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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...
Factors Affecting Drug Distribution: Physiological Barriers01:23

Factors Affecting Drug Distribution: Physiological Barriers

Drug distribution in the body is intricately regulated by various physiological barriers that control the passage of substances. These include the capillary endothelial barrier, the blood-brain, blood-cerebrospinal fluid, blood-placental, and blood-testis barriers.
The capillary endothelial barrier allows only smaller molecules below 600 Da (Daltons) to pass through. It also restricts drugs like heparin that are bound to blood components, limiting their movement within the bloodstream.
The...
Drug Delivery: Parenteral Route01:29

Drug Delivery: Parenteral Route

The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems01:22

Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems

Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug absorption...
Bioavailability: Overview01:17

Bioavailability: Overview

Bioavailability refers to the proportion of an administered drug that reaches the systemic circulation in its active, unaltered form. It is a crucial pharmacokinetic parameter that determines the effectiveness of a drug in achieving its intended therapeutic outcomes. The route of administration significantly influences bioavailability, with intravenous administration achieving 100% bioavailability as the drug directly enters the bloodstream. In contrast, oral administration often results in...

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Related Experiment Video

Updated: Jun 18, 2026

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

Blood-brain interfaces and cerebral drug bioavailability.

J-F Ghersi-Egea1, K S Mönkkönen, C Schmitt

  • 1Inserm, U842, faculté de médecine Laennec, université de Lyon, université Lyon-1, UMR-S842, 69008 Lyon, France. jean-francois.ghersi-egea@inserm.fr

Revue Neurologique
|November 17, 2009
PubMed
Summary
This summary is machine-generated.

Drug delivery to the brain is challenging due to the blood-brain barrier and blood-cerebrospinal fluid barrier. Understanding efflux transporters is crucial for improving neurological disease treatments.

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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

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Predicting In Vivo Payloads Delivery using a Blood-brain Tumor-barrier in a Dish
13:34

Predicting In Vivo Payloads Delivery using a Blood-brain Tumor-barrier in a Dish

Published on: April 16, 2019

Area of Science:

  • Neuroscience
  • Pharmacology
  • Biochemistry

Background:

  • The low bioavailability of drugs in the brain hinders the treatment of neurological disorders.
  • The blood-brain barrier (BBB) and blood-cerebrospinal fluid (CSF) barrier tightly regulate substance entry into the brain.
  • Mechanisms include endothelial tight junctions and efflux transporters, impacting drug distribution.

Purpose of the Study:

  • To review the mechanisms limiting drug penetration across blood-brain interfaces.
  • To highlight the role of efflux transporters in cerebral drug disposition.
  • To discuss implications for neurological disease and brain tumor treatment.

Main Methods:

  • Literature review of studies on drug transport across blood-brain interfaces.
  • Analysis of the role of tight junctions and efflux transporters (ABC and SLC families).
  • Examination of transporter regulation in pathophysiological conditions and development.

Main Results:

  • Tight junctions impede water-soluble drugs, while efflux transporters restrict lipid-soluble drugs.
  • Efflux transporters significantly impact drug efficacy, especially in brain tumors.
  • Transporter expression is altered in conditions like epilepsy and inflammation.

Conclusions:

  • Cerebral drug bioavailability is governed by complex interactions at blood-brain interfaces.
  • Targeting efflux transporters holds promise for enhancing neurological therapies.
  • Further research is needed on transporter development and regulation for optimized drug delivery.