Identification of Peptide Ligands for Targeting to the Blood-Brain Barrier.

I. van Rooy
S. Cakir-Tascioglu
G. Storm
W. E. Hennink
R. M. Schiffelers
E. Mastrobattista
Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, 3584 CA, Utrecht, The Netherlands,

The technique of phage display was used in a murine brain perfusion model, to screen for new brain endothelium peptide ligands. Two selected phage clones showed affinity for human brain endothelium in vitro (hCMEC/D3). This affinity was not seen for other humanendothelial cells (HUVEC). When the selected phage were individually perfused through the murine brain, their brain affinity was 5 to 6-fold higher compared to a random control phage. 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.