【摘要】 目的:制备青蒿琥酯纳米粒,并对其性质及体外细胞抑制作用进行研究。方法:以聚乳酸-羟基乙酸共聚物(PLGA)为载体,采用自乳化方法制备青蒿琥酯纳米粒。扫描电镜观察纳米粒的形态,激光粒度仪测定纳米粒的粒径及其分布;考察纳米粒的载药量、包封率、体外释放情况;MTT法考察纳米粒对人白血病细胞株K562在不同时间(24、48、72h)的体外细胞抑制率,并与青蒿琥酯(原料药)比较。结果:所制青蒿琥酯纳米粒为圆球形,表面光滑,平均粒径为(144±3.0)nm,Zeta电位是-31.5mV,平均载药量和包封率分别为14%、84%;体外释放试验前期有明显突释现象,前24h累积释放度为46%,其后释放均匀,120h累积释放度达65%,具有缓释作用;其在72h时对细胞抑制率高于青蒿琥酯组(76.4%vs.59.1%),有较强抑制作用(P<0.05)。结论:所制青蒿琥酯纳米粒在体外具有较好的缓释性,对K562细胞有较强的抑制作用。更多还原

【Abstract】 OBJECTIVE: To prepare Artesunate nanoparticles,and to investigate their characteristics and inhibitory effect on cell in vitro.METHODS:Spontaneous emulsion solvent diffusion method was used to prepare Artesunate nanoparticles using poly (lactide-co-glycolide) (PLGA) as carrier.Then their morphology was detected by scanning electron microscorpe.The particle size and its distribution of nanoparticles were determined by laser particle measurer.The drug-loading amount,encapsulation rate and drug released characteristics were identified.The inhibition effects of nanoparticles on K562 cells at different time (24 h,48 h,72 h) were determined by MTT assay and compared with that of artesunate raw material.RESULTS:Prepared Artesunate nanoparticles were spherical and uniform with mean diameter of (144±3.0) nm.Zeta potential was -31.5 mV.Their mean drug-loading amount and encapsulation rate were 14% and 84%,respectively.At early period of in vitro release test,Artesunate nanoparticles released suddenly.At first 24 h,accumulative drug release rate was 46% and showed significant sustained release.Accumulative drug release rate was 65% at 120 h.At 72 h,cell inhibition rate of Artesunate nanoparticles was higher than that of artesunate raw material (76.4% vs.59.1%).The inhibitory effect on K562 cells of Artesunate nanoparticles was significant (P<0.05).CONCLUSION: Prepared Artesunate nanoparticles are characterized with sustained-release property.Artesunate nanoparticles can inhibit K562 cells proliferation efficiently in vitro.更多还原