School of Chemistry, The University of New South Wales (UNSW), Sydney, NSW 2052, Australia.
Molecules. 2024 Oct 19;29(20):4949. doi: 10.3390/molecules29204949.
Covalent drugs can offer significant advantages over non-covalent drugs in terms of pharmacodynamics (i.e., target-binding properties). However, the development of covalent drugs is sometimes hampered by pharmacokinetic limitations (e.g., low bioavailability, rapid metabolism and toxicity due to off-target binding). Polymeric nanoparticles offer a potential solution to these limitations. Delivering covalent drugs via polymeric nanoparticles provides myriad benefits in terms of drug solubility, permeability, lifetime, selectivity, controlled release and the opportunity for synergistic administration alongside other drugs. In this short review, we examine each of these benefits in turn, illustrated through multiple case studies.
共价药物在药效学（即靶标结合特性）方面相对于非共价药物具有显著优势。然而，共价药物的开发有时受到药代动力学限制（例如，由于非靶标结合导致生物利用度低、代谢和毒性快）的阻碍。聚合物纳米粒子为这些限制提供了潜在的解决方案。通过聚合物纳米粒子递送共价药物在药物溶解度、渗透性、寿命、选择性、控制释放以及与其他药物联合使用的协同给药方面提供了多种益处。在这篇简短的综述中，我们依次检查了这些益处，通过多个案例研究进行了说明。
