Oleanolic acid-based nanoparticles for the treatment of ulcerative colitis.

IF 3.9 Nanomedicine (London, England) Pub Date : 2025-04-01 Epub Date: 2025-02-23 DOI:10.1080/17435889.2025.2467019
Dan Zhang, Beiwei Zhu, Yu Xu, Fengxian Luo, Tao Chen, Lihang Chen, Xinchuang Wang, Di Wu, Jiangning Hu
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Abstract

Aim: This study aims to develop and assess the therapeutic potential of oleanolic acid nanoparticles (OA NPs) in treating ulcerative colitis (UC).

Materials & methods: OA NPs were synthesized using an emulsion solvent evaporation method, forming spherical nanoparticles with an average diameter of 138.1 nm. The nanoparticles were designed to target the colon through the enhanced permeability and retention (EPR) effect. Network pharmacology and molecular docking identified key inflammatory pathways, and in vitro (RAW264.7 cells) and in vivo (DSS-induced UC mouse model) experiments evaluated their anti-inflammatory effects and therapeutic efficacy.

Results: OA NPs successfully targeted the colon and demonstrated improved bioavailability. In vitro experiments showed that OA NPs reduced oxidative stress and inflammation by downregulating pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β) and promoting macrophage polarization from M1 to M2. In the DSS-induced UC mouse model, oral administration of OA NPs significantly alleviated colitis symptoms, improved colon length, reduced inflammation, and mitigated tissue damage.

Conclusion: OA NPs mitigate UC pathology through targeted delivery, enhanced stability, and modulation of inflammatory pathways, providing a promising approach for UC treatment. Further studies are needed to evaluate their long-term safety and clinical applicability.

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齐墩果酸纳米颗粒治疗溃疡性结肠炎。
目的:本研究旨在开发和评估齐墩果酸纳米颗粒(OA NPs)在治疗溃疡性结肠炎(UC)方面的治疗潜力:采用乳液溶剂蒸发法合成齐墩果酸纳米粒子,形成平均直径为138.1 nm的球形纳米粒子。该纳米粒子旨在通过增强渗透性和滞留性(EPR)效应靶向结肠。网络药理学和分子对接确定了关键的炎症通路,体外(RAW264.7 细胞)和体内(DSS 诱导的 UC 小鼠模型)实验评估了它们的抗炎作用和疗效:结果:OA NPs 成功靶向结肠并提高了生物利用度。体外实验表明,OA NPs 通过下调促炎细胞因子(TNF-α、IL-6 和 IL-1β)和促进巨噬细胞从 M1 极化到 M2,减少了氧化应激和炎症反应。在 DSS 诱导的 UC 小鼠模型中,口服 OA NPs 能显著缓解结肠炎症状、改善结肠长度、减少炎症反应并减轻组织损伤:结论:OA NPs 通过靶向递送、增强稳定性和调节炎症通路缓解了 UC 病理学,为 UC 治疗提供了一种前景广阔的方法。还需要进一步的研究来评估其长期安全性和临床适用性。
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oleanolic acid (OA)
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