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Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles

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...

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Autores principales: Peñalva, Rebeca, Morales, Jorge, González-Navarro, Carlos J., Larrañeta, Eneko, Quincoces, Gemma, Peñuelas, Ivan, Irache, Juan M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6163610/
https://www.ncbi.nlm.nih.gov/pubmed/30231546
http://dx.doi.org/10.3390/ijms19092816
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author Peñalva, Rebeca
Morales, Jorge
González-Navarro, Carlos J.
Larrañeta, Eneko
Quincoces, Gemma
Peñuelas, Ivan
Irache, Juan M.
author_facet Peñalva, Rebeca
Morales, Jorge
González-Navarro, Carlos J.
Larrañeta, Eneko
Quincoces, Gemma
Peñuelas, Ivan
Irache, Juan M.
author_sort Peñalva, Rebeca
collection PubMed
description 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.
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spelling pubmed-61636102018-10-10 Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles Peñalva, Rebeca Morales, Jorge González-Navarro, Carlos J. Larrañeta, Eneko Quincoces, Gemma Peñuelas, Ivan Irache, Juan M. Int J Mol Sci Article 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. MDPI 2018-09-18 /pmc/articles/PMC6163610/ /pubmed/30231546 http://dx.doi.org/10.3390/ijms19092816 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Peñalva, Rebeca
Morales, Jorge
González-Navarro, Carlos J.
Larrañeta, Eneko
Quincoces, Gemma
Peñuelas, Ivan
Irache, Juan M.
Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles
title Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles
title_full Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles
title_fullStr Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles
title_full_unstemmed Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles
title_short Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles
title_sort increased oral bioavailability of resveratrol by its encapsulation in casein nanoparticles
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6163610/
https://www.ncbi.nlm.nih.gov/pubmed/30231546
http://dx.doi.org/10.3390/ijms19092816
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