Pharmacokinetics of quercetin-loaded nanodroplets with ultrasound activation and their use for bioimaging

• Published in: International journal of nanomedicine Vol. 10; pp. 3031 - 3042
• Main Authors: Chang, Li-Wen, Hou, Mei-Ling, Hung, Shuo-Hui, Lin, Lie-Chwen, Tsai, Tung-Hu
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01.01.2015; Taylor & Francis Ltd; Dove Medical Press
• Subjects: Bioavailability; Bubbles; Chemical properties; Complications and side effects; Contrast agents; Cytotoxicity; Design; Dosage and administration; Drugs; Lipids; Medical imaging; Medicine; Metabolism; Molecular Imaging - methods; Molecular weight; Nanoparticles; Nanoparticles - chemistry; Nanoparticles - radiation effects; Nanotechnology; Optical properties; Original Research; Particle size; Pharmacokinetics; Pharmacy; Polyethylene glycol; Quercetin; Quercetin - chemistry; Quercetin - pharmacokinetics; Quercetin - radiation effects; Ultrasonic imaging; Ultrasonic Waves; Taiwan; United States > US; Japan; nanodroplets; quercetin; ultrasonic pharmacokinetics; ultrasonic imaging; ultrasound
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S78983

Bubble formulations have both diagnostic and therapeutic applications. However, research on nanobubbles/nanodroplets remains in the initial stages. In this study, a nanodroplet formulation was prepared and loaded with a novel class of chemotherapeutic drug, ie, quercetin, to observe its pharmacokinetic properties and ultrasonic bioimaging of specific sites, namely the abdominal vein and bladder. Four parallel groups were designed to investigate the effects of ultrasound and nanodroplets on the pharmacokinetics of quercetin. These groups were quercetin alone, quercetin triggered with ultrasound, quercetin-encapsulated in nanodroplets, and quercetin encapsulated in nanodroplets triggered with ultrasound. Spherical vesicles with a mean diameter of 280 nm were formed, and quercetin was completely encapsulated within. In vivo ultrasonic imaging confirmed that the nanodroplets could be treated by ultrasound. The results indicate that the initial 5-minute serum concentration, area under the concentration-time curve, elimination half-life, and clearance of quercetin were significantly enhanced by nanodroplets with or without ultrasound.