Carrier-mediated intestinal transport of drugs

Pharm Res. 1996 Jul;13(7):963-77. doi: 10.1023/a:1016086003070.


Recent advances in the field of carrier-mediated intestinal absorption of of amino acids, oligopeptides, monosaccharides, monocarboxylic acids, phosphate, bile acids and several water-soluble vitamins across brush-border and basolateral membranes are summarized. An understanding of the molecular and functional characteristics of the intestinal membrane transporters will be helpful in the utilization of these transporters for the enhanced oral delivery of poorly absorbed drugs. Some successful examples of the synthesis of prodrugs recognized by the targeted transporters are described. Functional expression of the multidrug resistance gene product, P-glycoprotein, as a primary active transporter in the intestinal brush-border membrane leads to net secretion of some drugs such as anticancer agents in the blood-to-luminal direction, serving as a secretory detoxifying mechanism and as a part of the absorption barrier in the intestine.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / physiology
  • Amino Acids / metabolism
  • Animals
  • Bile Acids and Salts / metabolism
  • Biological Transport, Active / physiology
  • Carbohydrate Metabolism
  • Carboxylic Acids / metabolism
  • Drug Carriers / metabolism*
  • Humans
  • Intestinal Absorption*
  • Oligopeptides / metabolism
  • Pharmaceutical Preparations / metabolism*
  • Phosphates / metabolism
  • Vitamins / metabolism


  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Amino Acids
  • Bile Acids and Salts
  • Carboxylic Acids
  • Drug Carriers
  • Oligopeptides
  • Pharmaceutical Preparations
  • Phosphates
  • Vitamins