Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan 430072, PR China.
Colloids Surf B Biointerfaces. 2010 Sep 1;79(2):427-33. doi: 10.1016/j.colsurfb.2010.05.014. Epub 2010 May 7.
Hyperbranched amphiphilic polymer PG6-PLA-PEG was synthesized through grafting hydrophobic poly(D,L-lactide) (PLA) segments and hydrophilic poly(ethylene glycol) (PEG) blocks to hydrophilic hyperbranched polyglycerol core (PG6), subsequently. To achieve cell targeting property, folic acid (FA) was further incorporated to the hyperbranched polymer to obtain PG6-PLA-PEG-FA. The polymers were characterized by (1)H NMR, UV-vis spectroscopy and combined size-exclusion chromatography and multiangle laser light scattering (SEC-MALLS) analysis. Due to the amphiphilicity, PG6-PLA-PEG and PG6-PLA-PEG-FA could self-assemble to form nanoparticles in aqueous solutions. Antineoplastic drug, paclitaxel (PTX), was encapsulated into the nanoparticles. The nanoparticles were observed by transmission electron microscopy (TEM). The targeting property of PG6-PLA-PEG-FA was evaluated in vitro. The results showed that the PTX loaded PG6-PLA-PEG-FA nanoparticles exhibited enhanced inhibition on folate receptor positive tumor cells due to the folate mediated targeting.
超支化两亲性聚合物 PG6-PLA-PEG 通过接枝疏水性聚（D，L-丙交酯）（PLA）段和亲水性聚乙二醇（PEG）块到亲水性超支化聚甘油核（PG6）上合成。为了实现细胞靶向性，进一步将叶酸（FA）掺入超支化聚合物中，得到 PG6-PLA-PEG-FA。通过（1）H NMR、UV-vis 光谱和组合的尺寸排阻色谱和多角度激光光散射（SEC-MALLS）分析对聚合物进行了表征。由于两亲性，PG6-PLA-PEG 和 PG6-PLA-PEG-FA 可以在水溶液中自组装形成纳米粒子。将抗肿瘤药物紫杉醇（PTX）包封到纳米粒子中。通过透射电子显微镜（TEM）观察纳米粒子。体外评价了 PG6-PLA-PEG-FA 的靶向性。结果表明，由于叶酸介导的靶向作用，负载 PTX 的 PG6-PLA-PEG-FA 纳米粒子对叶酸受体阳性肿瘤细胞表现出增强的抑制作用。
