褪黑素脂质体的制备及理化性质研究  

Preparation of melatonin liposomes and their physico-chemical properties

作　　者：孙庆雪[1] 黄桂华[1] 邵伟[1] 

机构地区：[1]山东大学药学院药剂学教研室,济南250012

出　　处：《山东大学学报（医学版）》2010年第1期159-163,共5页Journal of Shandong University:Health Sciences

摘　　要：目的制备褪黑素脂质体并考察其理化性质。方法采用薄膜分散法制备褪黑素脂质体,在单因素考察基础上,采用均匀试验设计优化最佳处方和工艺;透射电镜下观察外观形态,激光散射测定Zeta电势和粒度分布,低温高速离心法分离脂质体与未包封的药物,UV法测定包封率与载药量,膜动态透析法探讨其体外释药特性。结果均匀试验设计优化的最佳处方为药脂比1∶25,磷脂和胆固醇比10∶1,温度40℃,最佳处方制备的脂质体为封闭的多层囊状或多层圆球体,大小均匀,平均粒径为(5.542±0.04)μm,Zeta电势为-31.68mV,包封率为(77.23±2.51)%,载药量为(3.60±0.29)%。体外释放可延长至72h,释放特性符合双相动力学方程(rα=0.9886和rβ=0.9874)。结论采用薄膜分散法制备的褪黑素脂质体,包封率较高,体外释药有明显的缓释效果。Objective To study the preparation of melatonin （MLT） liposomes and their physico-chemical property. Methods Liposomes were prepared by a film dispersion method. Based on a single test,the optimum formulations and the preparation technology were optimized by a uniform experiment. Morphology of the liposomes was detected by transmission electron microscopy. The Zeta potential and particle size distribution were evaluated by laser scattering. High speed centrifugation was applied to separate the free drug and liposomes. The entrapment efficiency and drug loading were determined by UV. The release character of melatonin liposomes was studied by the dialysis method. Results The optimal formula was obtained by a uniform design：the phosphatides to cholesterol ratio was 25∶1,and the drug to lipid ratio was 1∶10,40 ℃. The liposomes were a multi-layer spherical or ellipsoidal shape with a uniform size. The mean diameter of melatonin liposomes was（5.542±0.04）μm. The Zeta potential was -31.68 mV. The drug loading and entrapment efficiency of melatonin liposomes were （77.23±2.51）% and （3.60±0.29）%,respectively. In vitro release could be sustained for 72 h and conformed to bio-exponential kinetics （rα=0.988 6 and rβ=0.987 4）. Conclusion Melatonin liposomes made by using the film dispersion method have a high encapsulation efficiency and have a good delayed-release property in vitro.

关 键 词：褪黑素 脂质体 薄膜分散法 体外释放 

分 类 号：R944.15[医药卫生—药剂学]