Lab for Bone Metabolism, Key Lab for Space Biosciences and Biotechnology, School of Life Sciences, Northwestern Polytechnical University, Xi'an 710072, China.
Department of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi'an 710032, China.
Molecules. 2023 Jan 6;28(2):591. doi: 10.3390/molecules28020591.
Rheumatoid arthritis (RA) is a chronic, systemic immune disease that causes joint affection and even disability. Activated macrophages play an important role in the pathogenesis and progression of RA by producing pro-inflammatory factors. The use of dexamethasone (DXM) is effective in relieving the intractable pain and inflammatory progression of RA. However, long-term use of DXM is strongly associated with increased rates of diabetes, osteoporosis, bone fractures, and mortality, which hinders its clinical use. In this study, the dextran sulfate-cisaconitic anhydride-dexamethasone (DXM@DS-cad-DXM) micelles were prepared to treat RA by selectively recognizing scavenger receptor (SR) on the activated macrophages. The potent targeting property of DXM@DS-cad-DXM micelles to SR was by fluorescence microscope. Additionally, the effective accumulation and powerful anti-inflammatory activity of DXM@DS-cad-DXM micelles were observed in the inflamed joints of adjuvant-induced arthritis (AIA) rats after intravenous administration. Overall, DXM@DS-cad-DXM micelles are a potentially effective nanomedicine for targeted therapy of RA.
类风湿性关节炎（RA）是一种慢性、全身性免疫疾病，可导致关节受累甚至残疾。活化的巨噬细胞通过产生促炎因子在 RA 的发病机制和进展中起重要作用。地塞米松（DXM）的使用在缓解 RA 的难治性疼痛和炎症进展方面非常有效。然而，长期使用 DXM 与糖尿病、骨质疏松症、骨折和死亡率的增加密切相关，这阻碍了其临床应用。在这项研究中，通过选择性识别活化巨噬细胞上的清道夫受体（SR），用葡聚糖硫酸酯-顺丁烯二酸酐-地塞米松（DXM@DS-cad-DXM）胶束来治疗 RA。荧光显微镜观察到 DXM@DS-cad-DXM 胶束对 SR 的强大靶向特性。此外，在静脉注射后，在佐剂诱导的关节炎（AIA）大鼠的炎症关节中观察到 DXM@DS-cad-DXM 胶束的有效积累和强大的抗炎活性。总的来说，DXM@DS-cad-DXM 胶束是一种有潜力的用于 RA 靶向治疗的纳米医学。
