DESIGN AND OPTIMIZATION OF FLUCONAZOLE-LOADED PHARMACOSOME GEL FOR ENHANCING TRANSDERMAL PERMEATION AND TREATING FUNGAL INFECTIONS THROUGH BOX-BEHNKEN DESIGN

Abstract

Objective: The objective of the selected study was to develop and statistically optimize fluconazole (drug) loaded pharmacosomes (carrier) to enhance transdermal permeation by incorporating into gel base and to treat fungal infections by selecting the Box-Behnken model. Methods: Fluconazole is an antifungal drug which belongs to BCS class-II with high permeability and choice for topical drug delivery. In the study, the levels of the lecithin (lipid), dichloromethane and DMSO are selected as independent variables were varied to study the influence on particle size, % entrapment efficiency and in vitro drug release as dependent variables. Factorial designs through software Design expert version 13 (Box-Behnken design) is applied for this study and the optimization process was carried out using the desirability plots and point prediction techniques. Results: Results of the study with the application of a design expert shows that the optimized drug-loaded pharmacosomes with vesicle size of 158.87±0.56 nm as predicted and zeta potential of-30.6mV indicating good stability of the formulation, entrapment efficiency of 90.6±1.12% and in vitro drug release of 97.59±1.84% respectively. The optimized formulation loaded into gel base and compared with the marketed gel formulation. All the evaluation parameters confirmed that the physical mixture of drug and excipients was compatible without any interactions. Conclusion: Through obtained results, it’s concluded that; the independent variable plays a crucial role in optimizing formulation. Study data provided strong evidence that the optimized vesicular formulation through Box-Behnken factorial design can be potentially useful as a drug carrier for loading drug of selected category for enhancing transdermal delivery.