多聚物-药物偶合物的研究及应用进展

多聚物-药物偶合物由含有功能基团、具有较大相对分子质量的药物修饰多聚物与药物,包括蛋白质类药物、寡核苷酸类药物及化学抗癌药物通过化学键定点相连而形成。由于药物修饰多聚物的介入及参与,多聚物-药物偶合物与所连接的原药物相比,可显示抗酶解能力增强、稳定性提高、体内代谢半衰期延长、对肿瘤细胞膜的透过性增加、在肿瘤部位浓集、药性释放平缓、毒副作用降低等特点。多聚物-药物偶合物的研发正成为高效低毒新型药物研发的重要方向。

Progress in research and application of polymer-drug conjugates

Polymer-drug conjugates(PDCs) can be synthesized using drug modification polymers(DMP).PDCs have big molecular weights,functional groups and drugs used in clinic,and are formed by chemical bonds at a definitive position.Various types of drugs,including proteins,oligonucleotides and chemical anticancers,can be used to make PDCs.Since the participation and intervention of the DMP,the produced PDCs have stronger anti-enzymolysising ability,better stability and longer half-life of metabolism,better permeability...