Co-Loading of Ascorbic Acid and Tocopherol in Eudragit-Nutriosomes to Counteract Intestinal Oxidative Stress

在Eudragit-Nutriosomes中共同负载抗坏血酸和生育酚以对抗肠道氧化应激

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Abstract

The present study aimed at developing a new vesicular formulation capable of promoting the protective effect of ascorbic acid and tocopherol against intestinal oxidative stress damage, and their efficacy in intestinal wound healing upon oral administration. A pH-dependent copolymer (Eudragit(®) L100), a water-soluble prebiotic fibre (Nutriose(®) FM06), a phospholipid mixture (Lipoid S75), and two natural antioxidants (ascorbic acid and tocopherol) were combined to fabricate eudragit-nutriosomes by a simple, solvent-free procedure. The vesicles were spherical and oligolamellar, with some multicompartment structures in Eudragit-nutriosomes, small in size (~100 nm), with highly negative zeta potential. The effect of Eudragit(®) and Nutriose(®) on the stability on storage and in simulated gastrointestinal fluids were confirmed by the Turbiscan(®) technology and in vitro studies, respectively. Eudragit-nutriosomes exhibited a protective effect against H₂O₂-induced oxidative stress, and a proliferative effect in Caco-2 cells, as they provided the closure of the scratched area after 96 h of incubation.

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