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靶向给药系统(targeting drug delivery system,TDDS)能够选择性作用于病变部位,控制药物的分布与释放,提高药效和降低毒副作用,已成为癌症治疗领域的研究热点之一。聚酰胺-胺树状大分子(polyamidoamine dendrimer,PAMAMD)是一种新近发展起来的纳米级药物载体,多分枝、单分散性、三维结构和主-客体包裹能力使其可作为药物基因载体和影像试剂。PAMAMD丰富的末端功能团能同时连接各种具有特异选择性的靶向配基,再通过包裹作用或化学偶联作用将药物或治疗基因载入,最后将药物和治疗基因带到病变部位释放从而实现靶向治疗。这种以PAMAMD为基础制备的纳米靶向给药系统具有较小的粒径,强的高通透高滞留(enhanced permeability and retention,EPR)效应和低毒性等特点。本文概述了各种靶向配基修饰的PAMAMD的应用研究进展,并展望了今后的研究方向。
Targeting drug delivery system (TDDS) has been one of the hot topics in the field of cancer therapy because it can selectively act on diseased sites, control drug distribution and release, improve efficacy and reduce side effects. Polyamidoamine dendrimer (PAMAMD) is a newly developed nanophase drug carrier with multi-branching, monodispersity, three-dimensional structure and host-guest encapsulation ability that allows it to be used as a drug gene carrier and imaging Reagents. PAMAMD abundant terminal functional groups can be simultaneously connected with a variety of selective targeting ligand, and then through the package or the role of chemical coupling drug or therapeutic gene load, and finally the drug and therapeutic gene to the lesion site to release Targeted therapy. The PAMAMD-based nano-targeted delivery system has the characteristics of smaller particle size, enhanced EPR effect and low toxicity. This review summarizes the progress in the application of PAMAMD with various targeted ligands and looks forward to future research directions.