Quercetin nanocrystals stabilized by glycyrrhizic acid for liver targeted drug delivery: impact of glycyrrhizic acid concentrations.

IF 2.6 4区医学 Q2 PHARMACOLOGY & PHARMACY

Pharmaceutical Development and Technology Pub Date : 2025-05-01 DOI:10.1080/10837450.2025.2498370

Fengxia Wang, Chengying Shen, Fangwen Chen, Jinyun Cao, Pengfei Yue, Baode Shen

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Abstract

The purpose of this study was to investigate the impact of glycyrrhizic acid (GL) concentrations on in vitro and in vivo behavior of quercetin (QT) nanocrystals stabilized by GL (QT-NCs/GL), with a particular focus on its influence on liver targeted drug delivery. QT-NCs/GL with similar particle size around 200 nm were successfully prepared by media milling technique using different concentrations of GL, which were 10%, 20% and 40% (w/w) of the QT. All QT-NCs/GL showed oval and rod shapes, and remained in crystalline state with a reduced crystallinity as GL concentrations increased. All QT-NCs/GL exhibited significant solubility increase and drug release improvement of QT as compared to raw QT. Pharmacokinetics revealed similar plasma concentration-time profiles of QT after intravenous of all QT-NCs/GL. All QT-NCs/GL exhibited rapidly distribution of QT to liver with the maximum QT concentration more than 750 μg/g at 5 min after intravenous administration, and the AUC0∼t of QT for three formulations in liver were significant difference with the following order: QT-NCs/GL-40% > QT-NCs/GL-20% > QT-NCs/GL-10%. These results suggested that different GL concentrations exhibited significant influence on liver targeted delivery of QT-NCs/GL, and more GL used in QT-NCs/GL may contribute more liver distribution of QT.

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甘草酸稳定的槲皮素纳米晶体用于肝脏靶向药物递送：甘草酸浓度的影响。

本研究的目的是研究甘草酸（GL）浓度对GL稳定槲皮素（QT）纳米晶体（QT- nc /GL）体内外行为的影响，特别关注其对肝脏靶向给药的影响。采用介质碾磨技术，分别为QT的10%、20%和40% (w/w)，成功制备出粒径相近、粒径约为200 nm的QT- nc /GL，所有QT- nc /GL均呈椭圆形和棒状，且随着GL浓度的增加，其结晶度逐渐降低。与未处理的QT相比，所有QT- nc /GL的溶解度和药物释放均显著增加，药物动力学显示静脉注射所有QT- nc /GL后QT的血浆浓度-时间曲线相似。所有QT- ncs /GL均表现出快速的肝脏QT分布，静脉给药后5min最大QT浓度均大于750 μg/g，三种剂型的肝脏QT AUC0 ~ t差异有统计学意义，顺序为：QT- ncs /GL-40% > QT- ncs /GL-20% > QT- ncs /GL-10%。上述结果提示，不同GL浓度对QT- ncs /GL的肝脏靶向递送有显著影响，QT- ncs /GL使用的GL越多，QT在肝脏的分布可能越大。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Pharmaceutical Development and Technology 医学-药学

CiteScore

5.90

自引率

2.90%

发文量

审稿时长

1 months

期刊介绍： Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.