Citation: Xin-Yu Liu, He-Ying Mao, Jun-Sheng Hu, Tong-Rui Dou, Ben-Chi Liu, Chang-Xiu Lin, Jing-Shu Piao, Ming-Guan Piao. A c(RGDyK)-modified ROS-responsive polymeric micelle for hepatic stellate cell targeting[J]. Chinese Chemical Letters, ;2026, 37(1): 111237. doi: 10.1016/j.cclet.2025.111237 shu

A c(RGDyK)-modified ROS-responsive polymeric micelle for hepatic stellate cell targeting

Xin-Yu Liu ^{a, 1} ,
He-Ying Mao ^{a, 1} ,
Jun-Sheng Hu ^a ,
Tong-Rui Dou ^a ,
Ben-Chi Liu ^a ,
Chang-Xiu Lin ^{c, *,} ,
Jing-Shu Piao ^{a, *,} ,
Ming-Guan Piao ^{a, b, *,}

a.
School of Pharmacy, Yanbian University, Yanji 133002, China
b.
Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, Yanbian University, Yanji 133002, China
c.
Central Laboratory of The Affiliated Hospital, Yanbian University, Yanji 133000, China

2275735282@qq.com

piaojingshu@ybu.edu.cn

mgpiao@ybu.edu.cn

Received Date: 15 January 2025
Revised Date: 14 April 2025
Accepted Date: 21 April 2025
Available Online: 21 April 2025

Figures(4)

Hepatic fibrosis is regulated by the synergistic actions of various cells and cytokines, with the activation and proliferation of hepatic stellate cells (HSCs) being considered the central event in this process. To achieve specific targeting of activated hepatic stellate cells (aHSCs) and precise treatment of hepatic fibrosis, this study developed a dual-functional drug delivery system (SIL/cRGD-PEG-PPS PMs) with both targeting and responsive release capabilities. It aims to target the αvβ3 receptor specifically expressed on the surface of aHSCs using the cyclic peptide c(RGDyk), and to exploit the high reactive oxygen species (ROS) level in the cellular microenvironment to achieve concentrated burst release of drugs at the pathological sites of hepatic fibrosis. Based on multiple assessments, SIL/cRGD-PEG-PPS PMs specifically enhanced the targeted delivery of silybin (SIL) to aHSCs, inhibited the proliferation and migration of aHSCs, and exhibited good biosafety. Additionally, it demonstrated excellent anti-fibrotic activity in fibrotic mice. In summary, this study shows great potential in targeted treatment of hepatic fibrosis and provides a multifunctional tool for advancing the research and therapeutic strategies of hepatic fibrosis.
- Liver fibrosis,
- Targeted delivery,
- ROS responsive release,
- αvβ3,
- c(RGDyK)
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沈阳化工大学材料科学与工程学院沈阳 110142