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Aqueous injection of quercetin: An approach for confirmation of its direct in vivo cardiovascular effects

EP. Porcu, M. Cossu, G. Rassu, P. Giunchedi, G. Cerri, J. Pourová, I. Najmanová, T. Migkos, V. Pilařová, L. Nováková, P. Mladěnka, E. Gavini,

. 2018 ; 541 (1-2) : 224-233. [pub] 20180221

Language English Country Netherlands

Document type Journal Article

Persistent link   https://www.medvik.cz/link/bmc18033290

Potential positive effects of flavonol quercetin on humans were suggested by many studies. However, it is not clear if these effects are mediated by quercetin or its metabolites. The in vivo confirmation of quercetin effects is largely hindered by its low water solubility and thus impossibility to test directly its impact. Therefore, a solid dispersion of quercetin with polyvinylpyrrolidone (PVP) was developed to prepare an injectable formulation of water-soluble quercetin. The optimized formulation provided a 20,000-fold increase in quercetin solubility. This formulation was tested on conventional and spontaneously hypertensive rats; it lowered their blood pressure in both short- and long-term basis. Pharmacokinetic data are also provided. This study reports for the first time an injectable water-soluble formulation of quercetin suitable for confirmation of its vascular effect in vivo.

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$a Porcu, Elena Piera $u Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. Electronic address: elena.piera1988@gmail.com.
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$a Aqueous injection of quercetin: An approach for confirmation of its direct in vivo cardiovascular effects / $c EP. Porcu, M. Cossu, G. Rassu, P. Giunchedi, G. Cerri, J. Pourová, I. Najmanová, T. Migkos, V. Pilařová, L. Nováková, P. Mladěnka, E. Gavini,
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$a Potential positive effects of flavonol quercetin on humans were suggested by many studies. However, it is not clear if these effects are mediated by quercetin or its metabolites. The in vivo confirmation of quercetin effects is largely hindered by its low water solubility and thus impossibility to test directly its impact. Therefore, a solid dispersion of quercetin with polyvinylpyrrolidone (PVP) was developed to prepare an injectable formulation of water-soluble quercetin. The optimized formulation provided a 20,000-fold increase in quercetin solubility. This formulation was tested on conventional and spontaneously hypertensive rats; it lowered their blood pressure in both short- and long-term basis. Pharmacokinetic data are also provided. This study reports for the first time an injectable water-soluble formulation of quercetin suitable for confirmation of its vascular effect in vivo.
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$a Cossu, Massimo $u Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. Electronic address: mcossu@uniss.it.
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$a Rassu, Giovanna $u Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. Electronic address: grassu@uniss.it.
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$a Giunchedi, Paolo $u Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. Electronic address: pgiunc@uniss.it.
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$a Cerri, Guido $u Department of Architecture, Design and Urban Planning - GeoMaterials Lab, University of Sassari, Sassari, Italy. Electronic address: gcerri@uniss.it.
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$a Pourová, Jana $u Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic. Electronic address: pourova@faf.cuni.cz.
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$a Najmanová, Iveta $u Department of Biological and Medical Sciences, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic. Electronic address: najmanoi@faf.cuni.cz.
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$a Migkos, Thomas $u Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic. Electronic address: migkost@faf.cuni.cz.
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$a Pilařová, Veronika $u Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic. Electronic address: pilarovv@faf.cuni.cz.
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$a Nováková, Lucie $u Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic. Electronic address: novakoval@faf.cuni.cz.
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$a Mladěnka, Přemysl $u Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic. Electronic address: mladenkap@faf.cuni.cz.
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$a Gavini, Elisabetta $u Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy. Electronic address: eligav@uniss.it.
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