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Abstract: Polymeric bile acid sequestrants have received increasing attention as therapeutic agents for the treatment of hypercholesterolemia. These materials are usually cationic hydrogels that selectively bind and remove bile acid molecules from the gastrointestinal tract, decreasing plasma cholesterol levels. Due to their high molecular weight, the action of bile acid sequestrants can be limited to the gastrointestinal tract, avoiding systemic exposure, which constitutes an advantage over conventional small-molecule drugs. Different polymers, such as vinyl polymers, acrylic polymers and allyl polymers have been used to prepare potential bile acid sequestrants based on conventional polymerization techniques. Also, much effort has been devoted to understanding the structure-property relationships between these polymers and their ability to bind bile acid molecules. The efficacy of these polymeric drugs can be ascribed to five major variables: (i) the density of cationic charges, (ii) the length and distribution of the hydrophobic chains, (iii) the polymer backbone flexibility, (iv) the degree of cross-linking and (v) the polymer shape. This review summarizes the major synthesis pathways that are employed in the preparation of this type of polymer therapeutics and the polymer structural key factors that are of relevance to enhanced therapeutic efficacy. Herein, new synthesis approaches, based on ''controlled''/living radical polymerization techniques, are highlighted
Template and target information: Review - polymeric bile acid sequestrants
Author keywords: Bile acid sequestrants, living radical polymerization, cholesterol, drug discovery, polymers