Theranostics 2017; 7(1):97-105. doi:10.7150/thno.16844

Research Paper

Scavenger Receptor-Mediated Targeted Treatment of Collagen-Induced Arthritis by Dextran Sulfate-Methotrexate Prodrug

Modi Yang1,3, Jianxun Ding1,✉, Xiangru Feng1, Fei Chang2,✉, Yinan Wang4, Zhongli Gao3, Xiuli Zhuang1, Xuesi Chen1

1. Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P. R. China;
2. Department of Orthopedics, The Second Hospital of Jilin University, Changchun 130041, P. R. China;
3. Department of Orthopedics, China-Japan Union Hospital of Jilin University, Changchun 130033, P. R. China;
4. Institute of Immunology, Academy of Translational Medicine, First Hospital of Jilin University, Changchun 130021, P. R. China.

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Yang M, Ding J, Feng X, Chang F, Wang Y, Gao Z, Zhuang X, Chen X. Scavenger Receptor-Mediated Targeted Treatment of Collagen-Induced Arthritis by Dextran Sulfate-Methotrexate Prodrug. Theranostics 2017; 7(1):97-105. doi:10.7150/thno.16844. Available from

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Rheumatoid arthritis (RA) is a chronic autoimmune disorder implicated in multiple joint affection and even disability. The activated macrophages perform a predominant role in onset and persistence of RA. Scavenger receptor (SR), one of several receptors overexpressed on the activated macrophages, is a specific biomarker for targeted therapy of numerous chronic inflammation diseases like RA. In this work, dextran sulfate-graft-methotrexate conjugate (DS-g-MTX) is synthesized and characterized, which exhibits excellent targetability to SR on the activated RAW 264.7 cells. Additionally, the enhanced accumulation and potent inflammatory inhibition are observed in the affected joint after intravenous injection of DS-g-MTX, compared to the treatment with dextran-graft-methotrexate (Dex-g-MTX), as is confirmed by the detection of histopathology and pro-inflammatory cytokines. Our work highlights DS-g-MTX as a potential therapeutic option for RA aiming the SR-expressed activated macrophages.

Keywords: collagen-induced arthritis, controlled release, scavenger receptor, methotrexate prodrug, rheumatoid arthritis therapy.