Institute of Organic Chemistry, Johannes Gutenberg-University Mainz, Duesbergweg 10-15, 55128, Mainz, Germany.
Macromol Biosci. 2014 May;14(5):607-18. doi: 10.1002/mabi.201400028. Epub 2014 Mar 19.
Poly[N-(2-hydroxypropyl) methacrylamide] (HPMA) was one of the first polymers applied as polymer drug conjugate in the clinics. Since then many attempts have been made to expand the functionality of HPMA-based copolymers from advanced synthetic pathways to multiple biomedical applications. This Feature Article highlights multifunctional HPMA based copolymers prepared by controlled radical polymerization and subsequent post-polymerization modification of activated ester precursor polymers via aminolysis. This approach combines precise control of the polymer's microstructure (molecular weight, dispersity, block copolymer formation, end group functionalization) with an easy introduction of various multifunctional groups. The obtained polymers can be used as versatile targeted drug carriers for sophisticated molecular imaging techniques that provide detailed information about structure property relationships both in vitro as well as in vivo. Moreover, recent studies have shown that such multifunctional HPMA copolymers may have high potential as advanced carriers in the field of tumor immunotherapy.
聚[N-(2-羟丙基)甲基丙烯酰胺]（HPMA）是最早应用于临床的聚合物药物偶联物之一。从那时起，人们尝试通过先进的合成途径和多种生物医学应用，来拓展基于 HPMA 的共聚物的功能。本文重点介绍了通过可控自由基聚合以及随后通过氨解对活化酯前体聚合物进行后聚合修饰制备的多功能 HPMA 共聚物。这种方法结合了聚合物微观结构（分子量、分散度、嵌段共聚物形成、端基官能化）的精确控制与各种多功能基团的简便引入。所得聚合物可用作多功能靶向药物载体，适用于复杂的分子成像技术，这些技术可提供关于体外和体内结构-性能关系的详细信息。此外，最近的研究表明，这种多功能 HPMA 共聚物可能具有作为肿瘤免疫治疗领域中高级载体的巨大潜力。
