Development and thermodynamically characterization of Food Grade secondary oil in water nanoemulsions and in vitro validation through digestion simulation and muco-adhesion evaluation by intestine on chip and INFOGEST protocol

Title : Development and thermodynamically characterization of Food Grade secondary oil in water nanoemulsions and in vitro validation through digestion simulation and muco-adhesion evaluation by intestine on chip and INFOGEST protocol

Abstract:

Among oral delivery systems, oil in water nano-emulsions (O/W NEs) are of particular interest to improve pharmacokinetics of lipophilic compounds. Recently, we have implemented a successful strategy to improve O/W NEs stability, based on a polymeric coating on an oil core, through the use of pharma grade formulations. However, in the field of food supplements, food grade materials are the top choice since they combine safety and cost effectiveness. Here, we have replaced pharma grade (PG) with food grade (FG) materials in the preparation of the secondary O/W NEs and performed a comparative study between the two formulations to assess the FG one. Additionally, in order to provide formulations with improved muco-adhesion to the intestinal barrier, secondary O/W NEs were prepared by adding thiol groups to chitosan (Ct) via a simple non-covalent procedure based on N-acetyl-cysteine (NAC) salification, which is compliant with food supplement formulations. PG and FG formulations, in different materials combinations, were prepared and physio-chemically characterized (DLS, 1H-NMR, ITC). The obtained findings demonstrate that FG and PG formulations are similar and have comparable stability. FG formulations (NEs, Ct-NEs and Ct-NAC-NEs) loaded with curcumin were prepared and compared with the free drug in terms of drug bioaccessibility through the INFOGEST modified protocol confirming improved bioaccessibility as compared to free curcumin. Very interestingly, by comparing muco-adhesion properties of the two polymeric coatings (Ct and Ct-NAC) within an intestine on chip device able to mimic the complex intestinal functions, a significant improvement in the muco-adhesive properties of Ct-NAC was observed with respect to Ct due to the presence of thiol groups. Nonetheless, in-vivo assays are required as a final assessment of the proposed system.

Audience take-away:

• Optimized layering of nanomaterials trough different method.
• Improve bioavability and  muco-adhesive properties of nano formulation.
• The non-covalent thiol functionalization of chitosan open the door to an immediate use of such formulation with no need for safety clinical tests.

Biography:

Elena Lagreca was graduated at University of Naples Federico II in Medicinal Chemistry and Pharmaceutical Technology and She is a PhD candidate in “INDUSTRIAL PRODUCT AND PROCESS ENGINEERING” at Department of Chemical, Materials and Production Engineering (DICMaPI) of University of Naples Federico II and Istituto Italiano di Tecnologia in Naples. She is expert in preparation and characterization of polymeric micro-particles, primary and secondary nano-emulsion oil in water as drug delivery system for enzyme, proteins, small molecules and nutraceuticals. In the last 3 years She  become an expert in biomaterial synthesis, peptide synthesis, functionalization and characterization by novel techniques such as IR, QCM, SEM, CRYO-TEM, AFM, ITC  confocal microscopies; moreover she works in cell culture and cell membrane extraction.