Improving Drug Delivery to the Brain

  • Author: Melania Tesio
  • Published: 20 September 2012
  • Copyright: Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
  • Source / Publisher: Proceedings of the National Academy of Sciences/National Academy of Sciences
thumbnail image: Improving Drug Delivery to the Brain

The blood-brain barrier separates the blood from the extracellular fluids of the brain. It consists of a capillary endothelium endowed with drug efflux pumps such as P-glycoprotein. By transporting compounds out of the brain, this molecule represents a major obstacle to deliver therapeutic drugs to this organ.

Ronald E. Cannon, National Institute of Health, USA, and colleagues identified a signaling pathway which can pharmacologically target P-glycoprotein. The scientists discovered that the activity of the pump is reduced by the sphingolipid sphingosine-1-phosphate (S1P). As a consequence, when they delivered to rats S1P or its therapeutic analogs (FTY720 and FTY720P), they could rapidly and reversibly inhibit P-glycoprotein and, therefore, increase the uptake of the transporter’s substrates.

Sphingolipid-based drugs could, therefore, be useful to improve drug delivery across the blood brain barrier.

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