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目的:采用自行合成的高分子载体,制备负载多西紫杉醇(DOC)的纳米微球,全面评价其性质。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)两嵌段聚合物载体,考察载体的结构、相对分子质量、纳米微球粒径、形貌、生物相容性等性质。以改良的丙酮-纳米沉淀法制备负载DOC的载药纳米微球,以CCK-8法,评价该载药微球在体外对于肝癌细胞株H22的抗肿瘤活性,并与泰素帝相比较。结果:通过开环聚合法合成mPEG-PCL两嵌段聚合物,测定相对分子质量和设计相对分子质量相近。DOC纳米微球为不规则的圆形,表面光滑,其粒径<100nm。载体在高浓度时对细胞生长无抑制作用,毒性低。DOC的载药效率为81.3%,载药量为18.7%。体外细胞毒性显示,DOC纳米载体组IC50略小于裸药泰素帝。结论:该实验制备并评估了DOC载药纳米微球,为进一步研究提供了实验依据。
OBJECTIVE: To prepare docetaxel (DOC) loaded nanospheres by self-synthesized macromolecule carrier and evaluate its properties comprehensively. Methods: The monomeric poly (ethylene glycol) -polycaprolactone (mPEG-PCL) diblock polymer was prepared by ring-opening polymerization. The structure, molecular weight and particle size of the nanospheres were investigated. Appearance, biocompatibility and other properties. The drug-loaded nanospheres loaded with DOC were prepared by modified acetone-nano-precipitation method. The anticancer activity of the drug-loaded microspheres against H22 cell line H22 was evaluated by CCK-8 assay and compared with Taxus. Results: mPEG-PCL diblock polymer was synthesized by ring-opening polymerization. The relative molecular mass and relative molecular mass were similar. DOC nanospheres are irregular round, smooth surface, the particle size of <100nm. The carrier does not inhibit cell growth at high concentrations and has low toxicity. DOC loading efficiency was 81.3%, drug loading was 18.7%. In vitro cytotoxicity showed that the IC50 of the DOC nanocarrier group was slightly smaller than that of the taxotere. Conclusion: This experiment prepared and evaluated the drug loaded nano-microspheres for DOC, which provided the experimental basis for further study.