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Updated: Aug 27, 2025

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
Considerations in the developability of peptides for oral administration when formulated together with transient
Staffan Berg1, Helena Edlund2, William R F Goundry3
1Advanced Drug Delivery, Pharmaceutical Science, R&D, AstraZeneca, Gothenburg, Sweden; The Swedish Drug Delivery Center, Department of Pharmacy, Uppsala University, Biomedicinskt Centrum, Uppsala, Sweden.
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.
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