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Related Concept Videos

The Blood-brain Barrier00:49

The Blood-brain Barrier

Overview
Physiological Barriers01:25

Physiological Barriers

Physiological barriers are semi-permeable cellular structures restricting drug diffusion into intracellular compartments and tissues. There are six types of physiological barriers: blood endothelial, cell membrane, blood-brain, blood-cerebrospinal fluid (CSF), blood-placenta, and blood-testis barriers.
The blood endothelial barrier is the most porous of these. It allows all small ionized, un-ionized, and lipophilic molecules to pass through the endothelial lining into the interstitial space...

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Updated: Jul 10, 2026

An In Vivo Blood-brain Barrier Permeability Assay in Mice Using Fluorescently Labeled Tracers
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Challenges for blood-brain barrier (BBB) screening.

P Jeffrey1, S G Summerfield

  • 1Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, Harlow, UK.

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
|October 31, 2007
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Summary

Achieving effective central nervous system drug delivery requires balancing blood-brain barrier permeability with efflux and physicochemical properties. An integrated approach improves understanding of drug disposition beyond simple brain-blood ratios.

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Last Updated: Jul 10, 2026

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09:35

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A Human Blood-Brain Interface Model to Study Barrier Crossings by Pathogens or Medicines and Their Interactions with the Brain
07:52

A Human Blood-Brain Interface Model to Study Barrier Crossings by Pathogens or Medicines and Their Interactions with the Brain

Published on: April 9, 2019

Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Discovery

Background:

  • Blood-brain barrier (BBB) permeability is crucial for central nervous system (CNS) drug efficacy.
  • Traditional methods often isolate BBB permeability, neglecting other critical factors.
  • An integrated approach is needed to optimize CNS drug penetration.

Purpose of the Study:

  • To highlight the necessity of an integrated approach for CNS drug penetration.
  • To emphasize the combined roles of permeability, efflux, and physicochemical properties.
  • To move beyond arbitrary brain-blood ratio metrics for CNS drug assessment.

Main Methods:

  • Integrating data from permeability studies with P-glycoprotein efflux assessments.
  • Measuring drug-free fractions in both blood and brain tissue.
  • Analyzing the impact of physicochemical properties on CNS drug disposition.

Main Results:

  • An integrated approach provides a more comprehensive understanding of BBB impact on CNS uptake.
  • Physicochemical properties significantly influence drug partitioning and distribution in brain tissue.
  • This method offers a more nuanced evaluation of CNS drug penetration compared to simple ratios.

Conclusions:

  • Optimal CNS drug penetration relies on a balance of BBB permeability, low efflux, and suitable physicochemical properties.
  • Integrated data analysis enhances the prediction of drug disposition in the brain.
  • This approach refines the assessment of CNS-penetrating compounds in drug discovery.