Formulation, Development and Characterization of Liposome-based Gel of Eberconazole Nitrate for Topical Delivery

Objectives: The present investigation was aimed to develop Liposome-Based Gel (LBG) for Eberconazole nitrate. The purpose was to administer the drug at a sustained rate through skin to improve bioavailability for longer period of time. Materials and Methods: Thin film hydration technique was used for the preparation of EBZ loaded liposomes. Preliminary trials were conducted for the selection of type of lipid and its ratio with cholesterol along with the lipid:drug ratio. EBZ loaded liposomes was optimized by using central composite design with amount of phospholipid, cholesterol and lipid:drug ratio as independent variables along with vesicle size and %Entrapment Efficiency (%EE) as dependent variables. Each formulation was evaluated for vesicle size, polydispersity index, % entrapment efficiency, pH and zeta potential. Further, with an aim to provide enhanced patient compliance the optimized batch of EBZ loaded liposomes was transformed into Liposomal Based Gel (LBG). Results and Conclusion: Results of all design batches showed nano size of the liposomal vesicles with good dispersion. The optimized batch of EBZ loaded liposome showed a vesicle size of 183.4 nm and 92.4% entrapment efficiency. TEM images of the optimized liposomal formulation showed well separated vesicles with narrow size distribution. The results of ex vivo skin permeation study of the optimized batch of EBZ loaded LBG revealed a remarkable improvement in the dissolution as compared to its conventional formulation. All these concluded LBG as one of the suitable approaches for developing topical formulation of poorly water-soluble drugs like eberconazole nitrate.