Permeation Enhancers to Increase Oral Bioavailability

Brought to you by Gattefossé Asia Pacific

Poor permeability is a limitation of a growing number of BCS III and IV molecules.

To facilitate absorption, several pathways are possible.

Transcellular route

Paracellular route

Transient opening of the tight junctions (mainly used by large hydrophilic solutes)

Boost the passage of molecules through the intestinal epithelia, by paracellular and/or transcellular pathway
Medium chain fatty acids, whose carbon chain contains 8 or 10 carbon atoms (commonly called C8-C10) are known to enhance the permeation
Labrasol® ALF, Labrafac™ MC60 and Capryol® 90 are all esters of C8-C10 fatty acids
Listed in the FDA Inactive Ingredients Database (IID)
Act both as solubilizers and permeation enhancers, and increase oral bioavailability

What about large molecules (peptides and proteins)?

Permeation of large molecules was enhanced safely and efficiently, using insulin as a model (McCartney et al., 2024; McCartney et al., 2023; Ukai et al., 2020b)
Threshold of molecular weight critical for permeability: molecules up to 40kDa can pass through tight junctions safely

Check out our latest whitepaper, brochure and Fast and Curious Fact series video or contact us for more case studies!

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