• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

甘草酸稳定的槲皮素纳米晶体用于肝脏靶向给药的制备及其体外/体内评价

Fabrication and in vitro/vivo evaluation of quercetin nanocrystals stabilized by glycyrrhizic acid for liver targeted drug delivery.

作者信息

Shen Baode, Zhu Yuwen, Wang Fengxia, Deng Xiang, Yue Pengfei, Yuan Hailong, Shen Chenying

机构信息

Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China.

Department of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, China.

出版信息

Int J Pharm X. 2024 Apr 9;7:100246. doi: 10.1016/j.ijpx.2024.100246. eCollection 2024 Jun.

DOI:10.1016/j.ijpx.2024.100246
PMID:38628619
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11019285/
Abstract

The purpose of this study was to design novel drug nanocrystals (NCs) stabilized by glycyrrhizic acid (GL) for achieving liver targeted drug delivery due to the presence of GL receptor in the hepatocytes. Quercetin (QT) exhibits good pharmacological activities for the treatment of liver diseases, including liver steatosis, fatty hepatitis, liver fibrosis, and liver cancer. It was selected as a model drug owing to its poor water solubility. QT NCs stabilized by GL (QT-NCs/GL) were fabricated by wet media milling technique and systemically evaluated. QT-NCs stabilized by poloxamer 188 (QT-NCs/P188) were prepared as a reference for comparison of in vitro and in vivo performance with QT-NCs/GL. QT-NCs/GL and QT-NCs/P188 with similar particle size around 130 nm were successfully fabricated by wet media milling technique. Both of QT-NCs/GL and QT-NCs/P188 showed irregular particles and short rods under SEM. XRPD revealed that QT-NCs/GL and QT-NCs/P188 remained in crystalline state with reduced crystallinity. QT-NCs/GL and QT-NCs/P188 exhibited significant solubility increase and drug release improvement of QT as compared to raw QT. No significant difference for the plasma concentration-time curves and pharmacokinetic parameters of QT were found following intravenous administration of QT-NCs/GL and QT-NCs/P188. However, a significantly higher liver distribution of QT following intravenous administration of QT-NCs/GL was observed in comparison to QT-NCs/P188, indicating QT-NCs stabilized by GL could achieve liver targeted delivery of QT. It could be concluded that GL used as stabilizer of QT NCs have a great potential for liver targeted drug delivery.

摘要

本研究的目的是设计由甘草酸（GL）稳定的新型药物纳米晶体（NCs），由于肝细胞中存在GL受体，可实现肝脏靶向给药。槲皮素（QT）对包括肝脂肪变性、脂肪性肝炎、肝纤维化和肝癌在内的肝脏疾病具有良好的药理活性。由于其水溶性差，它被选为模型药物。通过湿介质研磨技术制备了由GL稳定的QT NCs（QT-NCs/GL）并进行了系统评价。制备了由泊洛沙姆188稳定的QT-NCs（QT-NCs/P188）作为与QT-NCs/GL进行体外和体内性能比较的参考。通过湿介质研磨技术成功制备了粒径约为130nm的QT-NCs/GL和QT-NCs/P188。扫描电子显微镜（SEM）下，QT-NCs/GL和QT-NCs/P188均呈现不规则颗粒和短棒状。X射线粉末衍射（XRPD）显示，QT-NCs/GL和QT-NCs/P188保持结晶状态，但结晶度降低。与原料药QT相比，QT-NCs/GL和QT-NCs/P188的QT溶解度显著增加，药物释放得到改善。静脉注射QT-NCs/GL和QT-NCs/P188后，QT的血浆浓度-时间曲线和药代动力学参数无显著差异。然而，与QT-NCs/P188相比，静脉注射QT-NCs/GL后观察到QT在肝脏中的分布显著更高，表明由GL稳定的QT-NCs可以实现QT向肝脏的靶向递送。可以得出结论，用作QT NCs稳定剂的GL在肝脏靶向给药方面具有巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/e3583d8cded9/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/731e1c47a8d5/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/e79245b2599a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/08abe9ad6c10/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/34a93e3fe9b2/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/0f85eaf1479d/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/fb3bdc0fd8cd/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/4184814065b4/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/dee15dab3b4f/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/e3583d8cded9/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/731e1c47a8d5/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/e79245b2599a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/08abe9ad6c10/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/34a93e3fe9b2/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/0f85eaf1479d/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/fb3bdc0fd8cd/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/4184814065b4/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/dee15dab3b4f/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dab2/11019285/e3583d8cded9/gr8.jpg

