新型顺铂纳米微球的制备及性质研究

Novel nanoparticles of cisplatin:Preparation and study of properties

目的:采用自行合成的高分子载体,制备负载顺铂的纳米微球,全面考察其性质。方法:通过开环聚合法,制备单甲氧基聚乙二醇-聚己内酯(mPEG-PCL)两嵌段聚合物以及末端带有羟基的PCL作为载体,采用优化的w/o/w双乳化扩散/挥发法,制备负载顺铂的纳米微球。考察载体的结构、分子量、纳米微球的形态、粒径分布、稳定性、生物相容性等性质。结果:通过开环聚合法合成mPEG-PCL两嵌段聚合物以及末端带有羟基的PCL,测定分子量和设计分子量相近。通过双乳剂法制备的空白粒子平均粒径为326.9±5.4nm,载药粒子在冻干前后的粒径分别为339.1±4.9及370.3±2.5nm。粒子呈规整的球形,在水溶液中稳定。顺铂的载药效率为77.4%,载药量为4.72%。体外释放实验显示,载药粒子具有缓释特征,在6h、24h、48h分别释放53%、75%、93%。载体在高浓度时对细胞生长无抑制作用,毒性低。结论:研究表明这种新型载药系统具有良好的应用价值。

Objective：to prepare cisplatin- loaded nanoparticles with bi -block copolymer mPEG -PCL and PCL, and evaluate their properties. Methods ： mPEG - PCL and HO - PCL were synthesized by ring - opening poly- merization method and the nanoparticles were prepared by developed w/o/w double emulsion method. The structure and molecular weight of the polymers, the morphology of the nanoparticles, as well as their stability and biocompatibility were studied. Results： mPEG - PCL and PCL were synthesized with desired molecular weight. The diameter of blank nanopaticles was 326.9 ± 5.4nm, and the diameters of cisplatin - loaded nanoparticles before and after freeze dry were 339.1 ± 4.9 and 370.3 ± 2.5nm, respectively. The encapsulation efficiency and drug loading content were 77.4% and 4.72% respectively. The in vitro release presented a sustain - release pattern. The blank nanoparticles were non - toxic to the Lo2 cell line. Conclusion： The above findings indicate the potential of this nanoparticles as carrier for cisplatin.