Related Experiment Video
Updated: Jul 17, 2026
08:43
Rat Model of Blood-brain Barrier Disruption to Allow Targeted Neurovascular Therapeutics
Published on: November 30, 2012
Blood-brain barrier delivery
1Department of Medicine, UCLA, Los Angeles, CA 90024, USA. wpardridge@mednet.ucla.edu
Drug Discovery Today
|January 3, 2007
Summary
Developing drugs for brain conditions is challenging due to the blood-brain barrier (BBB). Future neuropharmaceutics must leverage endogenous transporters to enable drug delivery across the BBB.
Area of Science:
- Neuroscience
- Pharmacology
- Biotechnology
Background:
- Neuropharmaceutics represents a significant growth area within the pharmaceutical industry.
- The primary obstacle to effective neuropharmaceutics is the blood-brain barrier (BBB), which prevents most drugs from reaching the brain.
- Currently, over 98% of small-molecule drugs and virtually all large-molecule drugs fail to cross the BBB.
Purpose of the Study:
- To address the challenge of drug delivery across the blood-brain barrier (BBB).
- To propose a new strategy for developing drugs that can effectively reach the brain.
Main Methods:
- Analysis of the physiological properties of the blood-brain barrier (BBB).
- Identification of endogenous transporters present within the BBB.
- Conceptual framework for re-configuring drug development programs.
Main Results:
- The BBB possesses multiple endogenous transporters capable of facilitating molecular transport.
- These transporters offer a viable pathway for drug molecules to cross the BBB.
Conclusions:
- Future brain drug development must be redesigned to utilize endogenous BBB transporters for drug delivery.
- Formulating drugs to interact with these transporters is crucial for successful neuropharmaceutic interventions.
Related Concept Videos
00:49The Blood-brain Barrier
Overview
01:25Physiological 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...
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...
01:23Factors 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...
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...
01:29Drug 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...
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...
01:24Cellular Membranes and Drug Transport
Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
01:23Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport
Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...