Related Experiment Video
Updated: Aug 14, 2026
08:43
Rat Model of Blood-brain Barrier Disruption to Allow Targeted Neurovascular Therapeutics
Published on: November 30, 2012
Targeted delivery across the blood-brain barrier
Pieter J Gaillard1, Corine C Visser, Albertus G de Boer
1to-BBB technologies BV, Bio Science Park Leiden, Gorlaeus Laboratories, LACDR Facilities-FCOL, The Netherlands. Gaillard@toBBB.com
Expert Opinion on Drug Delivery
|November 22, 2005
Summary
Targeting drugs to the brain safely and effectively uses receptor-mediated uptake at cerebral capillaries. This review examines transferrin, insulin, and lipoprotein receptor systems for potential human drug delivery applications.
Area of Science:
- Neuroscience
- Pharmacology
- Biotechnology
Background:
- Drug delivery to the brain is challenging due to the blood-brain barrier.
- Endogenous receptor-mediated uptake at cerebral capillaries offers a promising strategy for brain targeting.
- Existing animal model successes highlight the need for clinical translation.
Purpose of the Study:
- To review and compare endogenous receptor-mediated drug delivery systems for brain targeting.
- To discuss the potential and limitations of these systems for human applications.
- To explore future directions for clinical translation of brain-targeted drug delivery.
Main Methods:
- Review of literature on receptor-mediated brain drug delivery systems.
- Focus on transferrin, insulin, low-density lipoprotein-related protein (LRP) 1 and 2 receptors, and diphtheria toxin receptor pathways.
- Comparative analysis of system efficacy, limitations, and clinical potential.
Main Results:
- Transferrin and insulin receptor systems are well-characterized for brain uptake.
- Emerging systems utilize LRP1, LRP2 (megalin), and the diphtheria toxin receptor.
- No clinical trials have yet been conducted for these brain-targeting systems.
Conclusions:
- Receptor-mediated transcytosis across cerebral capillaries is a viable strategy for brain drug delivery.
- Various endogenous receptors offer distinct targeting possibilities and present unique challenges.
- Further research and clinical trials are essential to realize the therapeutic potential of these systems for neurological disorders.
More Related Videos
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...
01:29Drug 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...