土贝母皂苷甲长循环脂质体的制备及体外性质考察  

Study on the Preparation and in Vitro Properties of Tubeimoside A Long-circulating Liposomes

作　　者：董荧荧 余陈欢[2] 俞冰[1] 俞文英[2] DONG Yingying;YU Chenhuan;YU Bing;YU Wenying(Zhejiang Chinese Medical University,Hangzhou 310053,China;Zhejiang Academy of Medical Sciences,Hangzhou 310013,China)

机构地区：[1]浙江中医药大学,杭州310053 [2]浙江省医学科学院,杭州310013

出　　处：《中国现代应用药学》2020年第7期832-836,共5页Chinese Journal of Modern Applied Pharmacy

基　　金：浙江省公益技术应用研究院所专项(2015F50065)。

摘　　要：目的制备土贝母皂苷甲长循环脂质体(tubeimoside A long-circulating liposomes,TA-LC-Lipo),并进行体外性质考察。方法乙醇注入法制备TA-LC-Lipo;采用HPLC测定包封率及体外释放率;通过Marlvern激光粒径分析仪测定粒径和Zeta电位;肉眼观察法和紫外分光光度法评价其溶血作用。结果确定处方为大豆磷脂浓度10 mg·mL^-1、药脂比1∶10、大豆磷脂∶胆固醇=4∶1、DSPE-PEG 2000的摩尔含量为5%。制备得到的TA-LC-Lipo的平均粒径、PDI、电位、包封率分别为123.0 nm,0.134,-1.20 mV,86.2%。结论制得的TA-LC-Lipo粒度分布均匀,包封率较高,有较好的缓释作用,并能有效改善土贝母皂苷甲的溶血现象。OBJECTIVE To prepare tubeimuside A long-circulating liposomes(TA-LC-Lipo),and to study the in vitro properties of TA-LC-Lipo.METHODS TA-LC-Lipo was prepared by ethanol injection;encapsulation efficiency and in vitro release rate of TA-LC-Lipo were determined by HPLC;particle size and Zeta potential of TA-LC-Lipo were measured by a Marlvern Zetasizer Nano-ZS90;hemolysis of TA-LC-Lipo was assessed by visual observation and UV analysis.RESULTS The optimum prescription was as follows:the concentration of soybean phospholipid(SPC)was 10 mg·mL^-1,the ratio of drug to SPC was 1∶10,the ratio of SPC to cholesterol was 4∶1,and the molar content of DSPE-PEG 2000 was 5%.The average particle size,PDI,Zeta potential,and encapsulation efficiency of the prepared TA-LC-Lipo were 123.0 nm,0.134,-1.20 mV,and 86.2%,respectively.CONCLUSION The prepared TA-LC-Lipo shows uniform particle size distribution,high encapsulation efficiency,sustained release,and low hemolytic activity in vitro.

关 键 词：土贝母皂苷甲 长循环脂质体 体外释放 体外溶血 

分 类 号：R943[医药卫生—药剂学]