Fabrication of phosphatidylcholine-EGCG nanoparticles with sustained release in simulated gastrointestinal digestion and their transcellular permeability in a Caco-2 monolayer model

Abstract

In this study, we prepared phosphatidylcholine (PC)-EGCG complex nanoparticles (P-E NPs) by solvent reflux method. The physicochemical properties, in vitro digestion, uptake in Caco-2 cells, and bidirectional permeability of P-E NPs were systematically investigated. The constructed P-E1.5:1 NPs had an average particle size of 118 nm, a ζ-potential of −37.8 mV, and a polymerization dispersion index (PDI) of 0.16. The encapsulation efficiency (EE) of EGCG was 85.0% and the loading capacity (LC) was 24.4%. UV spectra, FTIR, XRD and intermolecular force results indicated that hydrophobic, electrostatic and hydrogen bonding interactions contributed to formate P-E1.5:1 NPs. P-E1.5:1 NPs exhibited first-order kinetics sustained release properties in simulated gastrointestinal digestion. Furthermore, P-E1.5:1 NPs were able to enhance absorptive transport and inhibit efflux transport mediated by MRP2 and P-gp compared to EGCG. These results indicated that P-E1.5:1 NPs may be a potential strategy to ameliorate EGCG bioavailability.