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Supercritical fluid coating of flavonoids on excipients enhances drug release and antioxidant activity

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机构: [1]School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China [2]The First Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou 510405, PR China [3]Shunde Hospital of Guangzhou University of Chinese Medicine, Foshan 528329, Guangdong, PR China [4]Institute of Infection, Immunity and Inflammation, University of Glasgow, Glasgow G12 8QQ, UK [5]Centre for Formulation Engineering, School of Chemical Engineering, University of Birmingham, Birmingham B15 2TT, UK [6]Department of Chemical and Process Engineering, University of Surrey, Guildford GU2 7XH, UK
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关键词: Flavonoids Naringenin Dihydromyricetin Luteolin Supercritical anti-solvent fluidized bed

摘要:
Supercritical anti-solvent fluidized bed (SAS-FB) technology can be applied to reduce particle size, prevent particle aggregation, and improve the dissolution and bioavailability of poorly soluble drugs. In this work, drug-loaded microparticles of three similar structures, the flavonoids luteolin (LUT), naringenin (NGR), and dihydromyricetin (DMY) were prepared using SAS-FB technology, to explore its effect on the coating of flavonoid particles. Operating temperature, pressure, carrier, solvent, and concentration of drug solution were investigated for their effects on the yield and dissolution of flavonoid particles. The results showed that temperature, pressure, carrier, and drug solution concentration have a large effect on yield. Within the study range, low supercritical CO2 density at higher temperature and lower pressure, a larger surface area carrier, and moderate drug solution concentration led to a higher yield. The effect of the solvent on the yield of flavonoids is a result of multiple factors. Scanning electron microscopy (SEM) images showed that the drug-loaded particles prepared from different carriers and solvents have different precipitations pattern on the carrier surface, and their particle sizes were smaller than unprocessed particles and those prepared by the SAS process. Fluorescence microscopy (FM) results showed that the flavonoids were uniformly coated on the carrier. X-ray powder diffraction (XRPD) results showed that the crystalline morphology of SAS-FB particles remained unchanged after the SAS-FB process, although the diffraction peak intensity decreased. The cumulative dissolution of SAS-FB particles was more than four times faster in the first 5 min than that of the unprocessed flavonoids. The antioxidant activity of SAS-FB processed LUT, NGR and DMY was 1.89-3.78 times, 4.92-10.68 times and 0.99-2.57 times higher than that of the untreated flavonoids, respectively. The approach provides a reference for the application of SAS-FB technology in flavonoids.Copyright © 2023 Elsevier B.V. All rights reserved.

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出版当年[2022]版:
大类 | 2 区 医学
小类 | 2 区 药学
最新[2025]版:
大类 | 2 区 医学
小类 | 2 区 药学
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第一作者机构: [1]School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China
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通讯机构: [1]School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China [2]The First Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou 510405, PR China [6]Department of Chemical and Process Engineering, University of Surrey, Guildford GU2 7XH, UK [*1]The First Affiliated Hospital, Guangzhou University of Chinese Medicine, PR China [*2]School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, 232 University City Ring Road East, Panyu District, Guangzhou 510006, China [*3]Department of Chemical and Process Engineering, Faculty of Engineering and Physical Sciences, University of Surrey, Guildford GU2 7XH, UK
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