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.
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
Keywords
SilymarinPLGAHPMCPNanoparticleRelease rate in vitro