Strategies to deliver peptide drugs to the brain

Aikaterini Lalatsa, Andreas G. Schatzlein, Ijeoma F. Uchegbu

Research output: Contribution to journalReview articlepeer-review

135 Citations (Scopus)
14 Downloads (Pure)


Neurological diseases such as neurodegeneration, pain, psychiatric disorders, stroke, and brain cancers would greatly benefit from the use of highly potent and specific peptide pharmaceuticals. Peptides are especially desirable because of their low inherent toxicity. The presence of the blood brain barrier (BBB), their short duration of action, and their need for parenteral administration limits their clinical use. However, over the past decade there have been significant advances in delivering peptides to the central nervous system. Angiopep peptides developed by Angiochem (Montreal, Canada), transferrin antibodies developed by ArmaGen (Santa Monica, USA), and cell penetrating peptides have all shown promise in delivering therapeutic peptides across the BBB after intravenous administration. Noninvasive methods of delivering peptides to the brain include the use of chitosan amphiphile nanoparticles for oral delivery and nose to brain strategies. The uptake of the chitosan amphiphile nanoparticles by the gastrointestinal epithelium is important for oral peptide delivery. Finally protecting peptides from plasma degradation is integral to the success of most of these peptide delivery strategies.

Original languageEnglish
Pages (from-to)1081-1093
Number of pages13
JournalMolecular Pharmaceutics
Issue number4
Publication statusPublished - 7 Apr 2014


  • blood brain barrier
  • brain delivery
  • cell penetrating peptides
  • intranasal
  • intravenous
  • nanoparticles
  • neurodegenerative diseases
  • opioid peptides
  • oral
  • peptides
  • receptor-mediated endocytosis


Dive into the research topics of 'Strategies to deliver peptide drugs to the brain'. Together they form a unique fingerprint.

Cite this