TY - JOUR
T1 - Drug delivery to the brain utilizing blood-brain barrier transport systems
AU - Terasaki, Tetsuya
AU - Tsuji, Akira
N1 - Funding Information:
This researchw ass upportedi n part by a Grant-in-Aid from the Ministry of Education, Sciences and Culture, Japan, the project Research Fund from the GraduateS chool of Natural Sciencea nd Technology, Kanazawa University, the Takeda Science Foundation, the Naito foundation, the Tokyo Biochemical Research Foundation, the Mochida Memorial Foundation for Medical and PharmaceuticalR esearcha nd the Uehara Memorial Foundation.
PY - 1994/2
Y1 - 1994/2
N2 - 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.
AB - 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.
KW - Absorptive-mediated endocytosis
KW - Blood-brain barrier
KW - Carrier-mediated transport
KW - Drug delivery
KW - Peptide drug
KW - Receptor-mediated endocytosis
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U2 - 10.1016/0168-3659(94)90132-5
DO - 10.1016/0168-3659(94)90132-5
M3 - Article
AN - SCOPUS:0028344380
SN - 0168-3659
VL - 29
SP - 163
EP - 169
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 1-2
ER -