Drug delivery to the brain utilizing blood-brain barrier transport systems

Tetsuya Terasaki, Akira Tsuji

Research output: Contribution to journalArticlepeer-review

27 Citations (Scopus)


The importance of the blood-brain barrier (BBB) transport system in drug delivery to the brain has been discussed. Carrier-mediated transport systems of monocarboxylic acid, amine and neutral amino acid at the BBB could be utilized as pathways for acidic, basic and amphoteric drug delivery, respectively. For peptide drug delivery, the transcytosis system would be a useful pathway. Especially by introducing the basic amino acids, arginine and lysine, to the peptide molecule, the possibilities of electrostatic interaction between the positively charged moiety of the peptide and the negatively charged region of the surface of the brain capillaries would be increased, resulting in the facilitation of an absorptive-mediated transcytosis. Further understanding of the various transport systems of nutrients and drugs among the BBB and peripheral organs would help provide more rational strategies for the brain-specific drug delivery design.

Original languageEnglish
Pages (from-to)163-169
Number of pages7
JournalJournal of Controlled Release
Issue number1-2
Publication statusPublished - 1994 Feb
Externally publishedYes


  • Absorptive-mediated endocytosis
  • Blood-brain barrier
  • Carrier-mediated transport
  • Drug delivery
  • Peptide drug
  • Receptor-mediated endocytosis

ASJC Scopus subject areas

  • Pharmaceutical Science


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