目的 制备雷公藤红素纳米结构脂质载体（nanostructured lipid carriers，NLC），考察其性质并进行体外透皮研究。方法 采用溶剂挥散法制备雷公藤红素NLC，并对其微观形态、粒径、Zeta电位、包封率及体外释放行为进行研究，用Franz扩散池考察其透皮吸收行为，HPLC法测定雷公藤红素的量。结果 雷公藤红素NLC平均粒径为（132.3±25）nm，Zeta电位为（?26.5±3.4）mV，包封率为（88.64±0.37）%，NLC的微观形貌呈类球形粒子。雷公藤红素NLC中药物的体外释放符合Higuchi方程（Q＝0.096 2 t^1/2－0.040 6，r＝0.995 1），其12 h药物累积透皮量虽低于雷公藤红素溶液，但皮肤滞留量是雷公藤红素溶液的11.59倍。结论 所制备的雷公藤红素NLC可以显著增加药物在皮肤中的滞留量，有望开发为雷公藤红素的新型局部给药制剂。

Objective To prepare tripterine-loaded nanostructured lipid carrier (NLC) and investigate its properties and transdermal absorption behavior. Methods The solvent evaporation method was used to prepare tripterine-loaded NLC. The morphology, particle size, Zeta potential, encapsulation efficiency (EE), and in vitro release were examined, respectively. The transdermal absorption of tripterine-loaded NLC was evaluated using Franz diffusion cells and tripterine content was determined by HPLC. Results The obtained tripterine-loaded NLC assumed spherical shape with the average particle size of (132.3 ± 25) nm, Zeta potential of (?26.5 ± 3.4) mV, and the EE of (88.64 ± 0.37)%. Drug release profile in vitro was in accordance with Higuchi equation (Q = 0.096 2 t^1/2－0.040 6, r = 0.995 1). Compared with tripterine solution, tripterine-loaded NLC had lower cumulative transdermal amount in 12 h, however, the skin retention amount was 10.59 times more. Conclusion These results indicate that the prepared tripterine-loaded NLC with imcreased skin retention amount could be developed into a novel preparation of tripterine for focal administration.

江苏省自然科学基金资助项目（SBK201022193）；江苏省中医药领军人才项目（LJ200913）