RT info:eu-repo/semantics/article
T1 A micellar formulation of quercetin prevents cisplatin nephrotoxicity
A1 Casanova, Alfredo G.
A1 Prieto, Marta
A1 Colino, Clara I.
A1 Gutiérrez Millán, Carmen
A1 Ruszkowska Ciastek, Barbara
A1 Paz Barragán, Esther de
A1 Gil Martínez, Miguel Ángel
A1 Morales Martin, Ana I.
A1 Lopez Hernandez, Francisco J.
K1 Cisplatin - Chemotherapy
K1 Nephrology
K1 Kidneys - Diseases
K1 Riñones - Enfermedades - Tratamiento
K1 Quercetina - Uso terapéutico
K1 Bioavailability
K1 Medicamentos - Biodisponibilidad
K1 Chemical processes
K1 Química - Notación
K1 3208.06 Quimioterapia
K1 3205.06 Nefrología
K1 3303 Ingeniería y Tecnología Químicas
AB The antioxidant flavonoid quercetin has been shown to prevent nephrotoxicity in animal models and in a clinical study and is thus a very promising prophylactic candidate under development. Quercetin solubility is very low, which handicaps clinical application. The aim of this work was to study, in rats, the bioavailability and nephroprotective efficacy of a micellar formulation of Pluronic F127-encapsulated quercetin (P-quercetin), with improved hydrosolubility. Intraperitoneal administration of P-quercetin leads to an increased plasma concentration and bioavailability of quercetin compared to the equimolar administration of natural quercetin. Moreover, P-quercetin retains overall nephroprotective properties, and even slightly improves some renal function parameters, when compared to natural quercetin. Specifically, P-quercetin reduced the increment in plasma creatinine (from 3.4 ± 0.5 to 1.2 ± 0.3 mg/dL) and urea (from 490.9 ± 43.8 to 184.1 ± 50.1 mg/dL) and the decrease in creatinine clearance (from 0.08 ± 0.02 to 0.58 ± 0.19 mL/min) induced by the nephrotoxic chemotherapeutic drug cisplatin, and it ameliorated histological evidence of tubular damage. This new formulation with enhanced kinetic and biopharmaceutical properties will allow for further exploration of quercetin as a candidate nephroprotector at lower dosages and by administration routes oriented towards its clinical use.
PB MDPI
SN 1422-0067
YR 2021
FD 2021
LK https://uvadoc.uva.es/handle/10324/59863
UL https://uvadoc.uva.es/handle/10324/59863
LA eng
NO International Journal of Molecular Sciences, 2021, Vol. 22, Nº. 2, 729
NO Producción Científica
DS UVaDOC
RD 01-jun-2024