Blood-brain barrier drug targeting: the future of brain drug development

Mol Interv. 2003 Mar;3(2):90-105, 51. doi: 10.1124/mi.3.2.90.


As human longevity increases, the likelihood of the onset of diseases of the brain (and other organs) also increases. Clinical therapeutics offer useful long-term treatments, if not cures, if drugs can be delivered appropriately and effectively. Unfortunately, research in drug transport to the brain has not advanced very far. Through better characterization of the transport systems utilized within the blood-brain barrier, a greater understanding of how to exploit these systems will lead to effective treatments for brain disorders. Pardridge reviews the functions of the various known transport systems in the brain and discusses how the development of BBB drug-targeting programs in pharmaceutical and academic settings may lead to more efficacious treatments.

Publication types

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

MeSH terms

  • Animals
  • Biological Transport
  • Blood-Brain Barrier / drug effects*
  • Brain Neoplasms / therapy
  • Carrier Proteins
  • Drug Administration Routes
  • Drug Delivery Systems / methods
  • Drug Design
  • Drug Industry / trends*
  • Genetic Therapy / methods
  • Humans
  • Lipid Metabolism
  • Molecular Weight
  • Parkinson Disease / therapy
  • Primates
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Zidovudine / pharmacokinetics


  • Carrier Proteins
  • Recombinant Proteins
  • Zidovudine