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DICLOFENAC LIPID-CORE NANOCAPSULES ARE EFFECTIVE TO CONTROL EXPERIMENTAL ARTHRITIS AND MONONUCLEAR CELLS INFLAMMATION
Diclofenac is a widely used non-steroidal anti-inflammatory drug to inflammation and pain control for rheumatoid arthritis and spondyloarthritis. However, the use of diclofenac is related to serious adverse effects. We developed this new diclofenac formulation - a diclofenac lipid-core nanocapsule as a promising effective and safe formulation. The aim of this work was to evaluate if diclofenac -loaded lipid-core nanocapsules reduce experimental arthritis and proinflammatory and T-cell-derived cytokines in activated mononuclear cells derived from RA patients.
Materials and methods
Formulations were prepared by self-assembling methodology. Adjuvant arthritis was induced in Lewis rats (AIA) and the effect on edema formation, TNF-alfa levels, interleukin-1 beta (IL1), C-Reactive protein levels (CRP) after treatment were evaluated. Mononuclear cells obtained from the synovial fluid of RA patients during infiltration procedures were treated with Diclofenac (DIC) solution and diclofenac lipid-core nanocapsules (DIC-LNC). TNF-alfa and IL6 cytokine levels were quantified at supernatant cultures from RA patients derived mononuclear cells. DIC-LNC reduced IL17 cytokine (r = 0.98, p=0.001) production on mononuclear cells culture in a dose-dependent manner compared to DIC.
Formulations showed nanometric and unimodal size distribution profiles with D[4.3] of 204±46 and span of 1.7±0.1. At the 28th day of the experiment the DIC-LNC, the hind paw volume was reduced than DIC (p <0.05) and arthritis group (p<0.05). We also observed an early edema inhibition on the 21st day of the experiment by DIN-LNC and we DIC formulation did not show similar properties. Inflammatory biomarkers TNF-alfa, IL1 and CRP (p <0.05 ) were significantly reduced for DIC-LNC (p<0.05) compared to DIC group (p <0.05). Interesting, TNF-alfa, IL-6 and IL17 cytokines produced by synovial mononuclear cells were also reduced compared to arthritis group (p <0.05) and conventional DIC (p <0.05).
Diclofenac lipid-core nanocapsules were more effective than common diclofenac formulation for inflammation control, reducing paw edema formation and TNF-alfa and IL1 cytokine levels, as well as the synovial cells TNF-alfa, IL-6, and IL17 cytokine production. These are promising features in the field of rheumatology especially for inflammatory arthritis, improving the quality and efficiency of a Diclofenac.
ANTONIO LUIZ BOECHAT, ANTONIO LUIZ BOECHAT, CATIUSCIA PADILHA OLIVEIRA, CATIUSCIA PADILHA OLIVEIRA, ANDREA MONTEIRO TARRAGO, ANDREA MONTEIRO TARRAGO, ALLYSON GUIMARAES COSTA, ALLYSON GUIMARAES COSTA, SILVIA STANISCUASKI GUTERRES, SILVIA STANISCUASKI GUTERRES, ADRIANA RAFFIN POHLMANN, ADRIANA RAFFIN POHLMANN