Self-emulsifying drug delivery systems (SEDDS) representing isotropic mixtures of oils, surfactants and hydrophilic cosolvents are commonly used to increase the oral bioavailability of poorly water-soluble drugs. This technology is also a promising tool to open the door for the oral administration of therapeutic peptides and proteins. Up to date, however, this promising strategy has by far not reached its full potential, as various hurdles still need to be overcome: the loading of hydrophilic peptides in lipid-based formulations, the protection of peptides against metabolic enzymes (proteases, lipases) and the reduction by glutathione, the efficient permeation of SEDDS through the mucus layer of the intestinal epithelium and finally the absorption of the large hydrophilic molecule. This presentation will present the latest results of peptide oral delivery with SEDDS where the aforementioned hurdles were overcome:<br/>- Hydrophobic ion pairing of peptides with anionic surfactants allows reaching more than 10% payload in SEDDS with protic solvent and surfactants like Labrasol® ALF.<br/>- SEDDS are also able to protect peptides against various metabolic enzymes (trypsin, α-chymotrypsin, elastase) and the reduction by glutathione as long as the peptide stay within the colloidal phase. The (micro)emulsions formed after dilution of SEDDS with peptides are stable in term of particle size and zeta potential for at least 4 hours and protect efficiently peptides against degradation.<br/>- Finally, SEDDS containing Labrasol® ALF are able to increase the absorption of peptides by membrane fluidization and opening of tight junctions of the intestinal barrier.<br/>

Advances in peptide delivery: Hydrophobic ion pairing in SEDDS for solubilization, protection, and enhanced delivery of oral peptides

256th National Meeting (2018)

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