聚合物-药物偶联物治疗学：进展、见解与展望。

Polymer-drug conjugate therapeutics: advances, insights and prospects.

机构信息

Departments of Biomedical Engineering, Chemistry, and Medicine, Boston University, Boston, MA, USA.

Department of Surgery, Brigham and Women's Hospital, Boston, MA, USA.

出版信息

Nat Rev Drug Discov. 2019 Apr;18(4):273-294. doi: 10.1038/s41573-018-0005-0.

DOI:10.1038/s41573-018-0005-0

PMID:30542076

Abstract

Polymer-drug conjugates have long been a mainstay of the drug delivery field, with several conjugates successfully translated into clinical practice. The conjugation of therapeutic agents to polymeric carriers, such as polyethylene glycol, offers several advantages, including improved drug solubilization, prolonged circulation, reduced immunogenicity, controlled release and enhanced safety. In this Review, we discuss the rational design, physicochemical characteristics and recent advances in the development of different classes of polymer-drug conjugates, including polymer-protein and polymer-small-molecule drug conjugates, dendrimers, polymer nanoparticles and multifunctional systems. Current obstacles hampering the clinical translation of polymer-drug conjugate therapeutics and future prospects are also presented.

摘要

聚合物-药物偶联物在药物输送领域一直是主要研究方向，已有几种偶联物成功转化为临床实践。将治疗剂与聚合物载体（如聚乙二醇）偶联具有许多优点，包括提高药物溶解度、延长循环时间、降低免疫原性、控制释放和提高安全性。在这篇综述中，我们讨论了不同类型的聚合物-药物偶联物的合理设计、物理化学特性和最新进展，包括聚合物-蛋白质和聚合物-小分子药物偶联物、树枝状大分子、聚合物纳米粒子和多功能系统。还介绍了当前阻碍聚合物-药物偶联物治疗剂临床转化的障碍和未来展望。