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1Department of Pharmaceutical Sciences, College of Pharmacy, 986025 Nebraska Medical Center, 68198-6025, Omaha NE, USA
Pharmaceutical Science & Technology Today
|October 26, 2000
Summary
P-glycoprotein and multidrug resistance-associated protein transporters are key components of the blood-brain barrier. These transporters act as a crucial defense mechanism, limiting drug entry into the brain.
Area of Science:
- Neuroscience
- Pharmacology
- Cell Biology
Background:
- The blood-brain barrier (BBB) protects the central nervous system from harmful substances.
- Efflux transporters like P-glycoprotein (P-gp) and multidrug resistance-associated proteins (MRPs) are highly expressed at the BBB.
- These transporters actively pump xenobiotics out of brain endothelial cells, limiting drug penetration.
Purpose of the Study:
- To review the role of P-gp and MRPs in the BBB.
- To highlight their significance in multidrug resistance.
- To discuss their impact on drug delivery to the brain.
Main Methods:
- Literature review and synthesis of existing research.
- Analysis of transporter expression and function at the BBB.
- Discussion of clinical implications for drug development.
Main Results:
- P-gp and MRPs are major determinants of drug disposition in the brain.
- Their activity contributes to therapeutic failures in central nervous system diseases.
- Understanding these transporters is crucial for designing effective brain-penetrant drugs.
Conclusions:
- P-gp and MRPs represent significant barriers to drug delivery across the BBB.
- Targeting these efflux transporters offers a potential strategy to enhance CNS drug efficacy.
- Further research is needed to fully elucidate their complex roles in neurological disorders.