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.


CONCLUSIONS
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.
Adenot
M
M
Synt:em, Nîmes, Paris, France. marc.adenot@voila.fr
Merida
P
P
Lahana
R
R
D000595:Amino Acid Sequence; D000818:Animals; D001692:Biological Transport; D001812:Blood-Brain Barrier / Q000378:metabolism*; D002490:Central Nervous System / Q000378:metabolism*; D002491:Central Nervous System Agents / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008954:Models, Biological; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics*; D019151:Peptide Library; D011379:Prognosis; D051381:Rats
D002491:Central Nervous System Agents; D004337:Drug Carriers; D009842:Oligopeptides; D019151:Peptide Library; C501559:SynB3 peptide