Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles

Autor:	Jorge C. Morales, Juan M. Irache, Eneko Larrañeta, Gemma Quincoces, Rebeca Peñalva, Iván Peñuelas, Carlos J González-Navarro
Rok vydání:	2018
Předmět:	Male 0301 basic medicine mucus-permeating Cardiotonic Agents Metabolite Administration Oral Biological Availability resveratrol Pharmacology Resveratrol casein resveratrol-O-3-glucuronide Article Catalysis lcsh:Chemistry Inorganic Chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine SDG 3 - Good Health and Well-being In vivo Casein Animals Anticarcinogenic Agents Rats Wistar Physical and Theoretical Chemistry lcsh:QH301-705.5 Molecular Biology Spectroscopy Drug Carriers Organic Chemistry Caseins food and beverages Biological activity General Medicine oral delivery In vitro Computer Science Applications Bioavailability 030104 developmental biology lcsh:Biology (General) lcsh:QD1-999 chemistry Polyphenol 030220 oncology & carcinogenesis nanoparticles bioavailability
Zdroj:	Penalva, R, Morales, J, Gonzalez-Navarro, C J, Larrañeta, E, Quincoces, G, Penuelas, I & Irache, J M 2018, ' Increased Oral Bioavailability of Resveratrol by Its Encapsulation in Casein Nanoparticles ', International journal of molecular sciences, vol. 19, no. 9, 2816 . https://doi.org/10.3390/ijms19092816 International Journal of Molecular Sciences Volume 19 Issue 9 International Journal of Molecular Sciences, Vol 19, Iss 9, p 2816 (2018)
ISSN:	1422-0067
Popis:	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 &mu g/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 &ldquo translocation&rdquo 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.
Databáze:	OpenAIRE
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