The challenges of oral peptide delivery
For oral peptide therapeutics to be effective, formulations must:
- prevent peptide degradation in the gastro-intestinal tract
- promote peptide permeability
Peptides need to be lipophilized to be incorporated in lipid excipients
Most peptides are hydrophilic and therefore cannot be incorporated in lipid-based formulations. They need to be lipidized (i.e. increase their LogP).
Hydrophobic ion pairing (HIP) is a strategy to increase the lipophilicity of peptides. Using three model peptides, a marked increase in LogP was obtained, demonstrating that HIP-peptides were lipophilic.
Self emulsifying drug delivery system (SEDDS): a simple and efficient solution
- consists of a mixture of oils, surfactants and solvents designed to solubilize the drug throughout the digestion process
- offers an effective protection of HIP-peptide from enzyme degradation and glutathione reduction
- permeates through the intestinal mucus
- enables high HIP-peptide payload
Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC): a promising solution