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聚合物-药物偶联物:最新进展和未来展望。

Polymer-drug conjugates: recent advances and future perspectives.

机构信息

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, India.

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, India.

出版信息

Drug Discov Today. 2020 Sep;25(9):1718-1726. doi: 10.1016/j.drudis.2020.06.028. Epub 2020 Jul 3.

DOI:10.1016/j.drudis.2020.06.028
PMID:32629170
Abstract

Polymer-drug conjugates (PDC) have exhibited clinical and commercial success in the field of drug delivery. A polymeric backbone, linker, targeting moiety, and drug constitute the building blocks of PDCs. Current attention is focusing on natural polymeric carriers, in particular the concept of graft copolymers, such as a combination of polymers and polysaccharides, to explore dual benefits such as combined vehicles and targeting moieties. Polymer heterogeneity, synthesis of PDCs, broad molecular weight distribution, conjugate variability, immunogenicity of polymers, safety, stability, and stringent regulatory approval are the major obstacles to the successful transition of PDCs to the clinic. In this review, we discuss natural and synthetic PDCs combined with computational modeling for diverse pharmaceutical and biomedical applications.

摘要

聚合物-药物偶联物(PDC)在药物输送领域已经取得了临床和商业上的成功。聚合物主链、连接子、靶向部分和药物构成了 PDC 的构建块。目前的注意力集中在天然聚合物载体上,特别是接枝共聚物的概念,如聚合物和多糖的组合,以探索联合载体和靶向部分的双重优势。聚合物异质性、PDC 的合成、广泛的分子量分布、缀合物变异性、聚合物的免疫原性、安全性、稳定性和严格的监管审批是 PDC 成功向临床转化的主要障碍。在这篇综述中,我们讨论了天然和合成的 PDC 与计算建模相结合,用于各种药物和生物医学应用。

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