Formulation and In Vitro Evaluation of Topical Ethosomal Gel Containing 5-Fluorouracil

Abstract

The aim of present study was to develop and evaluate the topical delivery of a novel vesicular carrier, ethosomes having 5-fluorouracil, an anticancer drug followed by incorporation into carbopol gel. Ethosomes of 5-Fluorouracil were prepared by cold method using phospholipids, ethanol and propylene glycol. 5-Flurouracil loaded ethosomal vesicles were characterized for vesicular shape and surface morphology, vesicular size, entrapment efficiency, zeta potential and FTIR studies. Transmission electron microscope (TEM) imaging showed a spherical with a smooth surface and almost homogenous structure for ethosomes. The prepared ethosomal formulations of 5-fluorouracil with different phospholipids have shown average particle size in the range of 202.3 ± 3.4 to 202.3 ± 7.1 nm, polydispersity index in the range of 0.37 to 0.41, zeta potential -1.35 ± 0.35 to -26.9 ± 0.98 mV and % entrapment efficiency in the range of 87.9 ± 1.7 % to 88.7 ± 2.3 %. FTIR study concluded that no major interaction occurred between drug and phospholipids used in the present study. The ethosomal formulations were incorporated into the 1% carbopol 980 gel and evaluated for in vitro drug release. In-vitro drug release through the cellophane membrane showed the release of drug from ethosomal gels was enhanced as compared to plain drug solution.