Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol

<i>Trans</i>-resveratrol, a polyphenolic phytoalexin found in various plant sources, has been the focus of increasing attention in recent years because of its role in the prevention of many human diseases, and particularly because of its antioxidant properties. However, the in vivo effec...

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Main Authors: Monica Argenziano, Irfan Aamer Ansari, Elisabetta Muntoni, Rita Spagnolo, Anna Scomparin, Roberta Cavalli
Format: Article
Language:English
Published: MDPI AG 2022-05-01
Series:Antioxidants
Subjects:
Online Access:https://www.mdpi.com/2076-3921/11/5/1007
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author Monica Argenziano
Irfan Aamer Ansari
Elisabetta Muntoni
Rita Spagnolo
Anna Scomparin
Roberta Cavalli
author_facet Monica Argenziano
Irfan Aamer Ansari
Elisabetta Muntoni
Rita Spagnolo
Anna Scomparin
Roberta Cavalli
author_sort Monica Argenziano
collection DOAJ
description <i>Trans</i>-resveratrol, a polyphenolic phytoalexin found in various plant sources, has been the focus of increasing attention in recent years because of its role in the prevention of many human diseases, and particularly because of its antioxidant properties. However, the in vivo effect of <i>trans</i>-resveratrol after oral administration is negligible when compared to its efficacy in vitro, due to its low bioavailability. Moreover, it presents stability issues as it is an extremely photosensitive compound when exposed to light. This work aims to develop lipid-coated nanocrystals in order to improve the antioxidant activity and bioavailability of <i>trans</i>-resveratrol. Lipid-coated <i>trans</i>-resveratrol nanocrystals with sizes lower than 500 nm, spherical shapes and smooth surfaces were obtained via a milling method. They showed a faster dissolution rate than the coarse <i>trans</i>-resveratrol powder. The antioxidant properties of <i>trans</i>-resveratrol were not impaired by the milling process. The in vivo pharmacokinetics of lipid-coated <i>trans</i>-resveratrol nanocrystals were evaluated after oral administration to rats, with a commercial Phytosome<sup>®</sup> formulation being used for comparison purposes. An increase in the <i>trans</i>-resveratrol area under the curve was observed and the lipid-coated nanocrystal formulation led to an enhancement in the oral bioavailability of the compound.
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spelling doaj.art-24208b4913894d1db00c2f1e633cf0052023-11-23T09:52:59ZengMDPI AGAntioxidants2076-39212022-05-01115100710.3390/antiox11051007Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of ResveratrolMonica Argenziano0Irfan Aamer Ansari1Elisabetta Muntoni2Rita Spagnolo3Anna Scomparin4Roberta Cavalli5Department of Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyDepartment of Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyDepartment of Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyDepartment of Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyDepartment of Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, ItalyDepartment of Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Turin, Italy<i>Trans</i>-resveratrol, a polyphenolic phytoalexin found in various plant sources, has been the focus of increasing attention in recent years because of its role in the prevention of many human diseases, and particularly because of its antioxidant properties. However, the in vivo effect of <i>trans</i>-resveratrol after oral administration is negligible when compared to its efficacy in vitro, due to its low bioavailability. Moreover, it presents stability issues as it is an extremely photosensitive compound when exposed to light. This work aims to develop lipid-coated nanocrystals in order to improve the antioxidant activity and bioavailability of <i>trans</i>-resveratrol. Lipid-coated <i>trans</i>-resveratrol nanocrystals with sizes lower than 500 nm, spherical shapes and smooth surfaces were obtained via a milling method. They showed a faster dissolution rate than the coarse <i>trans</i>-resveratrol powder. The antioxidant properties of <i>trans</i>-resveratrol were not impaired by the milling process. The in vivo pharmacokinetics of lipid-coated <i>trans</i>-resveratrol nanocrystals were evaluated after oral administration to rats, with a commercial Phytosome<sup>®</sup> formulation being used for comparison purposes. An increase in the <i>trans</i>-resveratrol area under the curve was observed and the lipid-coated nanocrystal formulation led to an enhancement in the oral bioavailability of the compound.https://www.mdpi.com/2076-3921/11/5/1007<i>trans</i>-resveratrolnanocrystalslipid coatingoral bioavailability
spellingShingle Monica Argenziano
Irfan Aamer Ansari
Elisabetta Muntoni
Rita Spagnolo
Anna Scomparin
Roberta Cavalli
Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol
Antioxidants
<i>trans</i>-resveratrol
nanocrystals
lipid coating
oral bioavailability
title Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol
title_full Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol
title_fullStr Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol
title_full_unstemmed Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol
title_short Lipid-Coated Nanocrystals as a Tool for Improving the Antioxidant Activity of Resveratrol
title_sort lipid coated nanocrystals as a tool for improving the antioxidant activity of resveratrol
topic <i>trans</i>-resveratrol
nanocrystals
lipid coating
oral bioavailability
url https://www.mdpi.com/2076-3921/11/5/1007
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AT elisabettamuntoni lipidcoatednanocrystalsasatoolforimprovingtheantioxidantactivityofresveratrol
AT ritaspagnolo lipidcoatednanocrystalsasatoolforimprovingtheantioxidantactivityofresveratrol
AT annascomparin lipidcoatednanocrystalsasatoolforimprovingtheantioxidantactivityofresveratrol
AT robertacavalli lipidcoatednanocrystalsasatoolforimprovingtheantioxidantactivityofresveratrol