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CNS Drug Design Based on Principles of Blood‐Brain Barrier Transport
Author(s) -
Pardridge William M.
Publication year - 1998
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1046/j.1471-4159.1998.70051781.x
Subject(s) - blood–brain barrier , drug , drug discovery , drug delivery , drug delivery to the brain , in vivo , pharmacology , chemistry , central nervous system , neuroscience , biology , medicine , biochemistry , microbiology and biotechnology , organic chemistry
Lipid‐soluble small molecules with a molecular mass under a 400–600‐Da threshold are transported readily through the blood‐brain barrier in vivo owing to lipid‐mediated transport. However, other small molecules lacking these particular molecular properties, antisense drugs, and peptide‐based pharmaceuticals generally undergo negligible transport through the blood‐brain barrier in pharmacologically significant amounts. Therefore, if present day CNS drug discovery programs are to avoid termination caused by negligible blood‐brain barrier transport, it is important to merge CNS drug discovery and CNS drug delivery as early as possible in the overall CNS drug development process. Strategies for special formulation that enable drug transport through the blood‐brain barrier arise from knowledge of the molecular and cellular biology of blood‐brain barrier transport processes.