Peptide pills for brain diseases? Reality and future perspectives

Dolores Remedios Serrano Lopez, Aikaterini Lalatsa

Research output: Contribution to journalArticlepeer-review

15 Citations (Scopus)


The peptide therapeutic market is one of the fastest growth areas of the pharmaceutical industry. Although few orally administered peptides are marketed and many are in different phases of clinical development, there is no marketed oral peptide therapeutic used for CNS disorders. The major challenges involved in orally delivering peptides to the brain relate to their enzymatic instability and inability to permeate across physiological barriers. The paucity of therapies for the treatment of brain diseases and the presence of the blood-brain barrier excluding 98% of therapeutic molecules necessitates parenteral administration. Various approaches have been applied to enhance oral peptide bioavailability, but only nanoparticulate strategies were able to deliver orally therapeutic peptides to the brain. Although industry may be reluctant to invest in developing oral peptide nanomedicines, the increasingly unmet clinical need and economic burden associated with brain diseases will fuel the development of the first marketed oral-to-brain peptide therapy.
Original languageEnglish
Pages (from-to)479-501
Number of pages23
JournalTherapeutic Delivery
Issue number4
Publication statusPublished - Apr 2013


  • Administration, Oral
  • Animals
  • Drug Stability
  • Nanomedicine
  • Protein Stability
  • Humans
  • Capillary Permeability
  • Brain Diseases
  • Drug Design
  • Biological Availability
  • Biotransformation
  • Peptides
  • Central Nervous System Agents
  • Blood-Brain Barrier


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