相似文献

1
Fabrication and in vitro/vivo evaluation of quercetin nanocrystals stabilized by glycyrrhizic acid for liver targeted drug delivery.甘草酸稳定的槲皮素纳米晶体用于肝脏靶向给药的制备及其体外/体内评价
Int J Pharm X. 2024 Apr 9;7:100246. doi: 10.1016/j.ijpx.2024.100246. eCollection 2024 Jun.
2
Quercetin nanocrystals for bioavailability enhancement: impact of different functional stabilizers on / drug performances.槲皮素纳米晶体提高生物利用度：不同功能稳定剂对药物性能的影响。
Pharm Dev Technol. 2024 Jul;29(6):551-558. doi: 10.1080/10837450.2024.2361654. Epub 2024 Jun 5.
3
Development of herpetrione nanosuspensions stabilized by glycyrrhizin for enhancing bioavailability and synergistic hepatoprotective effect.甘草次酸稳定的蛇足石杉纳米混悬剂的研制及其提高生物利用度和协同肝保护作用。
Drug Dev Ind Pharm. 2021 Oct;47(10):1664-1673. doi: 10.1080/03639045.2022.2045304. Epub 2022 Feb 25.
4
Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin.用于槲皮素口服递送的药物纳米晶体自稳定Pickering乳液的制备及其体外/体内评价
Pharmaceutics. 2022 Apr 20;14(5):897. doi: 10.3390/pharmaceutics14050897.
5
[Preparation and in vitro release of quercetin nanocrystals self-stabilized Pickering emulsion].槲皮素纳米晶体自稳定Pickering乳液的制备及体外释放
Zhongguo Zhong Yao Za Zhi. 2022 Mar;47(5):1230-1236. doi: 10.19540/j.cnki.cjcmm.20210525.301.
6
The contribution of absorption of integral nanocrystals to enhancement of oral bioavailability of quercetin.完整纳米晶体的吸收对槲皮素口服生物利用度提高的贡献。
Acta Pharm Sin B. 2021 Apr;11(4):978-988. doi: 10.1016/j.apsb.2021.02.015. Epub 2021 Feb 25.
7
Preparation and evaluation of N-caproyl chitosan nanoparticles surface modified with glycyrrhizin for hepatocyte targeting.制备并评价了经甘草酸表面修饰的 N-己酰化壳聚糖纳米粒用于肝细胞靶向。
Drug Dev Ind Pharm. 2009 Nov;35(11):1348-55. doi: 10.3109/03639040902939197.
8
Preparation and in vitro antitumor effects on MDA-MB-231 cells of niclosamide nanocrystals stabilized by poloxamer188 and PBS.尼氯硝唑纳米晶的制备及其对 MDA-MB-231 细胞的体外抗肿瘤作用，该纳米晶由泊洛沙姆 188 和 PBS 稳定。
Int J Pharm. 2020 Jun 30;584:119432. doi: 10.1016/j.ijpharm.2020.119432. Epub 2020 May 19.
9
Formulation of pluronic F127/TPGS mixed micelles to improve the oral absorption of glycyrrhizic acid.制备泊洛沙姆 F127/TPGS 混合胶束以提高甘草酸的口服吸收。
Drug Dev Ind Pharm. 2020 Jul;46(7):1100-1107. doi: 10.1080/03639045.2020.1775634. Epub 2020 Jun 8.
10
Fabrication and Characterization of Tedizolid Phosphate Nanocrystals for Topical Ocular Application: Improved Solubilization and In Vitro Drug Release.用于眼部局部应用的磷酸特地唑胺纳米晶体的制备与表征：改善溶解性和体外药物释放
Pharmaceutics. 2022 Jun 23;14(7):1328. doi: 10.3390/pharmaceutics14071328.

