Shen Kexin, Li Di, Guan Jingjing, Ding Jianxun, Wang Zhongtang, Gu Jingkai, Liu Tongjun, Chen Xuesi
Jilin University, Changchun, PR China; Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, PR China.
Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, PR China.
Nanomedicine. 2017 Apr;13(3):1279-1288. doi: 10.1016/j.nano.2016.12.022. Epub 2017 Jan 5.
A c(RGDfC)-decorated polylactide stereocomplex micelle (cRGD-SCM) was prepared through the stereocomplex and hydrophobic interactions among 4-arm poly(ethylene glycol)-block-poly(D-lactide) (4-arm PEG-b-PDLA), methoxy poly(ethylene glycol)-block-poly(L-lactide) (mPEG-b-PLLA), and c(RGDfC)-poly(ethylene glycol)-block-poly(L-lactide) (cRGD-PEG-b-PLLA) for targeted treatment of αβ integrin-positive C26 colon cancer. Doxorubicin (DOX), a model antitumor drug, was loaded into cRGD-SCM with a diameter of approximately 100nm, and the drug loading efficiency was 45.9wt.%. cRGD-SCM/DOX with a sustained release pattern exhibited prolonged circulation time, upregulated accumulation in tumor, enhanced tumor inhibition, and decreased side effects compared with free DOX and non-targeting SCM/DOX in vivo. More interestingly, the targeting ligand in the terminal of PEG can be easily replaced with other targeting groups according to the different types of malignancies. Therefore, the cRGD-decorated platform might be a promising targeted drug delivery system for personal chemotherapy clinically.
通过四臂聚（乙二醇）-嵌段-聚（D-丙交酯）（4-臂PEG-b-PDLA）、甲氧基聚（乙二醇）-嵌段-聚（L-丙交酯）（mPEG-b-PLLA）和c（RGDfC）-聚（乙二醇）-嵌段-聚（L-丙交酯）（cRGD-PEG-b-PLLA）之间的立体复合和疏水相互作用制备了一种c（RGDfC）修饰的聚丙交酯立体复合胶束（cRGD-SCM），用于靶向治疗αβ整合素阳性的C26结肠癌。将模型抗肿瘤药物阿霉素（DOX）负载到直径约为100nm的cRGD-SCM中，载药效率为45.9wt.%。与游离DOX和非靶向SCM/DOX相比，具有缓释模式的cRGD-SCM/DOX在体内表现出延长的循环时间、肿瘤中积累上调、增强的肿瘤抑制作用以及副作用减少。更有趣的是，PEG末端的靶向配体可根据不同类型的恶性肿瘤轻松替换为其他靶向基团。因此，cRGD修饰的平台可能是临床上一种有前景的个性化化疗靶向给药系统。
