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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Related Experiment Video

Updated: Jul 20, 2026

Focused Ultrasound Induced Blood-Brain Barrier Opening for Targeting Brain Structures and Evaluating Chemogenetic Neuromodulation
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Drug targeting to the brain.

A G de Boer1, P J Gaillard

  • 1Blood-Brain Barrier Research Group, Division of Pharmacology, Leiden-Amsterdam Center for Drug Research, University of Leiden, 2300 RA Leiden, The Netherlands. B.Boer@lacdr.leidenuniv.nl

Annual Review of Pharmacology and Toxicology
|September 12, 2006
PubMed
Summary

Drug delivery to the brain is challenging due to protective barriers like the blood-brain barrier (BBB). This review explores strategies for enhancing drug transport across these barriers for treating brain diseases.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Biomedical Engineering

Background:

  • The central nervous system (CNS) is protected by specialized barriers, including the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB).
  • These barriers tightly regulate the passage of substances into the brain, maintaining homeostasis.
  • Most drugs cannot effectively cross these barriers, hindering the treatment of neurological disorders.

Purpose of the Study:

  • To review the biology and physiology of the BBB and BCSFB.
  • To discuss current strategies for overcoming brain barriers in drug delivery.
  • To explore methods for delivering large-molecular-weight drugs to the brain.

Main Methods:

  • Brief overview of BBB and BCSFB physiology.
  • Discussion of local and global drug delivery approaches.
  • Exploration of viral and nonviral (receptor-mediated) delivery systems.

Main Results:

  • Drug delivery to the brain is significantly impeded by its protective barriers.
  • Various strategies are being developed to enhance drug transport and distribution.
  • Both local and systemic delivery methods, alongside viral and nonviral vectors, show promise.

Conclusions:

  • Overcoming CNS barriers is crucial for effective brain disease treatment.
  • A range of drug delivery strategies are available and under development.
  • Targeted delivery of large-molecule drugs to the brain remains an active area of research.