Abstract
Methodology to enhance the intestinal absorption of peptides is an important challenge due to their easily degradation and poor permeability across the intestinal epithelium. In this study, the fish-derived peptide (DGDDGEAGKIG)-loaded chitosan (CS) nanoparticles (CS/PEP-NPs) were prepared and investigated in Caco-2 monolayer model. The results indicated zeta potential of CS/PEP-NPs increased with the increase in molecular weight of CS (10-50kDa). Transmission electron microscopy images revealed the CS/PEP-NPs were uniform spherical-shaped nanoparticles with a diameter of 50-200nm (150kDa). Compared to other CS/PEP-NPs, 150-kDa CS/PEP-NPs performed an outstanding apparent permeability coefficient (Papp, 2.29×10-5 cms-1 ) and cumulative amount of peptide (120min, 2,987ng) in Caco-2 cells. CS/PEP-NPs could reduce the tight junction integrity of Caco-2 cells and enhance the intracellular fluorescence intensities of fluorescein isothiocyanate-labeled peptide. These findings suggest that chitosan nanoparticles are promising carriers to promote intestinal absorption of fish-derived peptide via paracellular pathway mediated by tight junctions. PRACTICAL APPLICATIONS: Chitosans are promising carriers to promote intestinal absorption of fish-derived peptide. The 150-kDa CS/PEP-NPs performed an outstanding apparent permeability coefficient (Papp, 2.29×10-5 cms-1 ) and cumulative amount of peptide (120min, 2,987ng) in Caco-2 cells. CS/PEP-NPs could reduce the tight junction integrity of Caco-2 cells and enhance the peptide uptake by paracellular pathway. Chitosan nanoparticles can be developed as vehicles for enhancing the cellular uptake of peptide in food industry.
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