Aqueous injection of quercetin: An approach for confirmation of its direct in vivo cardiovascular effects
Jazyk angličtina Země Nizozemsko Médium print-electronic
Typ dokumentu časopisecké články
PubMed
29474897
DOI
10.1016/j.ijpharm.2018.02.036
PII: S0378-5173(18)30117-0
Knihovny.cz E-zdroje
- Klíčová slova
- Cardiovascular effects, Injectable aqueous solution, Polyvinylpyrrolidone, Quercetin, Solid dispersion, Solubility enhancement,
- MeSH
- antihypertenziva chemie farmakologie terapeutické užití MeSH
- biologická dostupnost MeSH
- farmaceutická chemie MeSH
- hypertenze farmakoterapie MeSH
- injekce intravenózní MeSH
- krevní tlak účinky léků MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- modely nemocí na zvířatech MeSH
- potkani inbrední SHR MeSH
- potkani Wistar MeSH
- povidon chemie MeSH
- příprava léků metody MeSH
- quercetin chemie farmakologie terapeutické užití MeSH
- rozpustnost MeSH
- velikost částic MeSH
- voda chemie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antihypertenziva MeSH
- povidon MeSH
- quercetin MeSH
- voda MeSH
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.
Citace poskytuje Crossref.org
