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

Chemotherapy. 2007;53(1):73-6. doi: 10.1159/000098422. Epub 2007 Jan 3.

Abstract

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.

Publication types

  • Evaluation Study

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Biological Transport
  • Blood-Brain Barrier / metabolism*
  • Central Nervous System / metabolism*
  • Central Nervous System Agents / pharmacokinetics*
  • Drug Carriers / chemistry
  • Drug Carriers / pharmacokinetics*
  • Drug Evaluation, Preclinical
  • Humans
  • Models, Biological*
  • Molecular Sequence Data
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacokinetics*
  • Peptide Library
  • Prognosis
  • Rats

Substances

  • Central Nervous System Agents
  • Drug Carriers
  • Oligopeptides
  • Peptide Library
  • SynB3 peptide