聚合物胶束结合靶向在肿瘤化疗中的研究进展

Research Progress in Polymeric Micelles with Tumor-Targeting in Chemotherapy

肿瘤研究的一个主要方向是开发高效无毒副作用的药物载体系统。聚合物胶束由内部可装载难溶性药物的疏水内核,外部能提高体内运输作用的亲水外壳组成,粒径一般为10～100nm左右。这种粒径范围的载药体系既能逃脱肾脏的排泄清除,又能躲避内皮网状系统的吞噬,延长药物在血液中的循环时间。聚合物胶束结合肿瘤靶向在化疗方面的应用,能够有效改善化疗药物的水溶性,提高化疗药物的利用率和抗肿瘤活性,降低对机体正常细胞组织的毒副作用,克服多药耐药性问题,进而极大地提高了肿瘤化疗效果和促进了肿瘤化疗的发展进步。本文着重综述聚合物胶束在化疗药物载药与靶向策略方面的研究现状与进展。

A major field in cancer research is to develop carriers that can deliver drugs into targeted region effectively without side effects. Polymeric micelles （PMs） are core-shell structure with diameters of 10-100nm （suitable size with a narrow distribution could avoid rapid renal excretion and entrapment by the reticuloendothelial system）, which are self-assembled with good biodegradable and biocompatible polymer to form hydrophobic core and hydrophilic shell in an aqueous media. The preparation of PMs with stimuli-responsive block copolymers and modification of target molecules on PMs＇ surface could significantly improve the performance of the drug-loaded, enhance drug utilization and anti-tumor activity, reduce the normal tissue toxicity and solve the problem of multi-drug resistance, and thus contribute significantly to the development and progress of chemotherapy. Here we review some of the promising analog of targeting strategies that are under development for drug delivery. This review describes the preparation of polymeric micelles and the targeted modification which greatly enhance the effect of chemotherapy.