Design, synthesis of novel vesicular systems using turpentine as a skin permeation enhancer

Abstract

Addition of skin penetration enhancer in a formulation is the simplest and most common technique to improve transdermal permeation. We aimed to develop novel liposome and ethosome vesicular systems using turpentine as a skin penetration enhancer for improving fluconazole skin permeability.Fluconazole was encapsulated in various liposomal and ethosomal formulations. The prepared formulations were characterized for size, size distribution, zeta potential (Z), entrapment efficiency (EE %), drug content, in-vitro, ex-vivo skin permeation and stability studies. The vesicles were found spherical in structure as confirmed by Scanning Electron Microscopy (SEM). Fluconazole was successfully entrapped in liposomes and ethosomes with relatively uniform drug content and entrapment efficiency in the range of 90.84–91.0%. Liposome formulation; F3 and ethosome formulation; F7 with the highest drug entrapment efficiency were obtained as optimized formulations. Cumulative percent drug release for liposome (F3) and ethosome (F7) formulations were 82.52 and 90.84%, respectively. In-vitro, ex-vivo and antifungal effect of drug loaded ethosomes and liposomes, and the effect of penetration enhancer (turpentene) were studied and compared with free drug. The formulations containing turpentene showed higher permeation characteristics and can be proposed as promising delivery systems for fluconazole topical delivery.