Microemulgel of Voriconazole: an Unfathomable Protection to Counter Fungal Contagiousness

Abstract

Background: Fluconazole and ketoconazole both have poor minimum inhibitory concentration than voriconazole. Voriconazole had serious side effects in oral and intravenous doses. It has poor water solubility. The objective of the study was to prepare and optimize microemulgel of voriconazole for topical delivery. Aim: Formulation, development, and evaluation of voriconazole microemulgel for topical delivery. Methods: Oil and emulsifi ers selected were on the basis of equilibrium solubility study and emulsification property respectively. The pseudo-ternary plot and constrained simplex lattice design were applied for preparation of microemulsions. Microemulsions were subjected to micelle size, zeta potential, polydispersity index, and in vitro study. They were optimized by Design-Expert® 9.0.3.1 software. Formulation, development, evaluation and optimization of microemulgel were carried out. Microbial assay of an optimized batch of microemulgel was performed. Results: Solubility of voriconazole in Parker Neem® oil was 7.51±0.14 mg/g. Acrysol™K-150: PEG-400 in 4:1 ratio had the highest area for microemulsion. 59.2% Acrysol™K-150, 14.8% PEG-400, 11% Parker Neem® oil, 15% rose water, and 1% voriconazole as an optimized batch of microemulsion was selected for preparation of microemulgel. Carbomer 934P found a good gelling agent in 0-2% w/w concentration. An optimized batch of microemulgel had 0.974 desirability value. An optimized batch of microemulgel and Nizral® cream had 37.32±0.63% and 26.45±0.63% zones of inhibition. Conclusion: Topical antifungal treatment was successfully achieved with voriconazole microemulgel.

Keywords

• constrained simplex lattice design
• microemulgel
• microemulssharaion based gel
• Neem oil
• voriconazole