The Blood-brain barrier (BBB) protects the brain from harmful substances in the blood by restricting their entries. On the other hand, the barrier also prevents most therapeutic agents from reaching the brain leading to ineffectiveness of these therapeutics in treating brain diseases. Various strategies have been made to improve the delivery of therapeutic agents to the brain for the treatment of brain diseases. The BBB is featured with various receptors and transporters. The ligands of some of these transporters and receptors have been exploited for brain-targeting delivery. Glutathione (GSH) is a three amino acid peptide and endogenous antioxidant. GSH enters the brain through the GSH transporter that is enriched in the BBB. GSH has been successfully used as a brain-targeting ligand in brain delivery nanoparticles. GUNW-3, a GSH-based derivative, has been confirmed to be an effective brain-targeting agent from our laboratory. This study was aimed to investigate how effective GUNW-3 could help deliver liposomes and micelles encapsulated with tamoxifen to the brain. The preparation and characterization of GUNW-3 liposomes and GUNW-3 micelles encapsulated with tamoxifen will be presented. The in vivo studies with mice demonstrating both GUNW-3 liposomes and GUNW-3 micelles significantly increased the brain delivery of tamoxifen will be reported as well.

GUNW-3 as a brain-targeting agent to improve the delivery of tamoxifen to the brain

2019 Fall National Meeting

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