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Updated: Jun 16, 2026
Setting-up an In Vitro Model of Rat Blood-brain Barrier (BBB): A Focus on BBB Impermeability and Receptor-mediated Transport
Published on: June 28, 2014
Identification of peptide ligands for targeting to the blood-brain barrier
Inge van Rooy1, Serpil Cakir-Tascioglu, Pierre-Olivier Couraud
1Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082, 3508 TB, Utrecht, The Netherlands. i.vanrooy@uu.nl
Purpose:
Transport of drugs to the brain is limited by the blood-brain barrier. New, specific brain endothelium ligands can facilitate brain-specific delivery of drugs.
Methods:
We used phage display in an in situ brain perfusion model to screen for new brain endothelium peptide ligands.
Results:
Two phage clones, displaying 15 amino acid-peptides (GLA and GYR) that were selected for brain binding in the mouse model, showed significant binding to human brain endothelium (hCMEC/D3), compared to a random control phage. This binding was not seen for other human endothelial cells (HUVEC). Binding to hCMEC/D3 cells was dose dependent. When phage GLA and GYR were individually perfused through the murine brain, their ability to bind to the brain was 6-fold (GLA) and 5-fold (GYR) higher than the control phage. When compared to lung perfusion, phage showed an 8.5-fold (GYR) and 48-fold (GLA) preference for brain over lung compared to the control.
Conclusions:
These results indicate that two new peptide ligands have been identified that may be used for specific targeting of drugs to the blood-brain barrier.
