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

发布时间：2018-09-10 21:02

【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。
[Abstract]:Aim: to prepare silymarin enteric poly (lactic acid-glycolic acid) (PLGA) nanoparticles and study their drug release behavior in vitro. Methods: silymarin enteric PLGA nanoparticles and silymarin PLGA nanoparticles were prepared using hydroxypropyl methyl cellulose phthalate (HPMCP) as enteric material. The morphology of silymarin enteric PLGA nanoparticles and silymarin PLGA nanoparticles were observed. Stability, in vitro release of (Q). The mass ratio of PLGA-HPMCP in enteric PLGA nanoparticles of silymarin was screened according to the particle size, encapsulation efficiency and drug load. Results the optimum mass ratio of 1: 0. 25 for 1: PLGA-HPMCP. The silymarin enteric PLGA nanoparticles and silymarin PLGA nanoparticles had 224193 nm,Zeta potential of -37.8 and 40.7 MV respectively, the entrapment efficiency was (74.7 卤2.2), (71.7 卤2.5), the drug loading was (5.39 卤0.24), and the leakage rate of artificial stomach was 0.550 after storage at 4 鈩，

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