摘要
树枝状聚合物(dendrimer)是一种新近发展起来的纳米级聚合物,具有树枝状的骨架和球状外形,树枝状分支的末端连接数目众多的活性官能团。药物既可以被包封在树枝状聚合物骨架内部的空腔,也可以化学偶联在树枝状聚合物表面的官能团上。表面的官能团还能同时连接多种对机体某些器官、组织和细胞有特异性相互作用的靶向配基,从而将包封的药物或者偶联的药物带到病变部位实现靶向治疗。同时,树枝状聚合物粒径很小,范围从G0代到G10代只有1~15nm,偶联药物之后也不会超过30nm,这样的粒径范围使得以树枝状聚合物为基础制备的纳米粒具有较强的高通透高滞留效应效应(enhanced permeability and retention,EPR),从而对肿瘤组织实现被动靶向给药。
Dendrimer is a kind of newly developed polymer that possesses dendritic skelecton, spherical shapes and numerous terminal functional groups. Drug molecules can be either encapsulated in the hydrophobic chambers inside the dendritic skelecton, or conjugated to the functional groups on the surface of dendrimer. The terminal functional groups can meanwhile be used to chemically link to various ligands that have high affinity to specific organs, tissues or cells in the body, thus lead the encapsulated or conjugated drugs to the diseased sites for targeted therapy. Dendrimer is characteristic of small particle size (from G1 to G10 is only 1~15nm). Even after attachment of drag molecules, the resultant dendrimerdrag conjugates will definitely less than 30nm in size. This specific size range will provide the dendrimerbased conjugates or nanoparticles with strong enhanced permeability and retention effect (EPR effect), so as to achieve tumor-targeted drug delivery in the passive way.
出处
《中国医药技术经济与管理》
2008年第10期67-73,共7页
China Pharmaceutical Technology Economics & Management
基金
国家自然科学基金资助项目(项目编号:30600787)
关键词
树枝状聚合物
载体
靶向给药
dendrimer
drug carrier
targeted drug delivery