Peptide permeation enhancers for improving oral bioavailability of macromolecules

초록

Background: Oral delivery of macromolecules has been limited mainly by their low intestinal permeability. Chemical permeation enhancers (CPEs) are typically used to improve intestinal permeation. However, their targets are unspecified and absorption enhancing mechanisms are not fully proven. In addition, they show undesired toxicity. Peptide permeation enhancers (PPEs) have been gaining continuous interest as they modulate specific types of tight-junction proteins with high efficacy compared to that achieved by CPEs. Moreover, their reversible action on increasing the intestinal permeability demonstrably indicates their potential as a safe ingredient. Area covered: This review presents an overview of PPEs that have demonstrated sufficient safety and efficacy in increasing the intestinal absorption of synthetic peptides or biologics. Their basic concepts are briefly provided, and the distinct characteristics of each PPE are discussed with a particular focus on their absorption enhancement activity and the rationale for this improvement. Expert opinion: PPE is a highly promising active excipient for the oral formulations of macromolecules that can replace target-unspecified CPEs. The use of PPEs in oral formulations will rapidly increase as their in vivo safety and stability issues are being overcome. This review provides a guide to select the optimal PPEs for the oral formulations of macromolecules and can further be used to identify novel PPEs with the desired attributes for this purpose.

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