A Micellar Formulation of Quercetin Prevents Cisplatin Nephrotoxicity
| Autor: | Alfredo G. Casanova, Marta Prieto, Francisco J. López-Hernández, Ángel Martín, Carmen Gutierrez-Millan, Esther de Paz, Ana I. Morales, Clara I. Colino, Barbara Ruszkowska-Ciastek |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
Antioxidant medicine.medical_treatment Flavonoid cisplatin Pharmacology Kidney Function Tests Antioxidants quercetin lcsh:Chemistry chemistry.chemical_compound 0302 clinical medicine heterocyclic compounds lcsh:QH301-705.5 Spectroscopy chemistry.chemical_classification Kidney nephroprotection 3205.06 Nefrología Chemistry nephrotoxicity General Medicine Immunohistochemistry Cisplatin - Chemotherapy Computer Science Applications 3303 Ingeniería y Tecnología Químicas medicine.anatomical_structure Nephrology 030220 oncology & carcinogenesis 3208.06 Quimioterapia Riñones - Enfermedades - Tratamiento Quercetin medicine.drug kidney micelles Drug Compounding Chemical processes Medicamentos - Biodisponibilidad Biological Availability Renal function Antineoplastic Agents formulation Protective Agents Article Catalysis Nephrotoxicity Inorganic Chemistry 03 medical and health sciences Kidneys - Diseases medicine flavonoid Physical and Theoretical Chemistry Molecular Biology Cisplatin solubility Organic Chemistry Química - Notación Bioavailability 030104 developmental biology lcsh:Biology (General) lcsh:QD1-999 Quercetina - Uso terapéutico bioavailability Biomarkers |
| Zdroj: | International Journal of Molecular Sciences, Vol 22, Iss 729, p 729 (2021) International Journal of Molecular Sciences Volume 22 Issue 2 |
| ISSN: | 1661-6596 1422-0067 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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