Considerations in the developability of peptides for oral administration when formulated together with transient permeation enhancers

Abstract

This paper reviews many of the properties of a peptide that need to be considered prior to development as an oral dosage form when co-formulated with a permeation enhancer to improve oral bioavailability, including the importance and implications of peptide half-life on variability in pharmacokinetic profiles. Clinical considerations in terms of food and drug-drug interactions are also discussed. The paper further gives a brief overview how permeation enhancers overcome barriers that limit oral absorption of peptides and thereby improve their oral bioavailability, albeit bioavailabilities are still low single digit and variability is high.

Keywords: Bioavailability; Oral peptide delivery; Peptide properties; Permeation enhancer; Population pharmacokinetic modelling; Variability.