CNS drug delivery: Opioid peptides and the blood-brain barrier

Ken A. Witt, Thomas P. Davis

Research output: Chapter in Book/Report/Conference proceedingChapter


Peptides are key regulators in cellular and intercellular physiological responses and possess enormous promise for the treatment of pathological conditions. Opioid peptide activity within the central nervous system (CNS) is of particular interest for the treatment of pain owing to the elevated potency of peptides and the centrally mediated actions of pain processes. Despite this potential, peptides have seen limited use as clinically viable drugs for the treatment of pain. Reasons for the limited use are primarily based in the physiochemical and biochemical nature of peptides. Numerous approaches have been devised in an attempt to improve peptide drug delivery to the brain, with variable results. This review describes different approaches to peptide design/modification and provides examples of the value of these strategies to CNS delivery of peptide drugs. The various modes of modification of therapeutic peptides may be amalgamated, creating more efficacious hybrid peptides, with synergistic delivery to the CNS. The ongoing development of these strategies provides promise that peptide drugs may be useful for the treatment of pain and other neurologically-based disease states in the future.

Original languageEnglish (US)
Title of host publicationDrug Addiction
Subtitle of host publicationFrom Basic Research to Therapy
PublisherSpringer New York
Number of pages23
ISBN (Print)9780387766775
StatePublished - 2008


  • biphalin
  • delivery strategies
  • transport

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)


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