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Pardridge WM. Targeting Neurotherapeutic Agents Through the Blood-Brain Barrier. Arch Neurol. 2002;59(1):35–40. doi:10.1001/archneur.59.1.35
The blood-brain barrier (BBB) is maintained by the endothelial tight junctions within the brain microvasculature. Most small-molecule neuropharmaceutical agents and virtually all large-molecule drugs do not cross the BBB. The BBB problem is the rate-limiting factor preventing the transfer of progress in the molecular neurosciences to the development of clinically effective neurotherapeutic agents. The future development of neurotherapeutic agents will be accelerated by the development of BBB drug-targeting technology.
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