Development and characterization of topical ethosomal gel for improved antifungal therapeutics

Abstract

The present study aimed to develop Eberconazole nitrate (EBZ)-loaded ethosomes using Central Composite Design (CCD) by the cold method. The three-factor CCD model was implemented to investigate the effect of variables on ethosome characteristics and performance. For CCD modelling, dependent and independent variables were chosen. The percentage of soy phosphatidylcholine (PC) (X1; % w/v), ethanol (X2; % v/v), and Propylene glycol (PG) (X3; % v/v) were designated as independent variables. However, the dependent variables were particle size (Y1; nm), polydispersity index (PDI) (Y2), and encapsulation efficiency (EE) (Y3; %). The level of independent variables was changed to produce a total of 17 batches (F1-F17). Formulation code F2 with particle size; 227.9 nm, PDI; 0.160 and % EE; 90 ± 0.34 % was selected as the optimized batch. The optimized batch was further incorporated into the hydrogel matrix and investigated for several physicochemical parameters. When compared to the free drug-loaded hydrogel, the ethosomes-loaded hydrogel demonstrated controlled EBZ release with higher skin permeation and skin retention of EBZ. The assessment of antifungal efficacy of the developed formulation was carried out by in vivo animal model method. In vivo studies demonstrated that EBZ-loaded ethosomal gel may alleviate fungal infection caused by a resistant strain of Candida albicans. The study showed satisfactory results, which suggest the suitability of the developed formulation for the effective treatment of fungal infection.