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

Molecules. 2023 Jan 6;28(2):591. doi: 10.3390/molecules28020591.

Abstract

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.

Keywords: dexamethasone; dextran sulfate; micelles; rheumatoid arthritis; targeted therapy.

MeSH terms

  • Animals
  • Arthritis, Rheumatoid* / drug therapy
  • Dexamethasone
  • Dextran Sulfate
  • Macrophages
  • Micelles*
  • Rats
  • Receptors, Scavenger

Substances

  • Micelles
  • Dextran Sulfate
  • Receptors, Scavenger
  • Dexamethasone