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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 |
| TITLE： | |
| 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 |
| 阅读数： | 274 次 |
| 本月下载数： | 1 次 |
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