引用本文的文献

1
Quercetin-Loaded Ginkgo Starch Nanoparticles: A Promising Strategy to Improve Bioactive Delivery and Cellular Homeostasis in Functional Foods.负载槲皮素的银杏淀粉纳米颗粒：改善功能性食品中生物活性成分递送和细胞稳态的一种有前景的策略。
Foods. 2025 May 26;14(11):1890. doi: 10.3390/foods14111890.
2
Preparation and Evaluation of Tetrandrine Nanocrystals to Improve Bioavailability.粉防己碱纳米晶体的制备及其提高生物利用度的评价
Curr Drug Deliv. 2025;22(5):648-657. doi: 10.2174/0115672018341709241121092617.

本文引用的文献

1
Nanosuspensions technology as a master key for nature products drug delivery and In vivo fate.纳米混悬液技术作为天然产物药物递送及体内命运的关键技术。
Eur J Pharm Sci. 2023 Jun 1;185:106425. doi: 10.1016/j.ejps.2023.106425. Epub 2023 Mar 18.
2
Stabilizer-induced different in vivo behaviors for intramuscularly long-acting celecoxib nanocrystals.载体制剂诱导的体内长效塞来昔布纳米晶行为差异。
Int J Pharm. 2022 Nov 25;628:122298. doi: 10.1016/j.ijpharm.2022.122298. Epub 2022 Oct 17.
3
Nanocrystals for controlled delivery: state of the art and approved drug products.
纳米晶体用于控制释放：最新技术和已批准的药物产品。
Expert Opin Drug Deliv. 2022 Oct;19(10):1303-1316. doi: 10.1080/17425247.2022.2110579. Epub 2022 Aug 8.
4
Review of nanosuspension formulation and process analysis in wet media milling using microhydrodynamic model and emerging characterization methods.湿磨法中利用微流体动力学模型和新兴表征方法对纳米混悬剂制剂及工艺分析的综述。
Int J Pharm. 2022 Jul 25;623:121862. doi: 10.1016/j.ijpharm.2022.121862. Epub 2022 Jun 4.
5
Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin.用于槲皮素口服递送的药物纳米晶体自稳定Pickering乳液的制备及其体外/体内评价
Pharmaceutics. 2022 Apr 20;14(5):897. doi: 10.3390/pharmaceutics14050897.
6
Drug Nanocrystals for Active Tumor-Targeted Drug Delivery.用于主动肿瘤靶向给药的药物纳米晶体
Pharmaceutics. 2022 Apr 6;14(4):797. doi: 10.3390/pharmaceutics14040797.
7
Drug Nanocrystals: Focus on Brain Delivery from Therapeutic to Diagnostic Applications.药物纳米晶体：从治疗应用到诊断应用，聚焦脑递送
Pharmaceutics. 2022 Mar 23;14(4):691. doi: 10.3390/pharmaceutics14040691.
8
Nanocrystals as a master key to deliver hydrophobic drugs via multiple administration routes.纳米晶作为一把万能钥匙，可通过多种给药途径传递疏水性药物。
J Control Release. 2022 May;345:334-353. doi: 10.1016/j.jconrel.2022.03.012. Epub 2022 Mar 11.
9
Development of herpetrione nanosuspensions stabilized by glycyrrhizin for enhancing bioavailability and synergistic hepatoprotective effect.甘草次酸稳定的蛇足石杉纳米混悬剂的研制及其提高生物利用度和协同肝保护作用。
Drug Dev Ind Pharm. 2021 Oct;47(10):1664-1673. doi: 10.1080/03639045.2022.2045304. Epub 2022 Feb 25.
10
Glycyrrhizic Acid and Its Hydrolyzed Metabolite 18β-Glycyrrhetinic Acid as Specific Ligands for Targeting Nanosystems in the Treatment of Liver Cancer.甘草酸及其水解代谢产物18β-甘草次酸作为靶向纳米系统治疗肝癌的特异性配体。
Pharmaceutics. 2021 Oct 26;13(11):1792. doi: 10.3390/pharmaceutics13111792.