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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/3/743 |
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| author | Laura Di Renzo Antonella Smeriglio Mariarosaria Ingegneri Paola Gualtieri Domenico Trombetta |
| author_facet | Laura Di Renzo Antonella Smeriglio Mariarosaria Ingegneri Paola Gualtieri Domenico Trombetta |
| author_sort | Laura Di Renzo |
| collection | DOAJ |
| 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<sub>max</sub>, T<sub>max</sub>, T<sub>1/2</sub>, AUC<sub>0–440 min</sub>, AUC<sub>0–∞</sub>, AUC<sub>t–∞,</sub> AUC<sub>extrap_pred</sub>, C<sub>last</sub> and K<sub>el</sub>) were calculated. Results showed that DOPET C<sub>max</sub> (5.5 ng/mL) was reached after 123 min (T<sub>max</sub>), with a T<sub>1/2</sub> 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. |
| first_indexed | 2024-03-11T06:01:48Z |
| format | Article |
| id | doaj.art-03860cfbc9534cae8e6aee0ceb0193a4 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T06:01:48Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-03860cfbc9534cae8e6aee0ceb0193a42023-11-17T13:13:45ZengMDPI AGPharmaceutics1999-49232023-02-0115374310.3390/pharmaceutics15030743The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol PharmacokineticsLaura Di Renzo0Antonella Smeriglio1Mariarosaria Ingegneri2Paola Gualtieri3Domenico Trombetta4Section of Clinical Nutrition and Nutrigenomic, Department of Biomedicine and Prevention, University of Tor Vergata, Via Montpellier 1, 00133 Rome, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d’Alcontres 31, 98166 Messina, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d’Alcontres 31, 98166 Messina, ItalySection of Clinical Nutrition and Nutrigenomic, Department of Biomedicine and Prevention, University of Tor Vergata, Via Montpellier 1, 00133 Rome, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Ferdinando Stagno d’Alcontres 31, 98166 Messina, ItalyCurrent 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<sub>max</sub>, T<sub>max</sub>, T<sub>1/2</sub>, AUC<sub>0–440 min</sub>, AUC<sub>0–∞</sub>, AUC<sub>t–∞,</sub> AUC<sub>extrap_pred</sub>, C<sub>last</sub> and K<sub>el</sub>) were calculated. Results showed that DOPET C<sub>max</sub> (5.5 ng/mL) was reached after 123 min (T<sub>max</sub>), with a T<sub>1/2</sub> 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.https://www.mdpi.com/1999-4923/15/3/743hydroxytyrosolpharmaceutical formulationpharmacokineticsbioavailabilityDOPETDOPAC |
| spellingShingle | Laura Di Renzo Antonella Smeriglio Mariarosaria Ingegneri Paola Gualtieri Domenico Trombetta The Pharmaceutical Formulation Plays a Pivotal Role in Hydroxytyrosol Pharmacokinetics Pharmaceutics hydroxytyrosol pharmaceutical formulation pharmacokinetics bioavailability DOPET DOPAC |
| 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 | hydroxytyrosol pharmaceutical formulation pharmacokinetics bioavailability DOPET DOPAC |
| url | https://www.mdpi.com/1999-4923/15/3/743 |
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