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Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol

Resveratrol attracts great interest because of the plethora of in vitro effects at the micromolar concentration range. Unfortunately, these effects are difficult to establish in vivo, due to the low concentration of resveratrol reached. This discrepancy is due to the molecules low solubility in wate...

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Autores principales: Iannitti, Rossana Giulietta, Floridi, Alessandro, Lazzarini, Andrea, Tantucci, Alice, Russo, Roberta, Ragonese, Francesco, Monarca, Lorenzo, Caglioti, Concetta, Spogli, Roberto, Leonardi, Lucio, De Angelis, Massimiliano, Palazzetti, Federico, Fioretti, Bernard
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8377765/
https://www.ncbi.nlm.nih.gov/pubmed/34422874
http://dx.doi.org/10.3389/fnut.2020.570047
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author Iannitti, Rossana Giulietta
Floridi, Alessandro
Lazzarini, Andrea
Tantucci, Alice
Russo, Roberta
Ragonese, Francesco
Monarca, Lorenzo
Caglioti, Concetta
Spogli, Roberto
Leonardi, Lucio
De Angelis, Massimiliano
Palazzetti, Federico
Fioretti, Bernard
author_facet Iannitti, Rossana Giulietta
Floridi, Alessandro
Lazzarini, Andrea
Tantucci, Alice
Russo, Roberta
Ragonese, Francesco
Monarca, Lorenzo
Caglioti, Concetta
Spogli, Roberto
Leonardi, Lucio
De Angelis, Massimiliano
Palazzetti, Federico
Fioretti, Bernard
author_sort Iannitti, Rossana Giulietta
collection PubMed
description Resveratrol attracts great interest because of the plethora of in vitro effects at the micromolar concentration range. Unfortunately, these effects are difficult to establish in vivo, due to the low concentration of resveratrol reached. This discrepancy is due to the molecules low solubility in water that favors the propensity for an intestinal absorption rather than in the gastric compartment. To address these challenges, we developed a Solid Dispersion of Resveratrol Supported by Magnesium Di Hydroxide formulation (Resv@MDH). This formulation displays increased water solubility and better bioavailability relative to pure resveratrol in the rabbit animal model. In our study, we evaluated the pharmacokinetics profile of resveratrol in six healthy human subjects following 180 mg of oral resveratrol administration, derived from Resv@MDH or pure resveratrol. Free resveratrol was evaluated in the whole blood sample by using HPLC - MS/MS. In comparison with pure resveratrol that displays an increase of the maximum plasma concentration, Cmax at about 90 min and 2 μM, Resv@MDH displays an earlier peak of resveratrol concentration with an increase of Cmax at about 30 min and 6 μM. The different kinetics suggest a main gastric route for resveratrol absorption from Resv@MDH, where, because of its improved dissolution rate, there seems to be a higher propensity for an acidic environment, as opposed to that with pure resveratrol. This conclusion is also supported by the numerical simulation analysis, which considers the principal steps during the oral route administration. Moreover, there is a 2-fold increase in the amount of free resveratrol with respect to pure resveratrol confirming a better bioavailability observed in the animal model. The characteristic feature of the pharmacokinetic profile of Resv@MDH implies that the beneficial properties of resveratrol in human health should be capitalized on it.
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spelling pubmed-83777652021-08-21 Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol Iannitti, Rossana Giulietta Floridi, Alessandro Lazzarini, Andrea Tantucci, Alice Russo, Roberta Ragonese, Francesco Monarca, Lorenzo Caglioti, Concetta Spogli, Roberto Leonardi, Lucio De Angelis, Massimiliano Palazzetti, Federico Fioretti, Bernard Front Nutr Nutrition Resveratrol attracts great interest because of the plethora of in vitro effects at the micromolar concentration range. Unfortunately, these effects are difficult to establish in vivo, due to the low concentration of resveratrol reached. This discrepancy is due to the molecules low solubility in water that favors the propensity for an intestinal absorption rather than in the gastric compartment. To address these challenges, we developed a Solid Dispersion of Resveratrol Supported by Magnesium Di Hydroxide formulation (Resv@MDH). This formulation displays increased water solubility and better bioavailability relative to pure resveratrol in the rabbit animal model. In our study, we evaluated the pharmacokinetics profile of resveratrol in six healthy human subjects following 180 mg of oral resveratrol administration, derived from Resv@MDH or pure resveratrol. Free resveratrol was evaluated in the whole blood sample by using HPLC - MS/MS. In comparison with pure resveratrol that displays an increase of the maximum plasma concentration, Cmax at about 90 min and 2 μM, Resv@MDH displays an earlier peak of resveratrol concentration with an increase of Cmax at about 30 min and 6 μM. The different kinetics suggest a main gastric route for resveratrol absorption from Resv@MDH, where, because of its improved dissolution rate, there seems to be a higher propensity for an acidic environment, as opposed to that with pure resveratrol. This conclusion is also supported by the numerical simulation analysis, which considers the principal steps during the oral route administration. Moreover, there is a 2-fold increase in the amount of free resveratrol with respect to pure resveratrol confirming a better bioavailability observed in the animal model. The characteristic feature of the pharmacokinetic profile of Resv@MDH implies that the beneficial properties of resveratrol in human health should be capitalized on it. Frontiers Media S.A. 2020-11-13 /pmc/articles/PMC8377765/ /pubmed/34422874 http://dx.doi.org/10.3389/fnut.2020.570047 Text en Copyright © 2020 Iannitti, Floridi, Lazzarini, Tantucci, Russo, Ragonese, Monarca, Caglioti, Spogli, Leonardi, De Angelis, Palazzetti and Fioretti. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Nutrition
Iannitti, Rossana Giulietta
Floridi, Alessandro
Lazzarini, Andrea
Tantucci, Alice
Russo, Roberta
Ragonese, Francesco
Monarca, Lorenzo
Caglioti, Concetta
Spogli, Roberto
Leonardi, Lucio
De Angelis, Massimiliano
Palazzetti, Federico
Fioretti, Bernard
Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol
title Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol
title_full Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol
title_fullStr Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol
title_full_unstemmed Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol
title_short Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Represents an Oral Formulation of Resveratrol With Better Gastric Absorption and Bioavailability Respect to Pure Resveratrol
title_sort resveratrol supported on magnesium dihydroxide (resv@mdh) represents an oral formulation of resveratrol with better gastric absorption and bioavailability respect to pure resveratrol
topic Nutrition
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8377765/
https://www.ncbi.nlm.nih.gov/pubmed/34422874
http://dx.doi.org/10.3389/fnut.2020.570047
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