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目的:制备五肽YIGSR修饰的半边旗提取物5F脂质体(YIGSR-5F-LP)并研究其理化性质。方法:采用薄膜分散-超声法制备5F-LP,以包封率为指标,通过正交试验考察磷脂胆固醇质量比、药脂质量比、超声时间及反应温度对脂质体制备工艺的影响;采用后插入法修饰载药脂质体表面,制备表面含YIGSR的5F-LP。透射电镜法观察脂质体的形态和粒径;鱼精蛋白沉淀法测定脂质体包封率;高效液相色谱法测定脂质体中5F含量;透析法评价载药脂质体的体外释放性能。结果:优选的最优制备工艺为磷脂胆固醇质量比6∶1、药脂质量比1∶10、超声时间10 min、反应温度45℃。所制YIGSR-5F-LP呈球形或类球形,平均粒径为174.8nm,包封率为88.9%,载药量为8.2%;其体外释放比5F溶液慢,在48 h释放完全。结论:成功制得YIGSR-5F-LP,其具有缓释特性。
OBJECTIVE: To prepare 5F liposome (YIGSR-5F-LP) modified with pentapeptide YIGSR and study its physicochemical properties. Methods: 5F-LP was prepared by membrane dispersion-ultrasonic method. The entrapment efficiency was used as an index to study the effect of phospholipid cholesterol mass ratio, lipid mass ratio, ultrasonic time and reaction temperature on the liposome preparation process. After the insert method to modify the surface of drug-loaded liposomes, 5F-LP containing YIGSR on the surface was prepared. The morphology and particle size of liposomes were observed by transmission electron microscopy. The entrapment efficiency of liposomes was determined by protamine precipitation method. The content of 5F in liposomes was determined by high performance liquid chromatography. The release of drug-loaded liposomes in vitro was evaluated by dialysis performance. Results: The optimal preparation process was phospholipid cholesterol mass ratio 6: 1, lipid mass ratio 1:10, ultrasonic time 10 min and reaction temperature 45 ℃. The YIGSR-5F-LP was spherical or spheroidal with an average particle size of 174.8nm, encapsulation efficiency of 88.9% and drug loading of 8.2%. The in vitro release of YIGSR-5F-LP was slower than that of 5F solution and was completely released after 48 hours. Conclusion: YIGSR-5F-LP was successfully prepared and has sustained-release properties.