长春碱PCL-PEG-PCL纳米粒的制备及质量评价

目的： 制备负载长春碱的PCL-PEG₆₀₀₀-PCL纳米粒，并研究其理化性质及体外抗肿瘤活性。 方法： 采用开环聚合法制备PCL-PEG₆₀₀₀-PCL三嵌段元共聚物，通过共沉淀法制备了长春碱的PCL-PEG₆₀₀₀-PCL纳米粒，并测定其形态、粒径及多分散度、粒子产率、载药率和包封率、体外释放度，采用MTT法考察长春碱纳米粒对人白血病细胞耐药株K562/A02的细胞毒性。 结果： 透射电镜结果表明：得到了具有核-壳结构的球形粒子，并且纳米粒的平均粒径为（185±2.7） nm，载药率和包封率分别为28.83%和86.52%，体外释放研究表明：长春碱从纳米粒中的释放量（9 h）达70%以上，24 h释放基本完全。负载长春碱的纳米粒对K562/A02的抑制率比同浓度下长春碱溶液组显著增加。 结论： PCL-PEG-PCL纳米粒可以作为长春碱的载体，所得粒子形状规则，包封率高，性质稳定，药物释放缓慢。长春碱经过PCL-PEG-PCL纳米粒的包裹后，对K562/A02的细胞毒性显著增强。

Preparation and evaluation of vinblastine PCL-PEG-PCL nanoparticles

Aim:To prepare vinblastine-loaded PCL-PEG6000-PCL nanoparticles,and to study their physicochemical properties and in vitro antitumor activity.Methods:PCL-PEG6000-PCL triblock copolymer was prepared by ring-opening polymerization,and vinblastine-loaded PCL-PEG6000-PCL nanoparticles was prepared by coprecipitation.The morphous,particle size,polydisperse index,particle yield,the drug-loading content,the encapsulation efficiency and in vitro release rate of these vinblastine-loaded nanoparticles were determined...