目的 研究雷公藤甲素阿魏酸醇质体最佳制备工艺，并考察其制剂性能和体外透皮特性。方法 MTT法确定雷公藤甲素与阿魏酸的配伍比例。采用注入法制备雷公藤甲素阿魏酸醇质体，在单因素实验结果的基础上，采用Box-Behnken设计优化处方，并对其粒径、包封率、电位、分析方法学及体外释放行为进行研究。采用改良的Franz扩散池进行醇质体的体外透皮实验。结果 雷公藤甲素与阿魏酸的配伍比例为1∶100。醇质体优化处方为乙醇体积分数为20%，磷脂质量分数为2.2%，超声时间为90 s，制备出的醇质体外观为澄清液体，微有蓝色乳光，平均粒径为（46.75±2.39）nm，Zeta电位为（-46.32±3.76）mV，包封率为（67.72±1.10）%。醇质体中阿魏酸、雷公藤甲素的体外透皮行为均符合Higuchi方程。结论 醇质体粒径小、分布均匀、稳定性良好，有良好透皮吸收特性，可为雷公藤有效成分的局部透皮制剂开发提供一定依据。

Objective In order to optimize the preparation technology of triptolide and ferulic acid ethosomes and evaluate its characteristics of the in vitro transdermal penetration and the preparations performance using ethosome as carrier. Methods The compatibility ratio between triptolide and ferulic acid was determined by MTT. The triptolide and ferulic acid ethosomes were prepared with injection method based on the results of single factor experiments, Box-Behnken design was used to optimize the particle size, electric potential, and encapsulation efficiency (EE) of the ethosomes, and the in vitro release behavior prepared by the optimal formulation were studied. The in vitro transdermal absorption experiment was carried out in optimized Franz diffusion cells. Results The ratio of triptolide to ferulic acid was 1:100. The optimized prescription of the ethosomes was 20% ethanol, 2.2% phospholipid, 90 s ultrasonic time. The results showed that the appearance of the triptolide and ferulic acid ethosomes was clear liquid with blue opalescence in an average diameter of (46.75 ±2.39) nm at potential of (-46.32 ±3.76) mV, and the EE was (67.72 ±1.10)%. The in vitro transdermal behaviors of ferulic acid and triptolide in the ethosomes were in line with the Higuchi equation. Conclusion The ethosomes has the advantages of small particle size, uniform distribution, good stability, and good transdermal absorption property, so as to provide the basis for the development of the transdermal preparation of the effective components of Tripterygium wilfordii.

国家自然科学基金2014年度地区基金资助项目（81460607）