a good characteristic in the pharmaceutical gels. With the increase of the polymer concentration in the formulation, viscosity increased and in vitro release of fluconazole decreased. Among all the prepared formulations, 0.5% Carbopol 934P gel showed desired properties and exhibited the best fluconazole in vitro release that reaches 77% over a 3-hr period. This gel showed a good inhibition to the fungal growth against Candida albicans and Trichophyton mentagrophyte using cup plate method and also, showed good stability. Conclusion: 0.5% Carbopol 934P / Fluconazole gel is a promising dosage form for the treatment of superficial fungal infections and could be used for further clinical studies.