Transporter-mediated drug delivery: recent progress and experimental approaches

Drug Discov Today. 2004 Aug 15;9(16):712-20. doi: 10.1016/S1359-6446(04)03198-8.


A comprehensive list of drug transporters has recently become available as a result of extensive genome analysis, as well as membrane physiology and molecular biology studies. This review covers recent progress in identification and characterization of drug transporters, illustrative cases of successful drug delivery to, or exclusion from, target organs via transporters, and novel experimental approaches to therapeutics using heterologously transduced transporters in tissues. We aim to provide clues that could lead to efficient strategies for the use of transporters to deliver drugs and/or to optimize lead compounds.

Publication types

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

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Drug Delivery Systems*
  • Humans
  • Membrane Transport Proteins / metabolism*
  • Organic Anion Transporters / metabolism
  • Organic Cation Transport Proteins / metabolism
  • Pharmaceutical Preparations / administration & dosage*
  • Pharmaceutical Preparations / metabolism*
  • Pharmacokinetics
  • Symporters / metabolism


  • ATP-Binding Cassette Transporters
  • Membrane Transport Proteins
  • Organic Anion Transporters
  • Organic Cation Transport Proteins
  • Pharmaceutical Preparations
  • Symporters