Niu Chuanqiang, Sun Qiquan, Zhou Jingxing, Cheng Du, Hong Guobin
Department of Radiology, Fifth Affiliated Hospital, Sun Yat-Sen Memorial Hospital, China.
Asian Pac J Cancer Prev. 2011;12(8):1995-9.
Targeted delivery of anti-cancer drugs is a highly desirable strategy to improve therapeutic outcome because of the combination of enhanced efficacy and reduced toxicity. In this study, the anti-cancer drug doxorubicin (DOX) was accommodated in the cores of polymeric micelles self-assembled from amphiphilic block copolymers of poly(ethylene glycol)(PEGs) and poly(D,L-lactide) (PDLLA) with a targeting ligand (folate) attached to the distal ends of the PEG (Folate-PEG-PDLLA). In vitro tumor cell targeting efficacy was evaluated upon observing cellular uptake of these micelles by human hepatic carcinoma cells (Bel 7402 cells) overexpressing surface receptors for folate. In control release tests, DOX behavior of controlled release in folate receptor-mediated micellar folate-PEG-PDLLA-DOX-micelles was obvious, with pH sensitivity. Bel 7402 cells showed micelles to have low toxicity and suggested potential therapeustic application as a multifunctional platform for tumor management.
由于提高疗效和降低毒性的双重作用，靶向递送抗癌药物是一种非常理想的改善治疗效果的策略。在本研究中，抗癌药物阿霉素（DOX）被包裹在由聚乙二醇（PEG）和聚（D，L-丙交酯）（PDLLA）的两亲性嵌段共聚物自组装形成的聚合物胶束核中，且在PEG的远端连接了靶向配体（叶酸）（叶酸-PEG-PDLLA）。通过观察过表达叶酸表面受体的人肝癌细胞（Bel 7402细胞）对这些胶束的细胞摄取情况，评估了体外肿瘤细胞靶向效果。在控释试验中，叶酸受体介导的胶束叶酸-PEG-PDLLA-DOX-胶束中DOX的控释行为明显，具有pH敏感性。Bel 7402细胞显示胶束具有低毒性，并表明其作为肿瘤治疗多功能平台具有潜在的治疗应用价值。
