Design and formulation of Eudragit-coated zein/pectin nanoparticles for the colon delivery of resveratrol

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ORIGINAL PAPER

Design and formulation of Eudragit‑coated zein/pectin nanoparticles for the colon delivery of resveratrol Catia Contado1 · Laura Caselotto1 · Paola Mello1 · Annalisa Maietti1 · Lorenza Marvelli1 · Nicola Marchetti1 · Alessandro Dalpiaz1 Received: 30 January 2020 / Revised: 31 July 2020 / Accepted: 10 August 2020 © Springer-Verlag GmbH Germany, part of Springer Nature 2020

Abstract Resveratrol (RSV) is a naturally occurring polyphenolic phytoalexin with beneficial effects on human health, including the treatment and prevention of ulcerative colitis and cancer. This work proposes the formulation and characterization of new nanoparticles (NPs) for the specific colon delivery of RSV. RSV was encapsulated in zein (Z) NPs, coated by a hydrophilic pectin (P) shell to significantly increase the dissolution rate of RSV in aqueous environments. Since the dissolved drug was strongly degraded in a simulated gastrointestinal tract, the ZP-NPs were coated with Eudragit S 100. The coated particles, even if aggregated, had a spherical morphology with diameters in the 100–200 nm range. Release studies of RSV from the ZP coated NPs evidenced their potential ability to induce a specific colon delivery of this drug so that this formulation can be proposed to enrich natural food products to enhance their preventive and therapeutic effects in the lower GI tract. Keywords  Resveratrol · Zein nanoparticles · Pectin · Specific delivery · Controlled release · Field flow fractionation

Introduction Functional food and dietary supplements are increasingly used by citizens of industrialized countries for their purported health benefits, with the aim of enjoying a long life in good health. In the food supplement horizon, a growing area is the so-called botanical dietary supplements, sometimes called herbals or herbal dietary supplements, i.e. products made from plants, plant parts, or plant extracts [1], such the case of RSV (trans‐resveratrol; trans‐3,5,4′‐trihydroxy‐stilbene), a natural polyphenolic compound, found in a number of fruit, peanuts and in copious amounts in the skin of grapes, tomatoes, berries [2]. Assumed unknowingly since centuries in the traditional Chinese and Japanese medicine as Itadori tea, an herbal remedy for heart disease, strokes, anti-inflammatory, and Electronic supplementary material  The online version of this article (https​://doi.org/10.1007/s0021​7-020-03586​-w) contains supplementary material, which is available to authorized users. * Catia Contado [email protected] 1



Department of Chemical and Pharmaceutical Sciences, University of Ferrara, Via Luigi Borsari 46, 44121 Ferrara, Italy

anti-platelet agent, RSV became popular in the western culture thanks to the so-called “French paradox” [3, 4], for its presence in grapes and wine. Nowadays, RSV seems to be useful in reducing the risk of chronic diseases such as cardiovasculary, cancer and Alzheimer’s disease, contrasting the negative effects of free radicals on the cellular damages and inflammatory processes and preventing chronic int