乳糖化-去甲斑蝥素磷脂复合物及其pH敏感型脂质体的制备  

Preparation of lactosyl-norcantharitin phospholipid complex and its pH-sensitive liposomes

作　　者：周奕[1] 许静玉[1] 管敏[1] 张学农[1] 

机构地区：[1]苏州大学药学院药剂学教研室,苏州215123

出　　处：《中国新药杂志》2011年第17期1631-1638,共8页Chinese Journal of New Drugs

基　　金：国家“重大新药创制”科技重大专项(2009ZX09310-001);国家科技重大技术研究项目(973)(2009CB930300);国家科技支撑计划(2006BAI09B00);江苏省卫生厅项目(H200630);江苏省“六大人才高峰”资助项目

摘　　要：目的:合成乳糖化-去甲斑蝥素磷脂复合物,并制备其pH敏感型脂质体。方法:将乳糖化-去甲斑蝥素与磷脂聚合成药物磷脂复合物,并采用FT-IR、DSC和1H-NMR对其进行表征。逆向蒸发法制备药物磷脂复合物脂质体;利用羧甲基壳聚糖与脂质体表面的静电吸附作用,使羧甲基壳聚糖吸附在脂质体表面,制备乳糖化-去甲斑蝥素磷脂复合物pH敏感型脂质体;考察了药物与磷脂的复合率,磷脂复合物脂质体的包封率,粒径大小和分布,以及体外释药特性。结果:药物磷脂复合率为(97.2±2.01)%,磷脂复合物脂质体的平均包封率为(70.00±1.30)%,平均粒径为(47.18±4.16)nm,粒径跨距为(0.70±0.07),电镜显示其形态圆整,体外释药符合Weibull方程。结论:乳糖化-去甲斑蝥素磷脂复合率高,制成的pH敏感型脂质体性质稳定,且具有缓释特性。Objective： To prepare lactosyl-norcantharitin （Lac-NCTD） phospholipid complex and its pH- sensitive liposomes. Methods： Lac-NCTD phosphohpid complex was prepared using solvent-evaporation, and its correlated physicochemical properties were confirmed with solubility test, FT-IR, DSC and 1H-NMR. The phospholipid complex liposomes were prepared by the reverse phase evaporation method, and then pH-sensitive liposomes of Lac-NCTD phospholipid complex were obtained with the carboxymethyl chitosan （CMCT） absorbed on the surface of the liposomes. The drug loading rate, encapsulation efficiency, particle distribution and in vitro release of Lac- NCTD from liposomes were investigated, respectively. Results： The drug loading rate of phospholipid complex was （97.2 ±2.01 ） % , the average entrapment rate of liposome was （70.00 ± 1.30） %. The mean particle size was （47.18 ± 4.16） nm, particle span was （0.70 ± 0.07）, and in vitro release was followed Weibull equation. Conclusion： Alternative pH-sensitive liposomes of Lac-NCTD phospholipid complex with high drug loading rate and sustained release have been obtained.

关 键 词：乳糖化-去甲斑蝥素 磷脂复合物 pH敏感型脂质体 体外释放 

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