Prediction of blood–brain barrier permeation in drug discovery from in vivo, in vitro and in silico models

Abbott, N. Joan

doi:10.1016/j.ddtec.2004.11.014

Cited by 181Barrier Structure and Function StudiesDrug Transport and Resistance MechanismsComputational Drug Discovery Methods

Prediction of blood–brain barrier permeation in drug discovery from in vivo, in vitro and in silico models

Abbott, N. Joan·2004·Drug Discovery Today: Technologies

DOI 10.1016/j.ddtec.2004.11.014

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Abstract

The properties of the blood-brain barrier (BBB) are important considerations when designing drugs to target or avoid the brain. In vivo models provide some of the most reliable measurements of BBB drug permeability, whereas several new cell-based in vitro technologies give valuable mechanistic insights. Higher throughout methods (cell- and non-cell-based; in silico modelling) can help in prediction of permeation, but a combination of techniques is still required to cover the range of BBB drug entry and efflux mechanisms.:

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This typically results in higher penetrability by lipophilic compounds through the blood-brain barrier.
“This typically results in higher penetrability by lipophilic compounds through the BBB [46].”
From Polyphenol Microbial Metabolites Exhibit Gut and Blood–Brain Barrier Permeability and Protect Murine Microglia against LPS-Induced Inflammation (2019) · cites this paper as [46]
While many other factors contribute to blood-brain barrier permeability, such as plasma concentration, plasma binding, and metabolic modifications by barrier enzymes, PAMPA is a good predictor of passive movement across the blood-brain barrier.
“While there are many other factors that contribute to BBB permeability, such as plasma concentration, plasma binding, and metabolic modifications by barrier enzymes, PAMPA is a good predictor of passive movement across the BBB [35,46].”
From Polyphenol Microbial Metabolites Exhibit Gut and Blood–Brain Barrier Permeability and Protect Murine Microglia against LPS-Induced Inflammation (2019) · cites this paper as [46]

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Authors: Abbott, N. J.
Affiliations: King's College London (GB)
Corresponding author: Abbott, N. Joan
ORCID: Abbott, N. Joan
Venue: Drug Discovery Today: Technologies
Publisher: Elsevier BV
Published: 2004-12
Volume: 1
Issue: 4
Pages: 407-416
ISSN: 1740-6749 (ISSN-L)
DOI: 10.1016/j.ddtec.2004.11.014
OpenAlex: W1984360588
Cited by: 181
References: 45
Citations by year: 2026: 3 · 2025: 5 · 2024: 11 · 2023: 7 · 2022: 11 · 2021: 8 · 2020: 10 · 2019: 10 · 2018: 10 · 2017: 15 · 2016: 10 · 2015: 5 · 2014: 12 · 2013: 12 · 2012: 9
FWCI: 2.59
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Drug Discovery Today Technologies (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
Keywords: blood-brain barrier, drug permeation, BBB permeability prediction, in vivo models, in vitro BBB model, in silico modeling

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Prediction of blood–brain barrier permeation in drug discovery from in vivo, in vitro and in silico models

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