Therapeutic potential of bile acids and synthetic strategies of their incorporation into polymeric drug delivery systems

Abstract

Recently, lipid–polymer nanoparticles incorporating bile acids (BAs) have garnered significant interest in drug delivery research. Due to their amphiphilic nature, self-assembling properties, and steroid skeleton, BAs can serve as both drug-solubilizing and membrane-penetrating agents, facilitating drug transport across cell membranes. BAs exhibit diverse bioactivities, including anticancer, antimicrobial, and immunomodulatory effects, which further increase their potential for therapeutic applications. Their carboxyl and hydroxyl functional groups allow for easy derivatization, enabling the synthesis of a wide range of BA-based (macro)molecules. Introducing BAs into polymer systems leads to stable and biocompatible nanocarriers with high affinity to cell membranes, enabling the encapsulation, delivery, and controlled release of bioactive molecules. This review provides a comprehensive overview of polymers containing bile acids (BAs) as drug delivery vehicles. We first explore the biological roles and therapeutic potential of BAs. This is followed by a discussion of the synthetic strategies used to prepare polymers containing bile acid moieties. Finally, we assess the advantages and key challenges that will shape the future development of polymeric BA-based drug delivery systems.