Antioxidant Glycopolypeptide Micelles for Targeted Delivery of Silibinin to Hepatocellular Carcinoma Cells

Kai Chen; Ping Wei; Jing-Hua Chen

doi:10.1007/s10118-025-3429-0

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Antioxidant Glycopolypeptide Micelles for Targeted Delivery of Silibinin to Hepatocellular Carcinoma Cells

RESEARCH ARTICLE | Updated：2025-10-30

- Antioxidant Glycopolypeptide Micelles for Targeted Delivery of Silibinin to Hepatocellular Carcinoma Cells
- Antioxidant Glycopolypeptide Micelles for Targeted Delivery of Silibinin to Hepatocellular Carcinoma Cells
- 高分子科学（英文） 2025年43卷第11期页码：2051-2060
- Affiliations：
  
  Key Laboratory of Carbohydrate Chemistry and Biotechnology, Ministry of Education, School of Life Sciences and Health Engineering, Jiangnan University, Wuxi 214122, China
- Author bio：
  
  weiping@jiangnan.edu.cn (P.W.)
  chenjinghua@jiangnan.edu.cn (J.H.C.)
- Funds：
  
  This work was financially supported by the National Natural Science Foundation of China (No. 22305102), Basic Research Program of Jiangsu (No. BK20221097), and the Open Project of Key Laboratory of Carbohydrate Chemistry and Biotechnology (Jiangnan University), Ministry of Education (No. KLCCB-KF202405).;Electronic supplementary information (ESI) is available free of charge in the online version of this article at http://doi.org/10.1007/s10118-025-3429-0.
- DOI：10.1007/s10118-025-3429-0
  中图分类号：
- 收稿：2025-06-24，
  
  录用：2025-08-08，
  
  网络首发：2025-10-11，
  
  纸质出版：2025-11-05
- Accepted：
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Chen, K.; Wei, P.; Chen, J. H. Antioxidant glycopolypeptide micelles for targeted delivery of silibinin to hepatocellular carcinoma cells. Chinese J. Polym. Sci. 2025, 43, 2051–2060

Kai Chen, Ping Wei, Jing-Hua Chen. Antioxidant Glycopolypeptide Micelles for Targeted Delivery of Silibinin to Hepatocellular Carcinoma Cells[J]. Chinese Journal of Polymer Science, 2025, 43(11): 2051-2060.
Chen, K.; Wei, P.; Chen, J. H. Antioxidant glycopolypeptide micelles for targeted delivery of silibinin to hepatocellular carcinoma cells. Chinese J. Polym. Sci. 2025, 43, 2051–2060 DOI： 10.1007/s10118-025-3429-0.

Kai Chen, Ping Wei, Jing-Hua Chen. Antioxidant Glycopolypeptide Micelles for Targeted Delivery of Silibinin to Hepatocellular Carcinoma Cells[J]. Chinese Journal of Polymer Science, 2025, 43(11): 2051-2060. DOI： 10.1007/s10118-025-3429-0.

摘要

A versatile glycopolypeptide micelle system

featuring intrinsic antioxidant activity and specific targeting capability toward hepatocellular carcinoma cells

was rationally designed. This system demonstrates synergistic antioxidant effects through the combined action of encapsulated silibinin and the antioxidant glycopolypeptide scaffold

indicating promising bioapplications in the treatment of oxidative stress-related liver diseases.

Abstract

Silibinin

a natural flavanone extracted from the milk thistle plant (

Silybum marianum

)

has been shown to have various therapeutic applications

including liver protection

antioxidant

anticancer

anti-inflammatory

and many other effects. However

silibinin exhibits poor oral absorbance and low bioavailability owing to its limited water solubility

which limits its therapeutic efficiency and further clinical translation. To address these issues

we propose an antioxidant glycopolypeptide micelle strategy to target the delivery of silibinin to enhance its solubility

bioavailability

and antioxidant activity. This versatile micelle self-assembled from a glycopolypeptide

-acetylgalactosamine-grafted poly(glutamic acid)-

block

-poly(tyrosine).

-acetylgalactosamine (GalNAc) is incorporated to enable liver targeting by selectively binding to the asialoglycoprotein receptor

which is overexpressed on hepatocellular carcinoma cells. The antioxidant polypeptide polytyrosine

as well as encapsulated silibinin

exhibits a synergistic reactive oxygen species (ROS) scavenging effect. The obtained results confirmed that silibinin can be effectively encapsulated into the glycopolypeptide micelles through self-assembly

achieving a loading efficiency and loading content of 96.6% and 42.9%

spectively. The silibinin-loaded glycopolypeptide micelles exhibited enhanced cellular uptake and a synergistic ROS scavenging effect in hepatocellular carcinoma cells. Overall

these antioxidant glycopolypeptide micelles hold promise as safe and efficient drug delivery systems for targeting hepatocellular carcinoma cells

potentially providing an effective strategy to enhance the bioavailability and antioxidant activity of silibinin.

关键词

Keywords

references

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