多聚N-(2-羟丙基)甲基丙烯酰胺-抗肿瘤药物偶合物的研究进展

N-(2-hydroxypropyl)methacrylamide copolymer-anticancer drugs:research advances

大分子聚合物-抗肿瘤药物偶合物能利用增强渗透和滞留效应将抗肿瘤药物-偶合物选择性投放于肿瘤组织,从而提高抗肿瘤药物在肿瘤组织的浓度,减少药物的系统毒性。多聚N-(2-羟丙基)甲基丙烯酰胺(HPMA)作为大分子载体具有许多优点,如生物相容性、非免疫原性等,因此多聚HPMA-抗肿瘤药物偶合物成为当前大分子靶向抗肿瘤药物研究的热点之一。目前进入临床的偶合物有6种,还有许多处于临床前研究。本文综述多聚HPMA-抗肿瘤药物偶合物研究的进展。

The conjugates of polymer with anticancer drug,due to their enhanced permeability and retention effect can accumulate in solid tumors at a much higher concentration than in normal tissues or organs,which results in higher targeting distribution and lower systemic toxicity. As a macromolecule carrier,N-（2-hydroxypropyl）methacrylamide （HPMA） copolymer has many advantages,such as biocompatibility and nonimmunogenicity,so HPMA copolymer-anticancer conjugates has become the focus of large-weight-molecule targeted therapies. Now six HPMA copolymer-anticancer drugs have been evaluated clinically,and many other conjugates are in the stage of preclinical tests. In this paper,research advances in HPMA copolymer-anticancer conjugates are reviewed.