甲巯咪唑脂质体凝胶的制备和体外透皮性能考察

Preparation and in vitro transdermal performance of liposome thiamazole gel

目的制备甲巯咪唑(thiamazole)脂质体凝胶,考察不同渗透剂对脂质体凝胶促渗作用的影响,与复方甲巯咪唑软膏进行体外透皮性能比较和评价。方法采用逆向蒸发一超声法制备甲巯咪唑脂质体,分别加入2%桉叶油、2%薄荷、2%月桂醇氮酮为促渗剂,离体大鼠腹皮结合改良Franz扩散装置考察不同促渗剂体外透皮特性。结果甲巯咪唑脂质体凝胶呈乳白色黏稠状,性质较为稳定。体外释放实验结果显示,选用2%月桂醇氮酮制得的脂质体凝胶促渗效果最好。复方甲巯咪唑软膏与甲巯咪唑脂质体凝胶分别在8、15h左右药物释放达到平衡,其累积释放率分别为70.99%、80.10%,两者释药均符合Higuchi方程。结论采用优化后的甲巯咪唑脂质体的处方及工艺所制甲巯咪唑脂质体凝胶质量较好,可有效延缓药物的释放。

Objective To prepare liposome gel of thiamazole and investigate the effect of different osmotic agents on the permeation of liposome gel, comparing and evaluating transdermal performance of compound thiamazole ointment in vitro. Methods Thiamazole liposomes were prepared by reverse evaporation-ultrasonic method.Two percent eucalyptus oil,two percent menthol and two percent lauryl azone were added as osmotic enhancers respectively,and the extracorporeal transdermal characteristics of different osmotic enhancers were investigated in the rat abdominal skin in vitro combined with the modified Franz diffusion device. Results The methimazole liposome gel was milky white and sticky stable.The results of in vitro release test showed that the liposome gel prepared with 2% lauryl azone had the best osmotic effect.Compound thiamazole ointment and thiamazole liposome gel reached equilibrium at about 8 and 15 h,respectively,and their cumulative release rates were 70.99% and 80.10%,respectively,and both of them were in accordance with the Higuchi equation,were in line with Higuchi equation. Conclusion The gel quality of the methimazole liposomes prepared by the optimized formulation and technology has better quality, could effectively delay the release of the drug.