Ggt enzyme-responsive dexamethasone-oligopeptide antifibrotic prodrugs, preparations and uses

By designing a GGT enzyme-responsive dexamethasone-oligopeptide prodrug, the targeting and side effects of dexamethasone in the treatment of liver fibrosis were solved, achieving precise delivery to the site of liver fibrosis and dual therapeutic effects, significantly inhibiting the fibrosis process.

CN122404486APending Publication Date: 2026-07-17XINGHUOZHIYAO (BEIJING) TECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
XINGHUOZHIYAO (BEIJING) TECH CO LTD
Filing Date
2026-05-29
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing technologies for the treatment of liver fibrosis with dexamethasone have problems with systemic side effects and poor targeting, making it difficult to achieve precise targeted delivery and specific release. Furthermore, traditional nanocarriers cannot effectively solve the problems of off-target toxicity and inaccurate drug release.

Method used

We designed and synthesized a GGT enzyme-responsive dexamethasone-oligopeptide prodrug for liver fibrosis. By covalently coupling dexamethasone and oligopeptide through Michael addition reaction, we formed self-assembled nanoparticles, which enabled precise self-release of the drug at the site of liver fibrosis lesions and combined anti-inflammatory and immunomodulatory effects.

Benefits of technology

It achieves precise delivery and specific release of drugs at the site of liver fibrosis, significantly reduces systemic side effects, inhibits the progression of liver fibrosis, and demonstrates more comprehensive therapeutic potential than traditional drugs.

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Abstract

本发明公开了一种GGT酶响应型地塞米松‑寡肽抗肝纤维化前药、制备及应用,创新性合成了一种GGT酶响应的自释放两亲性前药,并制备成稳定的纳米颗粒。该前药由地塞米松与具有生物活性的寡肽衍生物通过迈克尔加成反应共价偶联而成,可自组装为纳米颗粒,兼具药物活性成分与载体功能。同时,通过GGT酶响应机制实现药物在肝纤维化病灶部位的“精准自释放”,显著降低了地塞米松对骨骼、免疫及代谢系统的全身性副作用。本发明形成了“抗炎+免疫调节”的双重协同途径,不仅抑制了I型胶原沉积,更实现了对肝内免疫微环境的系统性重塑,从根源上抑制了纤维化进程,可在制备治疗、改善或逆转肝纤维化、减轻肝损伤及降低糖皮质激素全身性毒性的药物中应用。
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