白藜芦醇载药纳米微球的制备?表征及体外对胶质瘤U251细胞的抑制作用
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Synthesis and characterization of nanoparticles loaded with resveratrol and observation of its inhibition on U251 cells
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    摘要:

    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-

    Abstract:

    Objective:To characterize nanoparticles which were prepared from biodegradable polymers loaded with resveratrol,and observe the in-vitro anti-tumor effect. Methods:Firstly,mPEG-PCL amphipathic block copolymers were synthesized with ring-opening method. Nanoparticles loaded with resveratrol were then successfully prepared with solvent dispersion method. The morphology,size distribution,encapsulation rate and loading capacity,in-vitro release and in-vitro cytotoxicity against malignant glioma were studied. Results:Nanoparticles prepared with solvent dispersion method proved to be spheric with the size of 71.8±0.2 nm. The highest encapsulation rate was 19.4%. In vitro release experiment revealed the existence of gradual release property. After co-cultured with fluorescein nanospheres,the cells can intake nanospheres through endocytosis. In-vitro cell experiment showed that resveratrol-loaded nanoparticles significantly inhibitied the growth of U251 cells. Especially in low concentrations,resveratrol-loaded nanospheres had stronger cytotoxicity on tumor cells than single free resveratrol. With the increase of drug concentration,resveratrol-loaded nanoparticles had similar cytotoxicity on tumor cells with free resveratrol medicine. Conclusion:Nanoparticles loaded with resveratrol are effective in inhibiting the growth of U251 tumor cells. The study also suggests that they are potentially useful due to their property of gradual release.

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姜志峰,冯素银,李晓林,陆小伟,邵君飞.白藜芦醇载药纳米微球的制备?表征及体外对胶质瘤U251细胞的抑制作用[J].南京医科大学学报(自然科学版),2010,(9):1240-1244

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  • 收稿日期:2010-04-29
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