Aqueous injection of quercetin: An approach for confirmation of its direct in vivo cardiovascular effects
Language English Country Netherlands Media print-electronic
Document type Journal Article
PubMed
29474897
DOI
10.1016/j.ijpharm.2018.02.036
PII: S0378-5173(18)30117-0
Knihovny.cz E-resources
- Keywords
- Cardiovascular effects, Injectable aqueous solution, Polyvinylpyrrolidone, Quercetin, Solid dispersion, Solubility enhancement,
- MeSH
- Antihypertensive Agents chemistry pharmacology therapeutic use MeSH
- Biological Availability MeSH
- Chemistry, Pharmaceutical MeSH
- Hypertension drug therapy MeSH
- Injections, Intravenous MeSH
- Blood Pressure drug effects MeSH
- Rats MeSH
- Humans MeSH
- Disease Models, Animal MeSH
- Rats, Inbred SHR MeSH
- Rats, Wistar MeSH
- Povidone chemistry MeSH
- Drug Compounding methods MeSH
- Quercetin chemistry pharmacology therapeutic use MeSH
- Solubility MeSH
- Particle Size MeSH
- Water chemistry MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Humans MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Antihypertensive Agents MeSH
- Povidone MeSH
- Quercetin MeSH
- Water 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.
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