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目的:用可生物降解的高分子材料制备白藜芦醇载药纳米微球,并检测该载药纳米微球的各项特征,评价其体外抗肿瘤效果。方法:通过开环聚合法制备mPEG-PCL二嵌段共聚物,采用溶剂分散法制备负载白藜芦醇的纳米微球。观察纳米微球的形态、粒径分布、包封率和载药量、体外释放和体外对于恶性胶质瘤细胞株U251的抗肿瘤活性。结果:通过溶剂分散法制备的纳米粒子呈球形,平均粒径为(71.8±0.2)nm,白藜芦醇纳米微球的最高载药量达到19.4%。体外释放实验显示,载药微球具有缓释特性。细胞与负载荧光素纳米微球共培养后发现,细胞可通过胞吞作用将纳米微球摄入。细胞实验表明,白藜芦醇纳米微球对U251细胞的生长有明显的抑制作用,特别是在低浓度下白藜芦醇微球对于肿瘤细胞的杀伤作用明显优于游离白藜芦醇,随着药物浓度的增加白藜芦醇微球与游离白藜芦醇对于肿瘤细胞的杀伤作用相差不大。结论:采用mPEG-PCL为载体制备的白藜芦醇纳米微球具有缓释特性和抑制U251细胞增殖的作用,具有良好的应用价值。
OBJECTIVE: To prepare resveratrol-loaded nanospheres by using biodegradable macromolecular materials and to detect the characteristics of the nanodisperse drug-loaded nanospheres and to evaluate its anti-tumor effect in vitro. Methods: The mPEG-PCL diblock copolymer was prepared by ring-opening polymerization and the resveratrol-loaded nanospheres were prepared by solvent dispersion method. The morphology, particle size distribution, encapsulation efficiency and drug loading of the nanospheres were investigated. The in vitro release and in vitro antitumor activity of the glioma cell line U251 were observed. Results: The nanoparticles prepared by solvent dispersion method were spherical with an average diameter of (71.8 ± 0.2) nm and the highest drug loading of resveratrol nanospheres was 19.4%. In vitro release experiments showed that drug-loaded microspheres with sustained release characteristics. After co-culture of cells with fluorescein-loaded microspheres, the cells can be taken up by nanospheres through endocytosis. Cell experiments showed that resveratrol nanoparticles microspheres significantly inhibited the growth of U251 cells, especially at low concentrations of resveratrol microspheres on the killing effect of tumor cells was significantly better than the free resveratrol, with With the increase of drug concentration, resveratrol microspheres and free resveratrol have little effect on tumor cells. CONCLUSION: Resveratrol nanospheres prepared with mPEG-PCL as carrier have the properties of sustained release and inhibition of proliferation of U251 cells, and have good application value.