Abstract
The 2-(4-chlorophenoxy)-2-methylpropionic acid (CMP) salt of chitosan (CS), CS-CMP, and that of a CS derivative (CP), were prepared and their ability to adsorb bile acids investigated. CS-CMP and CP-CMP rapidly adsorbed taurocholate (TCA) and glycocholate (GCA) when these bile acids were present together in the medium, with simultaneous release of CMP. A secondary bile acid, taurodeoxycholate, was preferentially adsorbed over TCA and GCA. Alginate gel beads containing CS-CMP did not differ from CS-CMP alone in their manner of bile acids take up. Furthermore, oral administration of CS-CMP to rats resulted in decreased serum cholesterol and triacylglycerol levels for two weeks. Therefore, CS-CMP, as well as a vehicle containing CS-CMP, might be a useful agent with which to treat hyperlipidemia.
Highlights
Chitosan (CS) is an attractive agent for drug development given its function in the gastrointestinal tract and its intrinsic safety when taken orally
One mechanism by which CS might decrease cholesterol levels is by adsorption of bile acids (BAs) [6]
BAs are secreted in the gastrointestinal tract, primarily as glycine or taurine conjugates, after which secondary BAs, such as deoxycholate, are produced from primary BAs by intestinal microorganisms
Summary
Chitosan (CS) is an attractive agent for drug development given its function in the gastrointestinal tract and its intrinsic safety when taken orally. CS-CMP to rats resulted in decreased serum cholesterol and triacylglycerol levels for two weeks. One mechanism by which CS might decrease cholesterol levels is by adsorption of bile acids (BAs) [6]. Oral administration of an anion-exchange resin, such as cholestyramine, inhibits the enterohepatic circulation of BAs, thereby decreasing serum cholesterol levels [7].
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