Preparation, physicochemical characterization, and antioxidant effects of quercetin nanoparticles

• Published in: International journal of pharmaceutics Vol. 346; no. 1; pp. 160 - 168
• Main Authors: Wu, Tzu-Hui, Yen, Feng-Lin, Lin, Liang-Tzung, Tsai, Tong-Rong, Lin, Chun-Ching, Cham, Thau-Ming
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 04.01.2008
• Subjects: 1-Octanol - chemistry; 1H nuclear magnetic resonance; Animals; Anti-lipid peroxidation; Antioxidants - chemistry; Antioxidants - metabolism; Biphenyl Compounds - chemistry; Calorimetry, Differential Scanning; Drug Compounding; Free radical-scavenging activity; Gastric Juice - chemistry; Hydrazines - chemistry; Lipid Peroxidation; Liver - metabolism; Magnetic Resonance Spectroscopy; Microscopy, Electron, Transmission; Nanoparticles; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Particle Size; Picrates; Quercetin; Quercetin - chemistry; Quercetin - metabolism; Rats; Solubility; Spectroscopy, Fourier Transform Infrared; Superoxides - chemistry; Water - chemistry; X-Ray Diffraction; Xanthine Oxidase - chemistry; Nanoparticles; Free radical-scavenging activity; 1H nuclear magnetic resonance; Anti-lipid peroxidation; Quercetin
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2007.06.036

The purpose of this study was to develop quercetin-loaded nanoparticles (QUEN) by a nanoprecipitation technique with Eudragit ® E (EE) and polyvinyl alcohol (PVA) as carriers, and to evaluate the antioxidant effects of quercetin (QU) and of its nanoparticles. The novel QUEN systems were characterized by particle size and morphology, yield and encapsulation efficiency, differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), 1H nuclear magnetic resonance ( 1H NMR), and dissolution study. It was observed that the weight ratio of QU:EE:PVA at 1:10:10 carried a particle size of <85 nm, a particle distribution with polydispersity index <0.3, and its yield and encapsulation efficiency were over 99%. The results from XRD and DSC of the QUEN showed that the crystal of the drug might be converted to an amorphous state. The FT-IR and 1H NMR demonstrated that QU formed intermolecular hydrogen bonding with carriers. The release of the drug from the QUEN was 74-fold higher compared with the pure drug. In addition, the antioxidant activity of the QUEN was more effective than pure QU on DPPH scavenging, anti-superoxide formation, superoxide anion scavenging, and anti-lipid peroxidation.