Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles

Rebeca Penalva, Jorge Morales, Carlos J. Gonzalez-Navarro, Eneko Larrañeta , Gemma Quincoces, Ivan Penuelas, Juan M. Irache

Research output: Contribution to journalArticlepeer-review

60 Citations (Scopus)
193 Downloads (Pure)

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.
Original languageEnglish
Article number2816
Number of pages17
JournalInternational journal of molecular sciences
Volume19
Issue number9
DOIs
Publication statusPublished - 18 Sep 2018

Keywords

  • resveratrol
  • casein
  • nanoparticles
  • oral delivery
  • mucus-permeating
  • bioavailability
  • resveratrol-O-3-glucuronide

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