Mimicking brain tissue binding in an in vitro model of the blood-brain barrier illustrates differences between in vitro and in vivo methods for assessing the rate of brain penetration

[Display omitted] •In vitro BBB does not predict permeability in vivo for highly lipophilic compounds.•In vitro BBB permeability does not account for brain tissue binding.•Glial cells could be use in vitro to mimic the influence of brain tissue binding.•New calculation method accounting for both BBB...

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Bibliographic Details
Published in:	European journal of pharmaceutics and biopharmaceutics Vol. 127; pp. 453 - 461
Main Authors:	Heymans, Marjolein, Sevin, Emmanuel, Gosselet, Fabien, Lundquist, Stefan, Culot, Maxime
Format:	Journal Article
Language:	English
Published:	Netherlands Elsevier B.V 01.06.2018 Elsevier
Subjects:	BBB permeability Blood-brain barrier Brain exposure Brain tissue binding Drug discovery Endothelial cells In vitro model In-situ brain perfusion Life Sciences Brain exposure PSf Pvivo BBB PS PSe bBCEC CNS Endothelial cells In-situ brain perfusion PSt Blood-brain barrier Papp MB Pe In vitro model Pvitro Drug discovery Brain tissue binding GC BBB permeability EC fu,br blood-brain barrier in vitro model endothelial cells drug discovery brain exposure brain tissue binding in-situ brain perfusion
ISSN:	0939-6411, 1873-3441, 1873-3441
Online Access:	Get full text
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