Challenges in oral peptide delivery: lessons learnt from the clinic and future prospects

Therapeutic peptides have become very successful drugs due to their specificity, potency and low toxicity, but they show challenges for their delivery, due to their short half-life and rapid plasma clearance. For these reasons, peptides are usually administered using injectable sustained-release for...

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Bibliographic Details
Published inTherapeutic delivery Vol. 8; no. 8; pp. 663 - 684
Main Author Richard, Joël
Format Journal Article
LanguageEnglish
Published England Future Science Ltd 01.07.2017
Subjects
Administration, Oral
Drug Delivery Systems
Half-Life
Humans
Intestinal Absorption
intestinal epithelium
intraenteral microinjection
nanoparticles
oral bioavailability
oral peptide delivery
peptides
Peptides - administration & dosage
permeation enhancers
protease inhibitors
tight junctions
intraenteral microinjection
nanoparticles
oral peptide delivery
protease inhibitors
peptides
intestinal epithelium
tight junctions
oral bioavailability
permeation enhancers
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Summary:Therapeutic peptides have become very successful drugs due to their specificity, potency and low toxicity, but they show challenges for their delivery, due to their short half-life and rapid plasma clearance. For these reasons, peptides are usually administered using injectable sustained-release formulations. Oral peptide route is highly compelling from a patient and commercial point of view. However, poor peptide stability and low permeability across the intestinal epithelium still make it very challenging to effectively deliver peptides by the oral route. In this paper, biopharmaceutical and formulation features of oral peptides, as well as key clinical outcomes, are reviewed and discussed in the perspective of designing next generation of oral peptide formulations for a true paradigm shift.
ISSN:2041-5990
2041-6008
DOI:10.4155/tde-2017-0024