冰片修饰的丹参酮ⅡA阳离子脂质体的制备及其特性  

Preparation and characterization of tanshinone ⅡA-loaded modifying borneol cationic liposomes

作　　者：叶晓莉[1] 王丛瑶[2] 张玲娣[3] 张超 王水霞 鲁明[1] 李晴宇[1] YE Xiaoli;WANG Congyao;ZHANG Lingdi;ZHANG Chao;WANG Shuixia;LU Ming;LI Qingyu(Department of Pharmacy,Hangzhou First People＇ s Hospital,Hangzhou 310006,China;Department of Pharma-cy,The First People＇ s Hospital of Xiaoshan District,Hangzhou 311200,China;Department of Pharmacy,Zhe-jiang Xiaoshan Hospital,Hangzhou 311201,China;Department of Pharmacy,Hangzhou Linan District People＇ s Hospital,Hangzhou 311300,China;Department of Pharmacy,Zhengiiang Xinchang Hospital of Traditional Chi-nese Medical,Shaoxing 312000,China)

机构地区：[1]杭州市第一人民医院药学部,杭州310006 [2]杭州市萧山区第一人民医院药剂科,杭州311200 [3]浙江萧山医院药剂科,杭州311201 [4]杭州市临安区人民医院药剂科,杭州311300 [5]浙江省新昌县中医院药剂科,绍兴312000

出　　处：《中国临床药学杂志》2018年第4期238-244,共7页Chinese Journal of Clinical Pharmacy

基　　金：浙江省中医药科技计划项目(编号2015ZB079);浙江省中医药科技计划项目(编号2014ZB075);浙江省药学会医院药学科研专项基金项目(编号2012ZYY15)

摘　　要：目的制备冰片(BO)修饰的丹参酮ⅡA(TA)阳离子脂质体(TA-BCLPs),并考察其理化性质、体外释药特性。方法采用乙醇注入法制备阳离子脂质体,通过正交设计,以粒径、包封率和载药量为评价指标优化处方工艺。结果制备TABCLPs的优化条件:药脂比为1∶10,胆固醇与磷脂的比为1∶3,磷脂质量浓度为30 g·L-1,高压均质时间90 s。按优化条件所制备的TA-BCLPs粒径为(152. 29±9. 59) nm,Zeta电位为(16. 50±0. 93) mV,包封率为(88. 49±1. 09)%,载药量为(4. 12±0. 13)%,药物释放曲线符合Weibull方程模型,BCLPs对人脑微毛细血管内皮细胞无明显的毒性作用。结论采用乙醇注入法成功制备了TA-BCLPs,为TA新剂型的研究开发提供了实验基础。AIM To prepare tanshinoneⅡ A （TA）-loaded modifying borneol cationic liposomes （TA- BCLPs） , to characterize their physicochemical properties, and to study the in vitro release behavior. METHODS The TA-BCLPs were prepared with ethanol injection method and were optimized through orthogonal test according to particle size, entrapment efficiency and drug loading of TA-BCLPs. RESULTS The optimal conditions for prepa- ration of TA-BCLPs were TA/HSPC （m/m） 1 ： 10, CH/HSPC （m/m） 1 ： 3, HSPC （m/V） 30 g · L- 1 and ultrasonic averaging time was 90 s. The mean particle size of the resulted TA-BCLPs was （ 152.29 ± 9.59） nm and Zeta po- tential was （ 16.50 ±0.93 ） mV, the average entrapment efficiency and drug-loading was （88.49 ± 1.09 ） % and （4.12 ±0.13 ）% , respectively. The profiles of release in vitro was fitted well by Weibull equation. BCLPs had no significant toxic effect on human brain microvascular endothelial cells. CONCLUSION The ethanol injection meth- od can be used to prepare TA-BCLPs, which can lay the foundation for the research on novel TA preparations.

关 键 词：冰片 丹参酮ⅡA 阳离子脂质体 正交设计 

分 类 号：TQ460.6[化学工程—制药化工]