pH梯度结合逆向蒸发法制备槐定碱纳米脂质体及体外释放度研究  

Preparation and in vitro drug-release behavior of sophoridine nano-liposomes using pH-gradients method coupled with reverse evaporation technique

作　　者：胡鹏翼[1] 郑琴[1] 刘彦君[1] 伍振峰[1] 岳鹏飞[1] 杨明[1] 

机构地区：[1]江西中医学院现代中药制剂教育部重点实验室,南昌330004

出　　处：《中国新药杂志》2011年第14期1275-1279,共5页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2009ZX09310-005);江西省自然科学基金(2008GQY0017);江西中医学院创新人才课题(JZ0909)

摘　　要：目的:采用pH梯度结合逆向蒸发法制备槐定碱纳米脂质体,对影响包封率和粒径的因素进行考察,并对其体外释放进行评价。方法:以正交设计及单因素实验考察影响脂质体包封率及粒径的主要因素,同时对优化后的脂质体进行了质量评价及体外释放度研究。结果:磷脂的浓度为5 mg.mL-1,药脂比为1∶15,胆脂比为1∶4,内水相的pH值为2.0,均质压力为100 bar时,制备的脂质体包封率可达(90.30±0.63)%,脂质体外观圆整均匀,平均粒径为(117±6)nm。结论:pH梯度结合逆向蒸发法制备的槐定碱纳米脂质体包封率高,粒径均匀,稳定性好,具有一定的缓释作用。Objective： To prepare the nano-liposomes loaded with sophoridine by pH-gradients method coupled with reverse evaporation techniquem,and to evaluate its in vitro release behavior.Methods： The influence of various factors on the entrapment efficiencies and the particle size were identified by single and orthogonal design.Then the quality was evaluated and the in vitro release behavior of the optimized liposomes was investigated.Results： Optimal conditions were that the concentrations of lipoid was 5 mg·mL-1,the ratio of drug and lipid was 1∶15,the ratio of cholesterol and lipid was 1∶4,pH value was 2.0 in the internal phase,and homogenization pressure was 100 bar.In such conditions,the entrapment efficiencies of sophoridine nano-liposome reached up to（90.30±0.63）%,the average particle size was（117±6） nm,and its appearance was round and uniform.Conclusion： Sophoridine nano-liposomes are prepared by pH-gradient method coupled with reverse evaporation technique;they are homogenous and have good stability,high encapsulation efficiency and sustained release behavior.

关 键 词：槐定碱 纳米脂质体 主动载药法 体外释药 

分 类 号：R943.41[医药卫生—药剂学] R979.1[医药卫生—药学]