Pharmacokinetics of quercetin-loaded nanodroplets with ultrasound activation and&amp;nbsp;their&amp;nbsp;use for bioimaging

Chang, Li‐Chun; Hou, Mei; Hung, Shuo-Hui; Lin, Lie Chwen; Tsai, Tung Hu

doi:10.2147/ijn.s78983

Cited by 5 publications

(1 citation statement)

References 57 publications

(63 reference statements)

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“…Data points represent mean ± SEM (n ≥ 4, where n is the number of mice per treatment group) Therefore, it is not surprising that efforts have been invested to develop alternative quercetin formulations. For example, when compared to free quercetin, liposomal quercetin formulations often displayed improved blood circulation and decreased rates of elimination from the plasma compartment [24,25,36]. In these previous studies, quercetin was formulated into liposomes passively when the liposomes are first made.…”

Section: Discussionmentioning

confidence: 99%

Characterization of a liposomal copper(II)-quercetin formulation suitable for parenteral use

Chen

Anantha

Leung

et al. 2019

Drug Deliv. and Transl. Res.

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Quercetin (3,3′,4′,5,7-pentahydroxyflavone) is a naturally derived flavonoid that is commonly found in fruits and vegetables. There is mounting evidence to suggest that quercetin has potential anticancer effects and appears to interact synergistically when used in combination with approved chemotherapeutic agents such as irinotecan and cisplatin. Unfortunately, quercetin has shown limited clinical utility, partly due to low bioavailability related to its poor aqueous solutions (< 10 μg/mL). In this study, liposomal formulations of quercetin were developed by exploiting quercetin's ability to bind copper. Quercetin powder was added directly to pre-formed copper-containing liposomes (2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and cholesterol (CHOL) (55:45 M ratio)). As a function of time and temperature, the formation of copper-quercetin was measured. Using this methodology, a final quercetin-to-lipid (mol:mol) ratio of 0.2 was achievable and solutions containing quercetin at concentrations of > 5 mg/mL were attained, representing at least a > 100-fold increase in apparent solubility. The resulting formulation was suitable for intravenous dosing with no overt toxicities when administered at doses of 50 mg/kg in mice. Pharmacokinetic studies demonstrated that the copper-quercetin formulations had an AUC 0-24H of 8382.1 μg h/mL when administered to mice at 50 mg/kg. These studies suggested that quercetin (not copper-quercetin) dissociates from the liposomes after administration. The resulting formulation is suitable for further development and also serves as a proof-of-concept for formulating other flavonoids and flavonoid-like compounds. Given that quercetin exhibits an IC 50 of >10 μM when tested against cancer cell lines, we believe that the utility of this novel quercetin formulation for cancer indications will ultimately be as a component of a combination product.

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Section: Discussionmentioning

confidence: 99%

Characterization of a liposomal copper(II)-quercetin formulation suitable for parenteral use

Chen

Anantha

Leung

et al. 2019

Drug Deliv. and Transl. Res.

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Quercetin as a protective agent for liver diseases: A comprehensive descriptive review of the molecular mechanism

Zhao

Wang

Deng

et al. 2021

Phytotherapy Research

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Quercetin is the major representative of the flavonoid subgroup of flavones, with good pharmacological activities for the treatment of liver diseases, including liver steatosis, fatty hepatitis, liver fibrosis, and liver cancer. It can significantly influence the development of liver diseases via multiple targets and multiple pathways via antifat accumulation, anti‐inflammatory, and antioxidant activity, as well as the inhibition of cellular apoptosis and proliferation. Despite extensive research on understanding the mechanism of quercetin in the treatment of liver diseases, there are still no targeted therapies available. Thus, we have comprehensively searched and summarized the different targets of quercetin in different stages of liver diseases and concluded that quercetin inhibited inflammation of the liver mainly through NF‐κB/TLR/NLRP3, reduced PI3K/Nrf2‐mediated oxidative stress, mTOR activation in autophagy, and inhibited the expression of apoptotic factors associated with the development of liver diseases. In addition, quercetin showed different mechanisms of action at different stages of liver diseases, including the regulation of PPAR, UCP, and PLIN2‐related factors via brown fat activation in liver steatosis. The compound inhibited stromal ECM deposition at the liver fibrosis stage, affecting TGF1β, endoplasmic reticulum stress (ERs), and apoptosis. While at the final liver cancer stage, inhibiting cancer cell proliferation and spread via the hTERT, MEK1/ERK1/2, Notch, and Wnt/β‐catenin‐related signaling pathways. In conclusion, quercetin is an effective liver protectant. We hope to explore the pathogenesis of quercetin in different stages of liver diseases through the review, so as to provide more accurate targets and theoretical basis for further research of quercetin in the treatment of liver diseases.

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Echographic and physical characterization of albumin-stabilized nanobubbles

Watanabe

Sheng

Endo

et al. 2019

Heliyon

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There has been increasing interest in using nanobubbles (NBs) for ultrasound mediated drug delivery as well as for ultrasound imaging. Albumin NBs are especially attractive for its potential of becoming a versatile platform for drug carriers and molecular targeted therapy agents. However, physical characterization of NBs is generally considered to be difficult due to various technical issues, such as concentration limitations, nanoparticle contamination, etc. In the present study, we measured the size distribution, concentration and weight density of albumin stabilized NBs by means of multiple nanoscale measurement modalities. Laser nanoparticle tracking analysis, multicolor flow cytometry, resonance mass evaluation showed consistent measurement results of the NBs with low mass weight density and diameter size ranging from 100 nm to 400 nm. Furthermore, the NB solution showed excellent images by high frequency ultrasound (30-50 MHz) in flow model acoustic phantoms. The NBs also induced acute cell disruption by low intensity ultrasound (0.8 W/cm 2) irradiation. We successfully fabricated and characterized albumin stabilized NBs which could serve as an effective platform for future theranositic agents.

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

Cited by 5 publications

References 57 publications

Characterization of a liposomal copper(II)-quercetin formulation suitable for parenteral use

Characterization of a liposomal copper(II)-quercetin formulation suitable for parenteral use

Quercetin as a protective agent for liver diseases: A comprehensive descriptive review of the molecular mechanism

Echographic and physical characterization of albumin-stabilized nanobubbles

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