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Targeted delivery of liposomal dexamethasone phosphate to the spleen provides a persistent therapeutic effect in rat antigen-induced arthritis
  1. U Rauchhaus1,
  2. R W Kinne2,
  3. D Pohlers2,
  4. S Wiegand3,
  5. A Wölfert4,
  6. M Gajda4,
  7. R Bräuer4,
  8. S Panzner1
  1. 1
    Novosom AG, Halle/Saale, Germany
  2. 2
    Experimental Rheumatology Unit, Department of Orthopaedics, University Hospital Jena, Jena, Germany
  3. 3
    Department of Nuclear Medicine, University Hospital Jena, Jena, Germany
  4. 4
    Institute of Pathology, University Hospital Jena, Jena, Germany
  1. Correspondence to Dr S Panzner, Novosom AG, Weinbergweg 22, 06120 Halle/Saale, Germany; steffen.panzner{at}novosom.com

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Although long-term suppression of experimental arthritis has been reported for liposomal glucocorticoids, direct effects on subsequent flare-up reactions have not been investigated. The glucocorticoid dexamethasone phosphate (DXM-P) was encapsulated in large, non-PEGylated liposomes (DPPC/DPPG/Chol, 50/10/40 mol%, size: 295 (SD 15) nm) and its therapeutic efficacy was compared with free (non-liposomal) drug in rat antigen-induced arthritis (AIA). The specific aim was to assess the therapeutic persistence of an initial acute phase treatment with liposomal DXM-P on the induction of a subsequent flare-up reaction.

Intravenous injection of liposomal DXM-P (1.25 mg/kg body weight) at 6, 24 and 48 h following arthritis induction completely suppressed joint swelling. The tight treatment schedule was chosen based on the rapid kinetics of arthritis development in this model (6 h: half-maximal swelling; 24–48 h peak arthritis). No rebound was seen until day …

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