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

Ken A. Witt, Thomas P. Davis

Research output: Contribution to journalReview articlepeer-review

83 Scopus citations


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)
Article number9
Pages (from-to)E76-E88
JournalAAPS Journal
Issue number1
StatePublished - Feb 24 2006


  • Biphalin
  • Delivery strategies
  • Transport

ASJC Scopus subject areas

  • Pharmaceutical Science


Dive into the research topics of 'CNS drug delivery: Opioid peptides and the blood-brain barrier'. Together they form a unique fingerprint.

Cite this