Institute of Chemistry and Biochemistry, Freie Universität Berlin, Takustr. 3, 14195, Berlin, Germany.
Angew Chem Int Ed Engl. 2022 Dec 5;61(49):e202203942. doi: 10.1002/anie.202203942. Epub 2022 Oct 26.
Poor water solubility and low bioavailability of active pharmaceutical ingredients (APIs) are major causes of friction in the pharmaceutical industry and represent a formidable hurdle for pharmaceutical drug development. Drug delivery remains the major challenge for the application of new small-molecule drugs as well as biopharmaceuticals. The three challenges for synthetic delivery systems are: (i) controlling drug distribution and clearance in the blood; (ii) solubilizing poorly water-soluble agents, and (iii) selectively targeting specific tissues. Although several polymer-based systems have addressed the first two demands and have been translated into clinical practice, no targeted synthetic drug delivery system has reached the market. This Review is designed to provide a background on the challenges and requirements for the design and translation of new polymer-based delivery systems. This report will focus on chemical approaches to drug delivery for systemic applications.
药物活性成分(APIs)的水溶性差和生物利用度低是制药行业的主要难题,也是药物开发的巨大障碍。药物传递仍然是新小分子药物和生物制药应用的主要挑战。合成传递系统面临的三个挑战是:(i)控制药物在血液中的分布和清除;(ii)增溶疏水性差的药物;(iii)选择性靶向特定组织。尽管有几种基于聚合物的系统已经满足了前两个需求,并已转化为临床实践,但没有靶向合成药物传递系统进入市场。本综述旨在为新的基于聚合物的传递系统的设计和转化提供背景知识,重点介绍用于全身应用的化学药物传递方法。