Ding Rong-min, He Hua, Li Juan
Department of Analytical Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Yao Xue Xue Bao. 2011 May;46(5):493-501.
Targeting drug delivery system (TDDS) is one of the most concerned research fields in cancer treatment because it can bind selectively and react with the target diseased sites at the cellular or sub-cellular level, making distribution and release of drugs in a controlled manner, thus enhance therapeutic effects and reduce toxic and side-effects on normal cells. Polyamidoamine dendrimer (PAMAMD) is a kind of newly developed polymer in nanometer degree. Hyper-branched, monodispersity, three-dimensional structure and host-guest entrapment ability make it used as drug carrier, gene delivery system and imaging agent. Various targeting ligands, which have high affinity to specific organs, tissues or cells in human body, can be linked to surface functional groups of PAMAMD. And drugs and theoretical gene are carried by encapsulation or chemical conjugation. Finally, PAMAMD targeting drug delivery system can carry drugs and theoretical gene to diseased sites and then release them for targeted therapy. The PAMAMD-based conjugates have small size, ligh permeability and retention effect (EPR), low toxicity and so on. The research progress of PAMAMD modified by different ligands in targeting drug delivery system is reviewed, and research direction of the PAMAMD targeting delivery system in the future is also suggested.
靶向给药系统（TDDS）是癌症治疗中最受关注的研究领域之一，因为它可以在细胞或亚细胞水平上与靶病变部位选择性结合并发生反应，以可控方式使药物分布和释放，从而提高治疗效果并减少对正常细胞的毒副作用。聚酰胺胺树枝状大分子（PAMAMD）是一种新开发的纳米级聚合物。超支化、单分散性、三维结构和主客体包封能力使其用作药物载体、基因递送系统和成像剂。各种对人体特定器官、组织或细胞具有高亲和力的靶向配体可与PAMAMD的表面官能团相连。药物和理论基因通过包封或化学偶联来携带。最后，PAMAMD靶向给药系统可将药物和理论基因携带至病变部位，然后释放它们进行靶向治疗。基于PAMAMD的缀合物具有尺寸小、光透过性和滞留效应（EPR）、低毒性等特点。综述了不同配体修饰的PAMAMD在靶向给药系统中的研究进展，并对PAMAMD靶向递送系统未来的研究方向提出了建议。
