School of Life Sciences, Tsinghua University, Beijing 100084, PR China.
Biomaterials. 2013 Aug;34(25):6058-67. doi: 10.1016/j.biomaterials.2013.04.052. Epub 2013 May 18.
We developed a system of nanoparticles (NPs) of cholic acid functionalized, star-shaped block copolymer consisting of PLGA and vitamin E TPGS for sustained and controlled delivery of docetaxel for treatment of cervical cancer, which demonstrated superior in vitro and in vivo performance in comparison with the drug-loaded PLGA NPs and the linear PLGA-b-TPGS copolymer NPs. The star-shaped block copolymer CA-PLGA-b-TPGS of three branch arms was synthesized through the core-first approach and characterized by (1)H NMR, GPC and TGA. The drug- or coumarin 6-loaded NPs were prepared by a modified nanoprecipitation technique and then characterized in terms of size and size distribution, surface morphology and surface charge, drug encapsulation efficiency, in vitro release profile and physical state of the encapsulated drug. The CA-PLGA-b-TPGS NPs were found to have the highest cellular uptake efficiency, the highest antitumor efficacy compared with PLGA-b-TPGS NPs and PLGA NPs. The results suggest that such a star-shaped copolymer CA-PLGA-b-TPGS could be used as a new molecular biomaterial for drug delivery of high efficiency.
我们开发了一种由胆酸功能化的星形嵌段共聚物纳米粒子（NPs）组成的系统，该共聚物由 PLGA 和维生素 E TPGS 组成，用于持续和控制多西他赛的递送，以治疗宫颈癌，与载药 PLGA NPs 和线性 PLGA-b-TPGS 共聚物 NPs 相比，其具有优越的体外和体内性能。通过核优先方法合成了具有三个支链臂的星形嵌段共聚物 CA-PLGA-b-TPGS，并通过（1）H NMR、GPC 和 TGA 进行了表征。通过改良的纳米沉淀技术制备了载药或香豆素 6 的 NPs，并对其粒径和粒径分布、表面形态和表面电荷、载药包封效率、体外释放曲线和包封药物的物理状态进行了表征。与 PLGA-b-TPGS NPs 和 PLGA NPs 相比，CA-PLGA-b-TPGS NPs 具有最高的细胞摄取效率和最高的抗肿瘤功效。结果表明，这种星形共聚物 CA-PLGA-b-TPGS 可用作高效药物递送的新型分子生物材料。
