title: Utilizing bile acid carrier mechanisms to enhance liver and small intestine absorption.
abstract: On the basis of the enterohepatocycling phenomenon of bile acids involving the intestines, liver, and gallbladder, it was conceptualized that bile acids could serve as a molecular carrier of drugs by taking advantage of the bile acid active transport mechanism. It was further proposed that derivatization or analogation of bile acids at the C3-OH position was the desired route because of the reactive hydroxyl group and, moreover, because of the active transport requirement of retaining the C17 side chain with a single terminal acidic function. Using 3-tosylcholic, 3-benzoylcholic, and 3-iodocholic acids, in situ liver absorption, biliary excretion, and intestinal absorption studies in the rat were successful in establishing the concept that C3-derivatives and analogs of bile acids are, potentially, novel molecular delivery systems for intestinal and liver-site directed absorption.
mesh_terms: D000465:Algorithms; D000818:Animals; D001647:Bile Acids and Salts / Q000378:metabolism*; D001693:Biological Transport, Active; D002793:Cholic Acids / Q000493:pharmacokinetics; D004337:Drug Carriers; D007408:Intestinal Absorption / Q000187:drug effects*; D007421:Intestine, Small / Q000378:metabolism*; D008099:Liver / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D013388:Succinimides
chemical_list: C055215:3-tosylcholic acid; D001647:Bile Acids and Salts; D002793:Cholic Acids; D004337:Drug Carriers; D013388:Succinimides; C051109:3-benzyl-N-(methanesulfonyloxy)succinimide; C055214:3-benzoylcholic acid; C055216:3-iodocholic acid