新型多西紫杉醇载药纳米微球的制备及其评价

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。

Preparation and evaluation of novel docetaxel-loaded nanoparticles

OBJECTIVE:To prepare docetaxel(DOC)-loaded nanoparticles with bi-block copolymers mPEG-PCL and evaluate their characters.METHODS: mPEG-PCL was synthesized by ring-opening polymerization method.The structure,molecular weight,diameters,morphology and biocompatibility of the nanoparticles were investigated.The DOC loaded nanodrug was prepared by a modified acetone nano-precipated method.The in vitro cytotoxicity of DOC-loaded nanoparticles against Taxotere was evaluated by CCK-8 assay on murine hepatic carcinoma H22 cells.RESULTS:mPEG-PCL copolymers were synthesized with desired molecular weight.The Doc-loaded nanoparticle was a monolayer spherical particle with a diameter less than 100 nm.The blank nanoparticles were non-toxic to the H22 cells.The encapsulation efficiency and drug loading content were 81.3% and 18.7%,respectively.In vitro cytotoxicity test demonstrated that the IC50 of DOC-loaded nanoparticles was slightly lower than that of Taxotere.CONCLUSION: This study was prepared,evaluated the DOC-loaded nanopartheles and provided an experimental basis for further research.