Scholarlink

Background <p>Idiopathic pulmonary fibrosis (IPF) is a fatal interstitial lung disease characterized by excessive extracellular matrix (ECM) accumulation and irreversible alveolar damage. Although currently available antifibrotic drugs can slow disease progression, their clinical utility is limited by systemic side effects and a lack of organ and cell specificity. Apigenin has been shown to exhibit antifibrotic properties by modulating reactive oxygen species (ROS) and inhibiting of the transforming growth factor-beta (TGF-β) signaling pathway. However, its poor solubility and bioavailability restrict its therapeutic application. To address these limitations, we developed an albumin-dibenzycyclooctyne-glucose/apigenin (AD-Glc/Api) nanocomplex designed for targeted delivery to fibrotic lung tissue.</p> Result <p>In this nanocomplex, albumin enhances the pharmacokinetic properties, while glucose modification enhances cellular uptake in vitro. In an IPF mouse model, positron emission tomography (PET) imaging demonstrated pulmonary-associated signals of [<sup>64</sup>Cu]Cu-AD-Glc/Api at week 1. At week 4, uptake of [<sup>68</sup>Ga]Ga-FAPI-46 was lowered in the AD-Glc/Api-treated group, indicating attenuation of fibrotic activity. These imaging findings were consistent with a marked reduction in collagen deposition and a decrease in fibrosis severity (<i>p</i> &lt; 0.01), as well as suppression of the TGF-β signaling pathway.</p> Conclusions <p>AD-Glc/Api is an effective antifibrotic nanotherapeutic, with efficacy driven by improved systemic circulation and enhanced cellular uptake. This theranostic platform represents a promising strategy for improving the diagnosis and treatment of IPF.</p> Graphical abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

The antifibrotic effects of a click chemistry-based albumin nanocomplex in an idiopathic pulmonary fibrosis model

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年4月20日

查看全文
  • Minji Kim,
  • Seobin Ma,
  • Kyuwan Kim,
  • Hyeri Chae,
  • Young Joo Kim,
  • Sung Hyun Hong,
  • Ran Ji Yoo,
  • Yun-Sang Lee

摘要

Background

Idiopathic pulmonary fibrosis (IPF) is a fatal interstitial lung disease characterized by excessive extracellular matrix (ECM) accumulation and irreversible alveolar damage. Although currently available antifibrotic drugs can slow disease progression, their clinical utility is limited by systemic side effects and a lack of organ and cell specificity. Apigenin has been shown to exhibit antifibrotic properties by modulating reactive oxygen species (ROS) and inhibiting of the transforming growth factor-beta (TGF-β) signaling pathway. However, its poor solubility and bioavailability restrict its therapeutic application. To address these limitations, we developed an albumin-dibenzycyclooctyne-glucose/apigenin (AD-Glc/Api) nanocomplex designed for targeted delivery to fibrotic lung tissue.

Result

In this nanocomplex, albumin enhances the pharmacokinetic properties, while glucose modification enhances cellular uptake in vitro. In an IPF mouse model, positron emission tomography (PET) imaging demonstrated pulmonary-associated signals of [64Cu]Cu-AD-Glc/Api at week 1. At week 4, uptake of [68Ga]Ga-FAPI-46 was lowered in the AD-Glc/Api-treated group, indicating attenuation of fibrotic activity. These imaging findings were consistent with a marked reduction in collagen deposition and a decrease in fibrosis severity (p < 0.01), as well as suppression of the TGF-β signaling pathway.

Conclusions

AD-Glc/Api is an effective antifibrotic nanotherapeutic, with efficacy driven by improved systemic circulation and enhanced cellular uptake. This theranostic platform represents a promising strategy for improving the diagnosis and treatment of IPF.

Graphical abstract