Lipid-based nanocarriers for oral delivery of peptides

Therapeutic peptides can treat a wide variety of diseases with selective and potent action. Their oral bioavailability is strongly limited by an important proteolytic activity in the intestinal lumen poor permeation across border. We have evaluated capacity solid lipid nanoparticles (SLN) nanostructured carriers (NLC) to overcome both limiting aspects, using leuprolide (LEU) as model peptide. Lipidization LEU formation hydrophobic ion pair (HIP) sodium docusate enables significant increase peptide encapsulation efficiency SLN NLC. The nanocarriers, obtained high-pressure homogenization, measured 120 nm were platelet shaped. Regarding protective effect towards degradation, only NLC maintained integrity presence trypsin. Intestinal transport, on Caco-2 (enterocyte-like model) Caco-2/HT29-MTX (mucin-secreting monolayers, showed nanocarriers internalization enterocytes but no improvement permeability. Indeed, combination platelet-shape stability HIP transport medium induces high burst release peptide, Stability lipidization needs be improved withstand biorelevant benefit from advantages consequently improve their bioavailability.