Pang Xin, Du Hong-Liang, Zhang Hai-Qun, Zhai Ying-Jie, Zhai Guang-Xi
College of Pharmaceutical Sciences, Shandong University, Jinan 250012, China.
Drug Discov Today. 2013 Dec;18(23-24):1316-22. doi: 10.1016/j.drudis.2013.09.007. Epub 2013 Sep 17.
Polymer conjugation is an efficient approach to improve therapeutic properties of drugs and biological agents. Since the first synthetic polymer-drug conjugate entered clinical trials in 1994, this technology has undergone notable development for the introduction and study of novel polymers and for the progress in the biological rationale for designing conjugates. Not surprisingly, new polymers, in addition to the best known polyethylene glycol, poly[N-(2-hydroxypropyl)methacrylamide], are continuously conjugated with drugs to achieve biodegradable, stimuli-sensitive and targeted systems in an attempt to prolong blood circulation times and enhance drug concentrations at the intended site of action. This overview focuses on bioconjugates of water-soluble polymers with low molecular weight drugs. Additionally, the most recent achievements in the polymer-drug conjugate field and several promising approaches for the future are discussed.
聚合物偶联是改善药物和生物制剂治疗特性的有效方法。自1994年首个合成聚合物-药物偶联物进入临床试验以来,这项技术在新型聚合物的引入和研究以及偶联物设计的生物学原理方面取得了显著进展。毫不奇怪,除了最知名的聚乙二醇、聚[N-(2-羟丙基)甲基丙烯酰胺]之外,新的聚合物不断与药物偶联,以实现可生物降解、刺激敏感和靶向系统,试图延长血液循环时间并提高药物在预期作用部位的浓度。本综述重点关注水溶性聚合物与低分子量药物的生物偶联物。此外,还讨论了聚合物-药物偶联领域的最新成果以及未来几种有前景的方法。