异补骨脂素纳米结构脂质载体的制备及其体外透皮研究  

Preparation of isopsoralen loaded nanostructured carrier and its in vitro transdermal permeation characteristics

作　　者：庞建云[1,2] 刘肖[1,2] 申宝德[2,3] 沈成英[2] 连王权 刘娟[1,2] 胡春晓[1,2] 钟芮娜 许润春[1] 袁海龙[2] 

机构地区：[1]成都中医药大学药学院,四川成都611137 [2]中国人民解放军空军总医院药学部,北京100142 [3]江西中医药大学现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《中国中药杂志》2017年第13期2473-2478,共6页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81573697);全军重大科研计划项目[军后综(2016)450]

摘　　要：为增加异补骨脂素的皮肤透过量及滞留量,提高其生物利用度。该文采用高压均质法制备异补骨脂素纳米结构脂质载体(IPRN-NLC),以包封率、载药量及平均粒径为评价指标,运用正交实验优化最佳处方。采用Franze扩散池法考察IPRN-NLC的体外透皮。结果表明,最优处方固液脂质比为7∶3,药脂比1∶30,表面活性剂1%,制备的IPRN-NLC平均包封率为(90.25±0.73)%,平均载药量为(1.56±0.27)%,平均粒径为(305±1.57)nm;体外透皮实验显示IPRN-NLC提高了IPRN的皮肤透过量,且皮肤滞留量是IPRN(水)溶液的3倍。采用高压均质法制备的IPRN-NLC提高了IPRN的皮肤透过量及滞留量,在经皮给药领域具有广阔的应用前景。To increase the permeation and retention of isopsoralen in skin, and improve its bioavailability. Isopsoralen loaded nano- structure liquid carrier （IPRN-NLC） was prepared by high pressure homogenization andoptimized by orthogonal experiment with the en- capsulation efficiency, drug loading and average particle size as the evaluation indexes. The in vitro transdermal permeation of IPRN- NLC was evaluated by Franze diffusion cells. The results showed that solid-liquid lipid ratio of optimum IPRN-NLC formulation was 7： 3, drug-lipid ratio of 1 ： 30, 1% surfactant. Under these conditions, IPRN-NLC had an average encapsulation of （90. 25 ± 0. 73 ） %, drug loading of （ 1.56 ±0. 27 ） % and an average particle size of （ 305 ±1.57 ） nm. The in vitro transdermal permeation results showed that IPRN-NLC could increase the amount of IPRN permeated though skin, with 3 times of the epidermal retention as compared withIPRN solution. From the results we can know that the IPRN-NLC prepared by high pressure homogenization can improve the permeation andaccumulation of IPRN in the skin, with wide application prospects in the field of transdermnal administration.

关 键 词：异补骨脂素 纳米结构脂质载体 体外透皮 皮肤滞留量 

分 类 号：R283.6[医药卫生—中药学]