Ready for Transfer

Methods for Improved Drug Delivery to the Central Nervous System

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Laboratory: National Institute of Environmental Health Sciences (NIEHS)

Technology: Methods for Improved Drug Delivery to the Central Nervous System (CNS) 

Opportunity: This novel NIEHS technology is available for licensing through the National Institutes of Health’s (NIH) Office of Technology Transfer.

Details: When using the tricyclic antidepressant amitriptyline, its bioactive metabolites, and other lysophosphatidic acid 1 receptor (LPA1R) activators, this invention demonstrated an improvement in the bioavailability and delivery of therapeutics to the CNS. When combined with other agents, amitriptyline could selectively decrease P-glycoprotein (P-gp) transport activity by ligand activation of LPA1R at the blood-brain barrier. 

Targeting P-gp as an effective method for increasing drug delivery to the brain CNS is positive for two main reasons:

  • Its substrates include a large portion of on-the-market drugs, including chemotherapeutics
  • Its directionality results in a net efflux of drugs from the brain.

Benefits: This technology’s ability to increase drug delivery to the CNS is beneficial in that improves overall drug efficacy during treatment.

Potential Applications:

  • Drug delivery to the CNS
  • Co-administration of therapeutics
  • Blood-brain barrier permeability.

Contact: For more information on this NIEHS available technology, contact Michael Shmilovich, J.D., at