High-Throughput In Vitro Permeation Enhancer Screening in Caco-2 Cells: Accelerating Oral Peptide Therapeutics Development

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September 01,2026

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The development of oral peptide therapeutics has gained significant attention in the pharmaceutical industry. However, one of the key challenges limiting peptide oral bioavailability is the poor permeability. To overcome this challenge, permeation enhancers (PEs) have emerged as a critical strategy in enhancing peptide delivery. Rodents have been commonly used for screening PEs for peptide therapeutics. To minimize animal testing and better align with FDA’s 3Rs (Replacement, Reduction, Refinement) principles, we developed a pre-screening strategy utilizing Caco-2 cells.

High-Throughput In Vitro Permeation Enhancer Screening in Caco-2 Cells Accelerating Oral Peptide Therapeutics Development.jpg

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