冬凌草甲素脂质体的制备及影响因素考察  

Investigation on factors affecting entrapment efficiency of oridonin-loaded liposome

作　　者：龚素娟[1] 蒋艳博[1] 杨琳琳[1] 石凯[1] 崔福德[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2010年第2期87-92,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的制备冬凌草甲素脂质体,考察各因素对其包封率的影响。方法以包封率为指标,对冬凌草甲素脂质体的处方和工艺因素进行了单因素考察,以确定最佳制备工艺条件。结果冬凌草甲素脂质体的最佳处方为:磷脂质量浓度为20 g.L-1、磷脂与胆固醇质量比为4∶1、磷脂与药物的质量比为20∶1。最佳制备条件为:吐温80的用量为水化介质体积的2%、水化介质为pH值6.5的PBS水溶液、水化时间为30 min、水化温度为50℃。优化后的包封率为(65.25±3.63)%(n=3)。结论磷脂质量浓度、药脂比、吐温80用量对包封率的影响较大。通过处方和工艺的优化,可以制备具有较高包封率的冬凌草甲素脂质体。Objective To prepare oridonin-loaded liposome and investigate the effects of different factors on the entrapment efficiency of oridonin-loaded liposome. Methods Liposomes were prepared by thin-film dispersion method. The entrapment efficiency was determined by centrifugation of mini-column. The formulation and manufacture parameters were optimized concerning the drug entrapment efficiency through the single factor investigation. Results The optimal conditions were as follows： the concentration of lipid was 20 g.L^-1 ,the mass ratio of lipid to cholesterol was 4：1 ,the mass ratio of drug to lipid was l：20,pH value was 7.4, the temperature of the hydration was 50 ℃, the time duration of hydration was 30 min. Entrapment efficiency reached（ 65.25 ± 3.63 ） % （ n = 3 ） after optimization. Conclusions The major factors affecting the entrapment efficiency of oridonin-loaded liposome are the concentration of lecithin, weight ratio of lecithin to drug and concentration of Tween80. A oridonin-loaded liposome with a high entrapment efficiency is obtained through the optimization of formulation and preparative parameters.

关 键 词：冬凌草甲素 脂质体 微柱离心 包封率 

分 类 号：R94[医药卫生—药剂学]