Research Progress In The Application Of Bile Acid-Drug Conjugates: A "Trojan Horse" Strategy

Bile acid transporters are highly expressed in intestinal cells and hepatocytes, and they determine the uptake of drugs in cells by modulating cellular entry and exit. In order to improve the oral bioavailability of drugs and investigate the potential application prospects of drugs used to target cancer, numerous studies have adopted these transporters to identify prodrug strategies. Through the connection of covalent bonds between drugs and bile acids, the resulting bile acid-drug conjugates continue to be recognized as similar to natural unmodified bile acid and is translocated by the transporter. The present mini-review provides a brief summary of recent progress of the application of bile acid-drug conjugates based primarily on ASBT, NTCP, and OATP, with the hope of contributing to subsequent research.