Applications of a blood-brain barrier technology platform to predict CNS penetration of various chemotherapeutic agents. 2. Cationic peptide vectors for brain delivery.

Background: SynB family peptides conjugated to several drugs have been shown to increase the brain uptake and in vivo activities of these drugs via an adsorptive-mediated transcytosis mechanism. Based on both in vivo and in vitro experimental data, a cell uptake component has been added to our computational model of blood-brain barrier.

Methods: In situ brain perfusion, in vitro cell model and a computational cell uptake model have been used to discover brain-penetrating properties of SynB peptides and to screen libraries of new rationally designed peptide vectors suitable for brain drug delivery.

Results And Conclusion: Starting from small peptide vectors that enhance the brain transport coefficient, the BBB platform has made it possible to design libraries of peptide vectors with enhanced transport properties.