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配比结构影响mPEG-PCL顺铂纳米粒子体外抗肿瘤的作用

Cisplatin-loaded mPEG-PCL Nanoparticles: Relation of PEG-PCL/PCL Hybrid Proportions and Antitumor Activity in Vitro

  • 摘要:
    目的 探讨实验室前期自行合成的5种配比的顺铂纳米粒子在体外的抗肿瘤作用。
    方法 通过开环聚合法制备mPEG-PCL两嵌段高分子和末端带有羟基的PCL,在开环聚合反应时,控制PEG和PCL的比例,合成不同亲水/疏水比例的聚合物。采用优化的w/o/w双乳化扩散/挥发法,制备负载顺铂药物的纳米粒子。采用MTT法研究其在体外对人胃癌细胞株BGC-823及SGC-7901的抗肿瘤活性,并在BGC-823及SGC-7901上验证空白纳米粒子的毒性。
    结果 体外实验显示5种配比纳米粒子的细胞毒性均呈现一定的异质性。所有纳米粒子均显示出良好的生物相容性。
    结论 纳米粒子的配比不同,其粒径、载药量等方面的性质也存在一定差异,体外抗肿瘤效果则呈现出一定的异质性,应当选择最佳配比进行深入研究和应用。

     

    Abstract:
    Objective To prepare cisplatin-loaded mPEG-PCL nanoparticles with different proportions of bi-block copolymer mPEG-PCL and PCL, and evaluate their antitumor effect in vitro.
    Methods mPEG-PCL and HO-PCL were synthesized by ring-opening polymerization method. Nanoparticles (NPs) prepared from mPEG-PCL/PCL hybrids were obtained by mixing PEG-PCL and PCL copolymer in different proportions. Drug-loading nanoparticles were prepared by w/o/w double emulsion method. The in vitro cytotoxicity of cisplatin-loaded nanoparticles on BGC-823 and SGC-7901 cell lines and the toxicity of the blank nanoparticles were evaluated by MTT assay.
    Results mPEG-PCL and PCL were synthesized with desired molecular weight. In vitro experiments showed the five kinds of nanoparticles had different antitumor activities and consistency in biocompatibility.
    Conclusion The properties of nanoparticles, such as diameters and drug loading capacities, vary with different ratio of components as well as the antitumor effect. The optimal hybrid proportions should be selected for further study and application.

     

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