紫杉烷类PEG-PDLLA纳米粒的制备及其体外评价

Preparation and in-vitro evaluation of PEG-PDLLA in nanoparticle containing taxanes

采用乳化-溶剂蒸发法制备紫杉烷类PEG-PDLLA纳米粒,马尔文激光粒度仪测其粒径及Zeta电位;HPLC法测定纳米粒包封率和载药量;研究载药纳米粒在PBS中的释放动力学;初步评价载药纳米粒在MGC803、HeLa细胞中的摄取及细胞毒性。结果表明,通过包载形成的纳米粒的粒径为(13±1)nm,分布较集中。载体与药物的质量比在20∶1时,紫杉醇的均一性最好,卡巴他赛的包封率最高,达到88.77%。载药纳米粒具有较好的缓释作用,MGC803、HeLa细胞的存活率降低,与临床用注射剂效果相近。紫杉烷类PEG-PDLLA纳米粒的性质、释放、细胞抑瘤率都较好,可为开发紫杉烷类新型静脉注射制剂提供实验依据。

PEG-PDLLA in nanoparticle containing taxanes was prepared by emulsion solvent evaporation method.The particle size and Zeta potential were evaluated by Malvern Zerta sizer.The encapsulation efficiency and drug-loading content were examined by HPLC method.The kinetics of taxanes released from the nanoparticle in phosphate buffer solution（PBS）was studied.The uptake and cell toxicity of drug-loading nanoparticle in MGC803 and HeLa were preliminary evaluated.The result showed that the particle size is（13±1）nm,and distributionis concentrated.The ratio of the carrier and the drug is preferably 20∶1.The homogeneity of taxol is best,and encapsulation efficiency of cabazitaxel is highest,reach 88.77%.The nanoparticle with drug has a better sustained release.Survival of cancer cells in vitro anti-tumor decreased with similar clinical results with injections.The nature,release,and cell inhibition rate of PEG-PDLLA in nanoparticle containing taxanes is good.The test provides an experimental basis for the development of novel taxanes intravenous formulations.