五肽YIGSR修饰的半边旗提取物5F脂质体的制备及理化性质研究  

Preparation of Pteris semipinnata Extract 5F-liposome Modified by Pentapeptide YIGSR and Physicochemical Property Study

作　　者：黄青燕[1,2] 吕应年[1] 邓小云[2] 刘明星[2] 纪周新 刘琳琳[1] 吴科锋[1] 梁念慈[1] 

机构地区：[1]广东医学院广东天然药物研究与开发重点实验室,广东湛江524023 [2]广东医学院药学院,广东东莞523808

出　　处：《中国药房》2016年第13期1842-1844,共3页China Pharmacy

基　　金：广东省自然科学基金项目(No.S2012010008163);广东高校优秀青年创新人才培养计划(No.LYM10083)

摘　　要：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 Pteris semipinnata extract 5F-liposome modified by pentapeptide YIGSR（YIGSR-5F-LP）and study its physicochemical property. METHODS：5F-LP were prepared by film-dispersion and ultrasonic method. Using encapsulation efficiency as index,orthogonal test was adopted to investigate the effects of phospholipid-cholesterol mass ratio,drug-lipid mass ratio,ultrasonic reaction time and temperature on the preparation of liposome. The appearance of drug-loaded liposome was modified by post-insertion method,and 5F-LP modified with pentapeptide YIGSR was prepared. The morphology and particle size of the liposome were also observed by TEM,and encapsulation efficiency of liposome was determined by protamine precipitation method. The content of 5F in liposome was determined by HPLC,and in vitro drug release of liposome was evaluated by dialysis method. RESULTS：The optimal preparation technology was as follows as phospholipid-cholesterol mass ratio of 6 ∶ 1,mass ratio of drug-lipid 1 ∶ 10,ultrasonic time 10 min,temperature 45 ℃. The prepared YIGSR-5F-LP was sphere or sphere type in shape with average particle size of 174. 8 nm,encapsulation efficiency of 88.9% and drug-loading amount of 8.2%. The release of liposome in vitro was slower than that of 5F solution and relased completely at 48 h. CONCLUSIONS：YIGSR-5F-LP is prepared successfully;and the YIGSR-5F-LP has sustained release property.

关 键 词：半边旗提取物5F 脂质体 制备工艺 正交试验 包封率 粒径 体外释放度 

分 类 号：R943[医药卫生—药剂学]