Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, 211198, People's Republic of China.
The Joint Laboratory of China Pharmaceutical University and Taian City Central Hospital, Taian City Central Hospital, Taian, 271000, China and Taian City institute of Digestive Disease, Taian City Central Hospital, Taian, 271000, China.
Biomater Sci. 2021 May 18;9(10):3621-3637. doi: 10.1039/d0bm02221g.
Short half-life is one of the main causes of drug attrition in clinical development, which also leads to the failure of many leading compounds and hits to become drug candidates. Nowadays, nanomaterials have been applied to drug development to address this problem. In fact, the clinical application of nanoparticles (NPs) is severely limited due to their rapid elimination by the reticuloendothelial system (RES) in vivo. In this paper, we aim to summarize representative strategies on prolonging the circulation time for bridging the gap between excellent pharmaceutics and proper half-life and encourage clinical translation.
半衰期短是临床开发中药物淘汰的主要原因之一,这也导致许多先导化合物和命中化合物无法成为候选药物。如今,纳米材料已被应用于药物开发以解决这个问题。事实上,由于纳米粒子(NPs)在体内会被网状内皮系统(RES)迅速清除,其临床应用受到严重限制。本文旨在总结延长循环时间的代表性策略,以弥合优秀药剂学和适当半衰期之间的差距,并鼓励临床转化。