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天麻素纳米脂质体的研制及其脑靶向性的初步研究
引用本文:黄静,何文,李秀芳,刘丹丹.天麻素纳米脂质体的研制及其脑靶向性的初步研究[J].广东药学院学报,2011,27(4):345-350.
作者姓名:黄静  何文  李秀芳  刘丹丹
作者单位:1. 武汉大学人民医院药学部,湖北武汉430060;武汉大学药学院,湖北武汉430072
2. 武汉大学人民医院药学部,湖北武汉,430060
3. 武汉大学药学院,湖北武汉,430072
摘    要:目的 研制天麻素纳米脂质体,并初步考察其在小鼠体内的脑靶向性.方法 采用逆向蒸发法制备天麻素脂质体,高压均质机均质成纳米级;以包封率为指标,正交试验筛选出最佳处方;并对脂质体的形态、粒径、Zeta电位、体外释放等特性进行考察.小鼠尾静脉给药后,于不同时间点离取脑组织及血浆,处理后HPLC检测,并与同剂量的天麻素水溶液对...

关 键 词:天麻素  纳米脂质体  脑靶向性

Study on the preparation and brain targeting property of gastrodin nanoliposomes
HUANG Jing,HE Wen,LI Xiu-fang,LIU Dan-dan.Study on the preparation and brain targeting property of gastrodin nanoliposomes[J].Academic Journal of Guangdong College of Pharmacy,2011,27(4):345-350.
Authors:HUANG Jing  HE Wen  LI Xiu-fang  LIU Dan-dan
Institution:1.Department of Pharmacy,Renmin Hospital of Wuhan University,Wuhan 430060,China;2.College of Pharmacy,Wuhan University,Wuhan 430072,China)
Abstract:Objective To prepare gastrodin nanoliposomes and evaluate its brain targeting property in mice.Methods Gastrodin liposomes were prepared by reverse evaporation method,and then homogenized into nanoliposomes by high pressure homogenizer.Orthogonal test was applied to optimize the formulation with encapsulation efficiency as index.The morphology,particle size,Zeta potential and release in vitro were investigated.After tail vein injection,brain and plasma were withdrawn at different time intervals,then the drug was determined by HPLC.Brain targeting property of the preparation was preliminarily evaluated with targeting index as the indicator.Results The best formulation were as follows:lecithin ∶cholesterol of 2 ∶1(ζ),gastrodin ∶lipid of 1 ∶30(ζ),lipid concentration of 16.7 mg·mL-1.The nanoliposomes under the electron microscope showed uniform spherical shape with the average diameter of(97.52±0.79) nm,zeta potential of(-1.36±0.57) mV and encapsulation efficiency of(29.8±0.14)%(n=3).The release in vitro fitted the first-order equation:ln(1-mt/m0)=-0.2944t+0.045.Compared with the gastrodin solution,targeting index was greater than 1.Conclusion The preparation of gastrodin nanoliposomes was feasible,and the quality was promising.Compared with the solution,the brain targeting of gastrodin nanoliposomes was significantly increased.
Keywords:gastrodin  nanoliposomes  brain targeting
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