Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid Arthritis

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...

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Main Authors: Jiangfan Han, Ren Na, Ningning Zhao, Xiaofeng Yuan, Linke Fu, Jianmei Jing, Airong Qian, Weiliang Ye
Format: Article
Language:English
Published: MDPI AG 2023-01-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/28/2/591
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author Jiangfan Han
Ren Na
Ningning Zhao
Xiaofeng Yuan
Linke Fu
Jianmei Jing
Airong Qian
Weiliang Ye
author_facet Jiangfan Han
Ren Na
Ningning Zhao
Xiaofeng Yuan
Linke Fu
Jianmei Jing
Airong Qian
Weiliang Ye
author_sort Jiangfan Han
collection DOAJ
description 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.
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spelling doaj.art-cf5fc92d192c42bb9d4a580a155788932023-11-30T23:41:58ZengMDPI AGMolecules1420-30492023-01-0128259110.3390/molecules28020591Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid ArthritisJiangfan Han0Ren Na1Ningning Zhao2Xiaofeng Yuan3Linke Fu4Jianmei Jing5Airong Qian6Weiliang Ye7Lab for Bone Metabolism, Key Lab for Space Biosciences and Biotechnology, School of Life Sciences, Northwestern Polytechnical University, Xi’an 710072, ChinaDepartment of Epidemiology and Health Statistics, Faculty of Military Preventive Medicine, Fourth Military Medical University, Xi’an 710032, ChinaDepartment of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi’an 710032, ChinaDepartment of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi’an 710032, ChinaDepartment of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi’an 710032, ChinaDepartment of Radiology, Xijing Hospital, Fourth Military Medical University, Xi’an 710038, ChinaLab for Bone Metabolism, Key Lab for Space Biosciences and Biotechnology, School of Life Sciences, Northwestern Polytechnical University, Xi’an 710072, ChinaDepartment of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi’an 710032, ChinaRheumatoid 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.https://www.mdpi.com/1420-3049/28/2/591dextran sulfatedexamethasonerheumatoid arthritismicellestargeted therapy
spellingShingle Jiangfan Han
Ren Na
Ningning Zhao
Xiaofeng Yuan
Linke Fu
Jianmei Jing
Airong Qian
Weiliang Ye
Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid Arthritis
Molecules
dextran sulfate
dexamethasone
rheumatoid arthritis
micelles
targeted therapy
title Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid Arthritis
title_full Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid Arthritis
title_fullStr Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid Arthritis
title_full_unstemmed Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid Arthritis
title_short Macrophage-Targeted Dextran Sulfate-Dexamethasone Conjugate Micelles for Effective Treatment of Rheumatoid Arthritis
title_sort macrophage targeted dextran sulfate dexamethasone conjugate micelles for effective treatment of rheumatoid arthritis
topic dextran sulfate
dexamethasone
rheumatoid arthritis
micelles
targeted therapy
url https://www.mdpi.com/1420-3049/28/2/591
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