Cheng Zhaoxia, Li Fenfen, Qie Yunkai, Sun Jingyi, Wang Yazhou, Zhao Ying, Nie Guangjun
College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.
CAS Key Laboratory for Biomedical Effects of Nanomaterials & Nanosafety, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology, Beijing 100190, China.
Nano Lett. 2024 Dec 11;24(49):15827-15836. doi: 10.1021/acs.nanolett.4c04820. Epub 2024 Nov 25.
Liver fibrosis is characterized by the excessive accumulation of extracellular matrix proteins primarily produced by activated hepatic stellate cells (HSCs). The activation of HSCs plays a pivotal role in driving the progression of liver fibrosis. Achieving specific targeted delivery of antifibrotic agents toward activated HSCs remains a formidable challenge. Here, we developed an HSC membrane-camouflaged nanosystem, named HSC-PLGA-BAY, for the precise delivery of the antifibrosis agent BAY 11-7082 to activated HSCs in the treatment of liver fibrosis. The designed HSC-PLGA-BAY nanosystem exhibited selective targeting toward activated HSCs, with internalization mediated by homologous cell adhesion molecules from the HSC membrane, namely integrins and N-cadherin. Furthermore, our findings demonstrate that treatment with HSC-PGA-BAY significantly increased apoptosis of activated HSCs and ameliorated liver fibrosis progression in a bile duct ligation (BDL)-induced fibrotic mice model. Collectively, the HSCs-targeted therapeutic platform holds promising potential as an effective strategy for liver fibrosis treatment.
肝纤维化的特征是细胞外基质蛋白过度积累,这些蛋白主要由活化的肝星状细胞(HSC)产生。HSC的活化在推动肝纤维化进展中起关键作用。实现抗纤维化药物向活化HSC的特异性靶向递送仍然是一项艰巨的挑战。在此,我们开发了一种HSC膜伪装纳米系统,命名为HSC-PLGA-BAY,用于将抗纤维化药物BAY 11-7082精确递送至活化的HSC以治疗肝纤维化。所设计的HSC-PLGA-BAY纳米系统表现出对活化HSC的选择性靶向,其内化由来自HSC膜的同源细胞粘附分子介导,即整合素和N-钙粘蛋白。此外,我们的研究结果表明,在胆管结扎(BDL)诱导的纤维化小鼠模型中,用HSC-PGA-BAY治疗可显著增加活化HSC的凋亡并改善肝纤维化进展。总体而言,HSC靶向治疗平台作为肝纤维化治疗的有效策略具有广阔的潜力。