Study of Fluconazole Release from O/W Cream and Water Soluble Ointment Bases.

Aims: Study the release of fluconazole from different O/W creams and PEG ointments. Study Design: In this study, different formulations were prepared with changing one of the added excipients and study the effect of this change on the drug release and then the selected formulations were subjected to antifungal activity study. Place and Duration of Study: Faculty of Pharmacy, Department of Pharmaceutics, Assiut University, Assiut, Egypt, between December 2011 and March 2012. Methodology: O/W creams were prepared with changing either fatty alcohol type or the concentration of the added emulsifying agent. Also, the PEG ointments were prepared with changing the type of the liquid PEG (low molecular weight). Then, the viscosity and the fluconazole release from the prepared formulations were studied. Results: Changing the fatty alcohol type from stearyl to cetostearyl and cetyl alcohol in the O/W creams caused an increase in the viscosity and a decrease in the drug release. Also, changing the liquid PEG from PEG 400 to PEG 600 resulted in an increase in the formulation viscosity and subsequent decrease in the drug release. Both F1 and F6 showed a good inhibition to the fungal growth against Candida albicans and Trichophyton mentagrophyte using cup plate method, also PEG base showed a slight fungal growth inhibition. Conclusion: Results obtained showed that the PEG ointment formulations exhibited higher fluconazole release after three hours over the O/W cream formulations. Also, the nature of the PEG base may be adjunctive to the efficacy of the antifungal agent.

Formulation and In vitro Evaluation of Fluconazole Topical Gels.

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.