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
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篇名: 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
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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 mV;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Q48 h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。
ABSTRACT: 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 mV and -40.7 mV; 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 h of them in simulated gastric fluid were 38.6% and 70.5%, and Q48 h of 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.
期刊: 2016年第27卷第34期
作者: 何静,邱妍川,杨延音,刘松青,林凤云,江尚飞,朱照静
AUTHORS: HE Jing1,QIU Yanchuan2,YANG Yanyin2,LIU Songqing3,LIN Fengyun2,JIANG Shangfei2,ZHU Zhaojing
关键字: 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
KEYWORDS: Silymarin; PLGA; HPMCP; Nanoparticle; Release rate in vitro
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