水飞蓟素肠溶聚乳酸-羟基乙酸共聚物纳米粒的制备及体外释药研究  

Preparation and in vitro Drug Release of Enteric-coated Silymarin-PLGA Nanoparticles

作　　者：何静[1] 邱妍川[2] 杨延音[2] 刘松青[3] 林凤云[2] 江尚飞[2] 朱照静[2] 

机构地区：[1]重庆医药高等专科学校继续教育学院,重庆401331 [2]重庆医药高等专科学校药学院,重庆401331 [3]第三军医大学第一附属医院药剂科,重庆400038

出　　处：《中国药房》2016年第34期4842-4844,共3页China Pharmacy

基　　金：重庆市科技攻关计划项目(No.cstc2012gg-yyjs10008);重庆市卫生局医学科研计划项目(No.2012-2-256)

摘　　要：目的:制备水飞蓟素肠溶聚乳酸-羟基乙酸共聚物(PLGA)纳米粒,并研究其体外释药行为。方法:以羟丙基甲基纤维素邻苯二甲酸酯(HPMCP)为肠溶材料,采用纳米沉淀法制备水飞蓟素肠溶PLGA纳米粒和水飞蓟素PLGA纳米粒,观察其形态,检测其粒径、Zeta电位、包封率、载药量、稳定性、体外释放度(Q)。以粒径、包封率、载药量为指标筛选水飞蓟素肠溶PLGA纳米粒中PLGA-HPMCP质量比。结果:PLGA-HPMCP的最佳质量比为1∶0.25。所制水飞蓟素肠溶PLGA纳米粒和水飞蓟素PLGA纳米粒的粒径分别为224、193 nm,Zeta电位分别为-37.8、-40.7 m V;包封率分别为(74.7±2.2)%、(71.7±2.5)%,载药量分别为(5.39±0.24)%、(5.21±0.22)%;4℃下储存3个月后的渗漏率分别为0.2%、0.5%;人工胃液中Q_(48h)分别为38.6%、70.5%,人工肠液中Q48 h分别为80.2%、73.5%。结论:成功制得水飞蓟素肠溶PLGA纳米粒,其稳定性较好,能有效抑制水飞蓟素在人工胃液中的释放。OBJECTIVE：To prepare enteric-coated silymarin-PLGA nanoparticles,and to study its in vitro release behavior.METHODS： Using HPMCP as enteric-coated material,nanoprecipitation method was used to prepare enteric-coated silymarin-PLGA nanoparticles and silymarin-PLGA nanoparticles.The morphology of nanoparticles were observed,and the particle size,Zeta-potential,encapsulation efficiency,drug-loading amount,stability and in vitro release rate（Q） were detected.The ratio of PLGA-HPMCP in enteric-coated silymarin-PLGA nanoparticles was screened by using particle size,encapsulation ratio and drug-loading capacity as indexes.RESULTS：The best PLGA-HPMCP ratio was 1 ∶ 0.25.The particle size of enteric-coated silymarin-PLGA nanoparticles and silymarin-PLGA nanoparticles were 224 nm and 193 nm,Zeta potential were-37.8 m V and-40.7m V;encapsulation ratio were（74.7 ± 2.2）% and（71.7 ± 2.5）%,and drug-loading amount were（5.39 ± 0.24）% and（5.21 ±0.22）%;the percolation rates of them were 0.2% and 0.5% at 4 ℃ 3 months later;Q48 hof them in simulated gastric fluid were38.6% and 70.5%,and Q48 hof them in simulated intestinal fluid were 80.2% and 73.5%,respectively.CONCLUSIONS：The enteric-coated silymarin-PLGA nanoparticles are prepared successfully with good stability,and can effectively inhibit the release of silymarin in simulated gastric fluid.

关 键 词：水飞蓟素 聚乳酸-羟基乙酸共聚物 羟丙基甲基纤维素邻苯二甲酸酯 纳米粒 体外释放度 

分 类 号：R943[医药卫生—药剂学] R927[医药卫生—药学]