多聚物-药物偶合物的研究及应用进展  

Progress in research and application of polymer-drug conjugates

作　　者：孔艳[1] 廖永祥[1] 胡乃峰[1] 王朴[1] 

机构地区：[1]山东大学药学院,济南250012

出　　处：《中国新药杂志》2010年第4期290-295,共6页Chinese Journal of New Drugs

基　　金：山东省自然科学基金(Y2006B15)

摘　　要：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。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 across cell membrane,increased concentration in cancer cells,smooth releasing,and lower toxic and side effects as compared with the original drugs in the human body.The research and development of the PDCs is an important direction in the new and efficient drug development fields.

关 键 词：多聚物-药物偶合物 药物修饰多聚物 功能基团 定点连接 

分 类 号：R914[医药卫生—药物化学]