Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles

Ivan Peñuelas,Carlos González-Navarro,Jorge Morales,Gemma Quincoces,Rebeca Peñalva,Juan Irache,Eneko Larrañeta

doi:10.3390/ijms19092816

Ivan Peñuelas, Carlos González-Navarro + Show 5 more

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https://doi.org/10.3390/ijms19092816

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Abstract

Resveratrol is a naturally occurring polyphenol that provides several health benefits including cardioprotection and cancer prevention. However, its biological activity is limited by a poor bioavailability when taken orally. The aim of this work was to evaluate the capability of casein nanoparticles as oral carriers for resveratrol. Nanoparticles were prepared by a coacervation process, purified and dried by spray-drying. The mean size of nanoparticles was around 200 nm with a resveratrol payload close to 30 μg/mg nanoparticle. In vitro studies demonstrated that the resveratrol release from casein nanoparticles was not affected by the pH conditions and followed a zero-order kinetic. When nanoparticles were administered orally to rats, they remained within the gut, displaying an important capability to reach the intestinal epithelium. No evidence of nanoparticle “translocation” were observed. The resveratrol plasma levels were high and sustained for at least 8 h with a similar profile to that observed for the presence of the major metabolite in plasma. The oral bioavailability of resveratrol when loaded in casein nanoparticles was calculated to be 26.5%, 10 times higher than when the polyphenol was administered as oral solution. Finally, a good correlation between in vitro and in vivo data was observed.

Highlights

Resveratrol (Rsv) is a nutraceutical named trans-3,4,5-trihydroxystilbene and consists of two aromatic rings which are linked through a methylene bridge
These results suggest that the release mechanism of resveratrol from casein nanoparticles would be ruled by the eroSsIFio(npHof6.t8h)e nanoparticulate matrix
The resveratrol release data from casein nanoparticles fitted well to both the Korsmeyer-Peppas model (KKT = 0.14 ± 0.01 h−n; n = 1.02 ± 0.04; R2 > 0.99) and the zero-order kinetics equation (K = 0.14 ± 0.00 h−1; R2 > 0.99). These results suggest that the release mechanism of resveratrol from casein nanoparticles would be ruled by the erosion of the nanoparticulate matrix

Summary

Introduction

Resveratrol (Rsv) is a nutraceutical named trans-3,4 ,5-trihydroxystilbene and consists of two aromatic rings which are linked through a methylene bridge It is a natural polyphenol found in more than 70 species of plants, in grapes, blueberries and peanuts [1]. The mechanism by which resveratrol exerts such arrange of beneficial effects across species and disease models is not yet elucidated These effects would be related to the capability of this polyphenol to enhance the nitric oxide bioactivity and/or its inhibitory effect on platelet COX-1 and NF-κB [6]. It has been demonstrated that resveratrol possesses cancer chemopreventive and chemotherapeutic activity [5,10] This fact would be related with its inhibitory effect over cyclooxygenase [2], NF-κB [11] and protein kinase C [12], among others. Resveratrol would inhibit the tumor-induced neovascularization acting as an antiangiogenic agent [10,13]

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