Li Ning Ning, Cai Xiao Yan, Chen Jiu Cun, Hu Xue Feng, Xu Li Qun
Institute for Clean Energy and Advanced Materials, Faculty of Materials and Energy, Southwest University, Chongqing 400715, China.
National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
Polymers (Basel). 2016 Oct 26;8(11):379. doi: 10.3390/polym8110379.
Amphiphilic poly(ε-caprolactone)--poly[2-(α-d-mannopyranosyloxy) ethyl acrylamide] (PCL--PManEA) block copolymers were synthesized via a combination of ring-opening polymerization (ROP), reversible addition-fragmentation chain transfer (RAFT) polymerization and reactive ester-amine reaction. The PCL--PManEA block copolymers can self-assemble into micelles and encapsulate anticancer drug doxorubicin (DOX). To enhance mucoadhesive property of the resulting DOX-loaded PCL--PManEA micelles, Concanavalin A (ConA) lectin was further conjugated with the micelles. Turbidimetric assay using mucin shows that the DOX-loaded PCL--PManEA@ConA micelles are mucoadhesive. DOX release from the DOX-loaded PCL--PManEA@ConA micelles in artificial urine at 37 °C exhibits an initial burst release, followed by a sustained and slow release over three days. Confocal laser scanning microscope (CLSM) images indicate that the DOX-loaded PCL--PManEA@ConA micelles can be effectively internalized by UMUC3 human urothelial carcinoma cells. The DOX-loaded PCL--PManEA@ConA micelles exhibit significant cytotoxicity to these cells.
两亲性聚（ε-己内酯）-聚[2-（α-D-甘露吡喃糖氧基）乙基丙烯酰胺]（PCL-PManEA）嵌段共聚物通过开环聚合（ROP）、可逆加成-断裂链转移（RAFT）聚合和活性酯-胺反应相结合的方法合成。PCL-PManEA嵌段共聚物可自组装成胶束并包封抗癌药物阿霉素（DOX）。为增强所得载DOX的PCL-PManEA胶束的粘膜粘附性能，将伴刀豆球蛋白A（ConA）凝集素进一步与胶束偶联。使用粘蛋白的比浊法表明，载DOX的PCL-PManEA@ConA胶束具有粘膜粘附性。载DOX的PCL-PManEA@ConA胶束在37℃的人工尿液中的DOX释放呈现出初始突释，随后在三天内持续缓慢释放。共聚焦激光扫描显微镜（CLSM）图像表明，载DOX的PCL-PManEA@ConA胶束可被UMUC3人膀胱癌细胞有效内化。载DOX的PCL-PManEA@ConA胶束对这些细胞表现出显著的细胞毒性。
