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Preparation, characterization, pharmacokinetics and ulcerative colitis treatment of hyperoside-loaded mixed micelles

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Abstract

At present, ulcerative colitis (UC) has become a global disease due to its high incidence. Hyperoside (HYP) is a naturally occurring flavonoid compound with many pharmacological effects. This study aimed to develop HYP-loaded mixed micelles (HYP-M) to improve oral bioavailability of HYP and to evaluate its therapeutic effect on UC. The prepared HYP-M exhibited stable physical and chemical properties, smaller particle size (PS) (21.48 ± 1.37 nm), good polydispersity index (PDI = 0.178 ± 0.013), negative Zeta potential (ZP) (− 20.00 ± 0.48 mV) and high entrapment rate (EE) (89.59 ± 2.03%). In vitro release and in vivo pharmacokinetic results showed that HYP-M significantly increased the releasing rate of HYP, wherein its oral bioavailability was 4.15 times higher than that of free HYP. In addition, HYP-M was more effective in the treatment of UC than free HYP. In conclusion, HYP-M could serve as a novel approach to improve bioavailability and increase anti-UC activity of HYP.

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All data and materials generated or analyzed during this study are included in this published article (and its supplementary information files).

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Acknowledgements

The authors appreciate the Institute of Pharmacy, Jiangsu University (Zhenjiang, China), for providing the necessary facilities to produce this manuscript. We also thank the University Ethics Committee for playing a key role in approving the animal experimentation directive.

Funding

This work was funded by the National Key R&D Program of China [grant numbers: 2018YFE0208600], National Natural Science Foundation of China [grant numbers: 81720108030 and 8217131836], Jiangsu Postdoctoral Research Foundation [grant numbers:2021K010A], Natural Science Foundation of Jiangsu Universities [grant numbers: 18KJB360001], Key planning social development projects of Zhenjiang in Jiangsu Province [grant numbers:SH2021024] and Natural Science Foundation of Jiangsu Province (BK20220529).

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Author notes

  1. Xingcheng Jin and Xiaoli Xia contributed equally to this work.

Authors and Affiliations

  1. Department of Pharmacy, the Second Affiliated Hospital, Anhui Medical University, Hefei, China

    Xingcheng Jin

  2. Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu Provincial Research Center for Medicinal Function Development of New Food Resources, Jiangsu University, Zhenjiang, Jiangsu, China

    Xiaoli Xia, Jiaying Li, Xiaowen Wang, Qilong Wang, Huaxiao Wu, Qingtong Yu, Xia Cao, Jiangnan Yu & Ximing Xu

  3. Department of Biochemistry and Forensic Sciences, School of Chemical and Biochemical Sciences, C. K. Tedam University of Technology and Applied Sciences (CKT-UTAS), Navrongo, Ghana

    Michael Adu-Frimpong

  4. Jiangsu Tian Sheng Pharmaceutical Co., Ltd., Zhenjiang, China

    Hao Ji

  5. Institute of Agriculture and Agrotechnologies of Karakalpakstan, Nukus, Uzbekistan

    Elmurat Toreniyazov

Authors
  1. Xingcheng Jin
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  2. Xiaoli Xia
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  3. Jiaying Li
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  11. Xia Cao
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  12. Jiangnan Yu
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Contributions

Xingcheng Jin and Xiaoli Xia: methodology, validation, formal analysis, data curation, writing—original draft, visualization. Jiaying Li: methodology, investigation. Xiaowen Wang: software, formal analysis. Huaxiao Wu: validation, investigation. Michael Adu-Frimpong: writing—review & editing. Qingtong Yu: project administration. Hao Jic: Project administration. Elmurat Toreniyazov: Project administration. Xia Cao: supervision. Qilong Wang: conceptualization, methodology, supervision. Jiangnan Yu: resources, supervision project administration, funding acquisition. Ximing Xu: supervision, project administration, funding acquisition.

Corresponding authors

Correspondence to Xia Cao, Jiangnan Yu or Ximing Xu.

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All institutional and national guidelines for the care and use of laboratory animals were followed.

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The authors declare no competing interests.

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Jin, X., Xia, X., Li, J. et al. Preparation, characterization, pharmacokinetics and ulcerative colitis treatment of hyperoside-loaded mixed micelles. Drug Deliv. and Transl. Res. 14, 1370–1388 (2024). https://doi.org/10.1007/s13346-023-01470-0

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