Scientific writing: Nanotechnology strategies for the insulin oral delivery

Federico Benetti – Executive Director at ECSIN LAB, a Mérieux NutriSciences Company – has been involved in the publication of a scientific paper entitled “A nanoemulsion/micelles mixed nanosystem for the oral administration of hydrophobically modified insulin” on Drug Delivery and Translational Research (2021).

The Nanotechnology strategy applied for the biopharmaceutical fields

Nowadays, patients receiving insulin treatment are obliged to take it by injection, a fact that is associated to a low patient compliance, especially in chronic treatments. Hence, the search for an alternative and non-invasive administration route for these molecules has become an attractive goal in the biopharmaceutical field. In this case, researchers are investing their efforts in therapeutics development that could be administered via oral route, since it would mimic the physiological pathway of the endogenously secreted insulin through the portal circulation.
Due to the high hydrosolubility and susceptibility to degradation by intestinal enzymes, nanotechnology is one of the strategies adopted to increase the oral bioavailability of insulin, and lipid-based nanocarriers are considered particularly interesting based on their biocompatibility and in the stabilizing and absorption enhancing properties of their lipid constituents.

The aim of the study

The aim of the study was to rationally design, develop, and fully characterize a new nanoemulsion intended for the oral administration of hydrophobically modified insulin (HM-insulin), by selecting biomaterials with stabilizing, penetration and mucodiffusive properties.

Results

The HM-loaded mixed nanosystem exhibited in vitro appropriate properties, such as good stability, mucodiffusion, cell interaction, and uptake without cytotoxic effects, which reinforced the interest of its further in vivo evaluation.
Following its intra-intestinal administration in both healthy and diabetic rats, a significant, but moderate hypoglycemic response more noticeable in the diabetic model, was observed in vivo.
Overall, the study shows the promising properties of the formulation and its significant effect observed in vivo, confirming the importance of in vitro–in vivo correlation when referring to the rational design of oral peptide delivery formulations.