
Molecular determinants of blood–brain barrier permeation
Author(s) -
Werner J. Geldenhuys,
Afroz S. Mohammad,
Chris E. Adkins,
Paul R. Lockman
Publication year - 2015
Publication title -
therapeutic delivery
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.619
H-Index - 46
eISSN - 2041-6008
pISSN - 2041-5990
DOI - 10.4155/tde.15.32
Subject(s) - blood–brain barrier , permeation , chemistry , medicine , central nervous system , biochemistry , membrane
The blood-brain barrier (BBB) is a microvascular unit which selectively regulates the permeability of drugs to the brain. With the rise in CNS drug targets and diseases, there is a need to be able to accurately predict a priori which compounds in a company database should be pursued for favorable properties. In this review, we will explore the different computational tools available today, as well as underpin these to the experimental methods used to determine BBB permeability. These include in vitro models and the in vivo models that yield the dataset we use to generate predictive models. Understanding of how these models were experimentally derived determines our accurate and predicted use for determining a balance between activity and BBB distribution.