Cargando…

The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics

Current evidence supports the use of extra virgin olive oil (EVOO) and its minor components such as hydroxytyrosol or 3,4-dihydroxyphenyl ethanol (DOPET), to improve cardiovascular and metabolic health. Nevertheless, more intervention studies in humans are needed because some gaps remain in its bioa...

Descripción completa

Detalles Bibliográficos
Autores principales: Di Renzo, Laura, Smeriglio, Antonella, Ingegneri, Mariarosaria, Gualtieri, Paola, Trombetta, Domenico
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10059125/
https://www.ncbi.nlm.nih.gov/pubmed/36986604
http://dx.doi.org/10.3390/pharmaceutics15030743
_version_ 1785016799861932032
author Di Renzo, Laura
Smeriglio, Antonella
Ingegneri, Mariarosaria
Gualtieri, Paola
Trombetta, Domenico
author_facet Di Renzo, Laura
Smeriglio, Antonella
Ingegneri, Mariarosaria
Gualtieri, Paola
Trombetta, Domenico
author_sort Di Renzo, Laura
collection PubMed
description Current evidence supports the use of extra virgin olive oil (EVOO) and its minor components such as hydroxytyrosol or 3,4-dihydroxyphenyl ethanol (DOPET), to improve cardiovascular and metabolic health. Nevertheless, more intervention studies in humans are needed because some gaps remain in its bioavailability and metabolism. The aim of this study was to investigate the DOPET pharmacokinetics on 20 healthy volunteers by administering a hard enteric-coated capsule containing 7.5 mg of bioactive compound conveyed in EVOO. The treatment was preceded by a washout period with a polyphenol and an alcohol-free diet. Blood and urine samples were collected at baseline and different time points, and free DOPET and metabolites, as well as sulfo- and glucuro-conjugates, were quantified by LC-DAD-ESI-MS/MS analysis. The plasma concentration versus time profiles of free DOPET was analyzed by a non-compartmental approach, and several pharmacokinetic parameters (C(max), T(max), T(1/2), AUC(0–440 min), AUC(0–∞), AUC(t–∞,) AUC(extrap_pred), C(last) and K(el)) were calculated. Results showed that DOPET C(max) (5.5 ng/mL) was reached after 123 min (T(max)), with a T(1/2) of 150.53 min. Comparing the data obtained with the literature, the bioavailability of this bioactive compound is about 2.5 times higher, confirming the hypothesis that the pharmaceutical formulation plays a pivotal role in the bioavailability and pharmacokinetics of hydroxytyrosol.
format Online
Article
Text
id pubmed-10059125
institution National Center for Biotechnology Information
language English
publishDate 2023
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-100591252023-03-30 The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics Di Renzo, Laura Smeriglio, Antonella Ingegneri, Mariarosaria Gualtieri, Paola Trombetta, Domenico Pharmaceutics Article Current evidence supports the use of extra virgin olive oil (EVOO) and its minor components such as hydroxytyrosol or 3,4-dihydroxyphenyl ethanol (DOPET), to improve cardiovascular and metabolic health. Nevertheless, more intervention studies in humans are needed because some gaps remain in its bioavailability and metabolism. The aim of this study was to investigate the DOPET pharmacokinetics on 20 healthy volunteers by administering a hard enteric-coated capsule containing 7.5 mg of bioactive compound conveyed in EVOO. The treatment was preceded by a washout period with a polyphenol and an alcohol-free diet. Blood and urine samples were collected at baseline and different time points, and free DOPET and metabolites, as well as sulfo- and glucuro-conjugates, were quantified by LC-DAD-ESI-MS/MS analysis. The plasma concentration versus time profiles of free DOPET was analyzed by a non-compartmental approach, and several pharmacokinetic parameters (C(max), T(max), T(1/2), AUC(0–440 min), AUC(0–∞), AUC(t–∞,) AUC(extrap_pred), C(last) and K(el)) were calculated. Results showed that DOPET C(max) (5.5 ng/mL) was reached after 123 min (T(max)), with a T(1/2) of 150.53 min. Comparing the data obtained with the literature, the bioavailability of this bioactive compound is about 2.5 times higher, confirming the hypothesis that the pharmaceutical formulation plays a pivotal role in the bioavailability and pharmacokinetics of hydroxytyrosol. MDPI 2023-02-23 /pmc/articles/PMC10059125/ /pubmed/36986604 http://dx.doi.org/10.3390/pharmaceutics15030743 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Di Renzo, Laura
Smeriglio, Antonella
Ingegneri, Mariarosaria
Gualtieri, Paola
Trombetta, Domenico
The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics
title The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics
title_full The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics
title_fullStr The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics
title_full_unstemmed The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics
title_short The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics
title_sort pharmaceutical formulation plays a pivotal role in hydroxytyrosol pharmacokinetics
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10059125/
https://www.ncbi.nlm.nih.gov/pubmed/36986604
http://dx.doi.org/10.3390/pharmaceutics15030743
work_keys_str_mv AT direnzolaura thepharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT smeriglioantonella thepharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT ingegnerimariarosaria thepharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT gualtieripaola thepharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT trombettadomenico thepharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT direnzolaura pharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT smeriglioantonella pharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT ingegnerimariarosaria pharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT gualtieripaola pharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics
AT trombettadomenico pharmaceuticalformulationplaysapivotalroleinhydroxytyrosolpharmacokinetics