Research progress in the application of bile acid-drug conjugates: A "trojan horse" strategy

Area of Science:

• Pharmacology
• Drug Delivery
• Biochemistry

Background:

• Bile acid transporters are crucial for drug uptake in intestinal cells and hepatocytes.
• Prodrug strategies using bile acids aim to improve oral bioavailability and cancer drug targeting.
• Bile acid-drug conjugates mimic natural bile acids for transporter recognition.

Purpose of the Study:

• To review recent advancements in bile acid-drug conjugate applications.
• To highlight the role of ASBT, NTCP, and OATP transporters in this strategy.
• To explore the potential of bile acid-drug conjugates in cancer therapy.

Main Methods:

• Conjugation of drugs to bile acids via covalent bonds.
• Utilizing bile acid transporters (ASBT, NTCP, OATP) for drug translocation.
• Reviewing existing literature on bile acid-drug conjugate applications.

Main Results:

• Bile acid-drug conjugates are effectively recognized and transported by specific bile acid transporters.
• This approach enhances cellular entry and exit of conjugated drugs.
• Demonstrated potential for improving oral bioavailability of various drugs.

Conclusions:

• Bile acid-drug conjugates represent a promising strategy for enhancing drug delivery and oral bioavailability.
• Targeting bile acid transporters offers a viable route for developing novel cancer therapeutics.
• Further research into bile acid-drug conjugates is warranted for broader pharmaceutical applications.