Scientific publications

Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles

Peñalva R (1), Morales J (2), González-Navarro CJ (3), Larrañeta E (4), Quincoces G (5), Peñuelas I (6), Irache JM (7).

(1) NANO-VAC Research Group, Department of Pharmacy and Pharmaceutical Technology, University of Navarra, 31008 Pamplona, Spain.
(2) NANO-VAC Research Group, Department of Pharmacy and Pharmaceutical Technology, University of Navarra, 31008 Pamplona, Spain. 
(3) Centre for Nutrition Research, University of Navarra, 31080 Pamplona, Spain. 
(4) NANO-VAC Research Group, Department of Pharmacy and Pharmaceutical Technology, University of Navarra, 31008 Pamplona, Spain.
(5) Radiopharmacy Unit, Department of Nuclear Medicine, Clinica Universidad de Navarra, University of Navarra, 31008 Pamplona, Spain.
(6) Radiopharmacy Unit, Department of Nuclear Medicine, Clinica Universidad de Navarra, University of Navarra, 31008 Pamplona, Spain. 
(7) NANO-VAC Research Group, Department of Pharmacy and Pharmaceutical Technology, University of Navarra, 31008 Pamplona, Spain.

Magazine: International Journal of Molecular Sciences

Date: Sep 18, 2018

Radiopharmacy Unit [SP]

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.

CITATIONI  Int J Mol Sci. 2018 Sep 18;19(9). pii: E2816. doi: 10.3390/ijms19092816

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