Microemulgel of Voriconazole: an Unfathomable Protection to Counter Fungal Contagiousness.

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.

Microemulgel: an overwhelming approach to improve therapeutic action of drug moiety.

As compared to gel and other topical preparations microemulgel has been prepared by screening of oils, emulsifier, and co-emulsifier on bases of solubility of an API in it. An API has high solubility and oil may also have more or less pharmacological property, so it may assist the therapeutic action of API. Due to presence of oil portion, it leads to more penetration of API in the skin. Oil Micelle Size was less than 500 nm which provides more area for absorption of API in the skin so more penetration and more effective than macro-emulsion. Microemulgel has an advantage of emulgel that has dual benefits of micro-emulsion and gel and several other desirable properties like good consistency, thyrotrophic, greaseless, easily spreadable as well as removable, emollient, non-staining, water soluble, longer shelf-life, bio-friendly, transparent, pleasant appearance, ability of patients for self-medication, termination of medications will be easy, etc.