Simulating the phase II metabolism of raloxifene on a screen-printed electrode

Vasiliadou, Rafaela; Welham, Kevin J.

doi:10.1139/cjc-2017-0279

Cited by 2 publications

(3 citation statements)

References 23 publications

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“…[ 81 , 82 ] Screen–printed electrodes have also been used for investigations in drug metabolism. [ 83 , 84 ] These are miniaturised and disposable electrode systems operating at ul levels. The electrodes are fabricated from inks or paste and are capable to investigate a range of electrochemical parameters such as stability studies and synthesis.…”

Section: Electrochemistry As a Complementary Technique In Preclinical...mentioning

confidence: 99%

“…Conventional flow cells coupled to MS [75–80] have been used for the mimicry of drug metabolism and simulated successfully a range of oxidation reactions such as dehydrogenation, aromatic hydroxylation, heteroatom oxidation and N‐dealkylation [81,82] . Screen–printed electrodes have also been used for investigations in drug metabolism [83,84] . These are miniaturised and disposable electrode systems operating at ul levels.…”

Section: Electrochemistry As a Complementary Technique In Preclinical...mentioning

confidence: 99%

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The Combination of Electrochemistry and Microfluidic Technology in Drug Metabolism Studies

2022

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Drugs are metabolized within the liver (pH 7.4) by phase I and phase II metabolism. During the process, reactive metabolites can be formed that react covalently with biomolecules and induce toxicity. Identifying and detecting reactive metabolites is an important part of drug development. Preclinical and clinical investigations are conducted to assess the toxicity and safety of a new drug candidate. Electrochemistry coupled to mass spectrometry is an ideal complementary technique to the current preclinical studies, a pure instrumental approach without any purification steps and tedious protocols. The combination of microfluidics with electrochemistry towards the mimicry of drug metabolism offers portability, low volume of reagents and faster reaction times. This review explores the development of microfluidic electrochemical cells for mimicking drug metabolism.

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Section: Electrochemistry As a Complementary Technique In Preclinical...mentioning

confidence: 99%

Section: Electrochemistry As a Complementary Technique In Preclinical...mentioning

confidence: 99%

The Combination of Electrochemistry and Microfluidic Technology in Drug Metabolism Studies

2022

Self Cite

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“…They play a crucial role in environmental monitoring, helping to detect and quantify pollutants [13], in microbiology [14] and in food industry analysis, and are also essential in clinical diagnostics, enabling the measurement of biomarkers and disease-related molecules in blood and urine samples [15]. Although, only carbon SPEs have been successfully employed to mimic the metabolism of eugenol [16], raloxifene [17], and paracetamol [18], efficiently generating both phase I and phase II metabolites of tested drugs. Carbon electrodes remain among the most commonly employed choices.…”

Section: Introductionmentioning

confidence: 99%

Electrochemical Simulation of Phase I Hepatic Metabolism of Voriconazole Using a Screen-Printed Iron(II) Phthalocyanine Electrode

Wroński,

Trawiński,

Skibiński

2023

Pharmaceutics

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Understanding the metabolism of pharmaceutical compounds is a fundamental prerequisite for ensuring their safety and efficacy in clinical use. However, conventional methods for monitoring drug metabolism often come with the drawbacks of being time-consuming and costly. In an ongoing quest for innovative approaches, the application of electrochemistry in metabolism studies has gained prominence as a promising approach for the synthesis and analysis of drug transformation products. In this study, we investigated the hepatic metabolism of voriconazole, an antifungal medication, by utilizing human liver microsomes (HLM) assay coupled with LC-MS. Based on the obtained results, the electrochemical parameters were optimized to simulate the biotransformation reactions. Among the various electrodes tested, the chemometric analysis revealed that the iron(II) phthalocyanine electrode was the most effective in catalyzing the formation of all hepatic voriconazole metabolites. These findings exemplify the potential of phthalocyanine electrodes as an efficient and cost-effective tool for simulating the intricate metabolic processes involved in drug biotransformation, offering new possibilities in the field of pharmaceutical research. Additionally, in silico analysis showed that two detected metabolites may exhibit significantly higher acute toxicity and mutagenic potential than the parent compound.

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Simulating the phase II metabolism of raloxifene on a screen-printed electrode

Cited by 2 publications

References 23 publications

The Combination of Electrochemistry and Microfluidic Technology in Drug Metabolism Studies

The Combination of Electrochemistry and Microfluidic Technology in Drug Metabolism Studies

Electrochemical Simulation of Phase I Hepatic Metabolism of Voriconazole Using a Screen-Printed Iron(II) Phthalocyanine Electrode

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