Guangxi Engineering Center in Biomedical Material for Tissue and Organ Regeneration, Collaborative Innovation Centre of Regenerative Medicine and Medical BioResource Development and Application Co-constructed By the Province and Ministry, Guangxi Key Laboratory of Regenerative Medicine, The First Affiliated Hospital of Guangxi Medical University, Nanning, 530021, China.
Pharmaceutical College, Guangxi Medical University, Nanning, 530021, China.
J Nanobiotechnology. 2024 May 9;22(1):221. doi: 10.1186/s12951-024-02494-5.
Intra-articular drugs used to treat osteoarthritis (OA) often suffer from poor pharmacokinetics and stability. Nano-platforms as drug delivery systems for drug delivery are promising for OA therapy. In this study, we reported an M1 macrophage-targeted delivery system Bai@FA-UIO-66-NH based on folic acid (FA) -modified metal-organic framework (MOF) loaded with baicalin (Bai) as antioxidant agent for OA therapy. With outstanding biocompatibility and high drug loading efficiency, Bai@FA-UIO-66-NH could be specifically uptaken by LPS-induced macrophages to serve as a potent ROS scavenger, gradually releasing Bai at the subcellular level to reduce ROS production, modulate macrophage polarization to M2, leading to alleviation of synovial inflammation in OA joints. The synergistic effect of Bai@FA-UIO-66-NH on macrophage polarization and ROS scavenging significantly improved the therapeutic efficacy of OA, which may provide a new insight into the design of OA precision therapy.
用于治疗骨关节炎 (OA) 的关节内药物通常存在药代动力学和稳定性差的问题。纳米平台作为药物传递系统在 OA 治疗中具有广阔的应用前景。在这项研究中，我们报道了一种基于叶酸 (FA) 修饰的金属有机骨架 (MOF) 负载黄芩苷 (Bai) 的 M1 巨噬细胞靶向递药系统 Bai@FA-UIO-66-NH，作为抗氧化剂用于 OA 治疗。Bai@FA-UIO-66-NH 具有出色的生物相容性和高载药效率，可被 LPS 诱导的巨噬细胞特异性摄取，作为一种有效的 ROS 清除剂，逐渐在亚细胞水平释放 Bai，减少 ROS 生成，调节巨噬细胞向 M2 极化，从而减轻 OA 关节的滑膜炎症。Bai@FA-UIO-66-NH 对巨噬细胞极化和 ROS 清除的协同作用显著改善了 OA 的治疗效果，这可能为 OA 精准治疗的设计提供新的思路。
