自组装型树形分子在生物医学领域的研究进展  

Self-assembling dendrimers for biomedical applications

作　　者：史康洁 陈家轩 刘潇璇 彭玲 SHI Kangjie;CHEN Jiaxuan;LIU Xiaoxuan;PENG Ling(State Key Laboratory of Natural Medicines,Center of Advanced Pharmaceuticals and Biomaterials,China Pharmaceutical University,Nanjing 210009,China;Interdisciplinary Center of Nanoscience of Marseille,Aix-Marseille University,CNRS,Marseille 13188,France)

机构地区：[1]中国药科大学,天然药物活性组分与药效国家重点实验室,药物科学研究院高端药物制剂与材料研究中心,南京210009 [2]法国国家科学院马赛纳米交叉科学研究中心,艾克斯马赛大学,法国马赛13188

出　　处：《中国药科大学学报》2021年第1期20-30,共11页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.50773127,No.81701815);国家重点研发计划“政府间国际科技创新合作/港澳台科技创新合作”重点专项资助项目(No.2018YFE0117800);江苏省自然科学基金资助项目(No.BK20170734);江苏省“高层次创新创业人才引进计划”资助项目;中国药科大学天然药物活性组分与药效国家重点实验室资助项目(No.SKLN⁃MZZ202007);法国外交部埃菲尔奖学金、法国国家癌症防治联盟资助项目。

摘　　要：树形分子因其具有独特的树枝状分子结构以及多价协同作用等特性在生物医学领域具有广阔的应用前景。然而树形分子合成繁琐费时、纯化困难,使得大规模制备高代无缺陷的树形分子困难重重。为了克服这一困难,研究人员提出了一种基于自组装的方法构建树形分子的策略,即利用低代的两亲性树形分子自组装构建非共价超分子树形分子,用以模拟高代共价树形分子。本文介绍超分子树形分子的研究及其在生物医学领域的应用,例如输送小分子抗肿瘤药物、核酸治疗试剂和分子造影剂等,并通过一些代表性的实例展现超分子树形分子的应用前景与挑战。Dendrimers,a special class of synthetic polymers known for their well-defined ramified structures and unique multivalent cooperativity,hold great promise for various biomedical applications.However,preparation of defect-free dendrimers of high-generation on a large scale remains challenging because of the tedious and time-consuming synthesis as well as difficult purification.To overcome these limitations,an alternative strategy based on self-assembling approach has been developed to construct supramolecular dendrimers using small amphiphilic dendrimer-building units.By virtue of the amphiphilic nature,these small dendrimer-building units self-assemble and form large non-covalent supramolecular dendritic structures that mimic high-generation covalent dendrimers.Here,we present a brief overview of the supramolecular dendrimers developed in our group for the delivery of nucleic acid therapeutics,anticancer drug and imaging agents.

关 键 词：聚酰胺-胺类树形分子 自组装型树形分子 树形分子合成 药物递送 基因递送 

分 类 号：R944[医药卫生—药剂学]