雷公藤红素纳米结构脂质载体的制备及其体外透皮研究  

Preparation of tripterine-loaded nanostructured lipid carrier and its in vitro transdermal absorption

作　　者：袁菱[1] 周蕾[1] 陈彦[1,2] 张振海[2] 吴青青[1] 曹伟[1] 

机构地区：[1]江苏大学药学院,江苏镇江212013 [2]国家中医药管理局中药释药系统重点研究室,江苏省中医药研究院中药新型给药系统重点实验室,江苏南京210028

出　　处：《中草药》2012年第8期1514-1518,共5页Chinese Traditional and Herbal Drugs

基　　金：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)

摘　　要：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 t1/2-0.040 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 uanostructured 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） rim, Zeta potential of（-26.5 4±3.4） mV, and the EE of（88.64 4± 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.

关 键 词：雷公藤红素 纳米结构脂质载体 体外透皮吸收 溶剂挥散法 局部给药 

分 类 号：R284.2[医药卫生—中药学]