Bile Acid Sequestrants Based on Natural and Synthetic Gels

Area of Science:

• Pharmacology
• Polymer Chemistry
• Biochemistry

Background:

• Bile acid sequestrants (BASs) are non-systemic agents for hypercholesterolemia management.
• They function by binding bile salts in the small intestine, preventing reabsorption and promoting excretion.
• BASs are generally recognized for their safety profile with minimal systemic adverse effects.

Purpose of the Study:

• To provide a comprehensive overview of bile acids and bile acid sequestrants.
• To detail the characteristics, mechanisms of action, and chemical structures of commercial and potential BASs.
• To explore the relationship between polymer structure and bile salt binding affinity.

Main Methods:

• Review of existing literature on bile acids and BASs.
• Analysis of chemical structures and synthesis methods for first- and second-generation BASs.
• Examination of novel BAS candidates, including synthetic polymers and biopolymers, and molecular imprinting polymers (MIPs).

Main Results:

• Commercial BASs include first-generation (cholestyramine, colextran, colestipol) and second-generation (colesevelam, colestilan).
• Potential BASs are based on diverse polymers like poly((meth)acrylates/acrylamides), cellulose, and cyclodextrins.
• Molecular imprinting polymers (MIPs) show high selectivity and affinity for bile salt binding.

Conclusions:

• Understanding the structure-activity relationship is crucial for developing effective BASs.
• Various synthetic and biopolymer-based BASs offer potential for hypercholesterolemia treatment.
• The review covers synthetic pathways and evaluates in vitro and in vivo hypolipidemic activities.