Anti-arthritic activity of diclofenac lipid-core nanocapsules: a stereolofical analysis approach of arthritis model

Abstract

Rheumatoid Arthritis (RA) is an autoimmune disease, known for inflammation of the synovium in small joints that causes pain and stiffness. Some of the mechanisms of pathogenesis are auto-antigenic T lymphocytes and auto-antibodies expressed by B lymphocytes. These mechanisms are the target for treatment. The current pharmaceuticals used for the treatment of RA are Disease-Modifying Anti-Rheumatic Drugs (DMARDs), Biologic DMARD and Non-steroidal Anti-inflammatory Drugs (NSAIDs). All of these pharmaceuticals cause toxicity when used for a long period of time and have major adverse effects on the patients due to their low specificity for inflamed tissue. For this reason, researchers are beginning to test nanoformulations for treatment. Nanodrugs or nanopharmaceuticals are medications encapsulated in a nanoscale size. This conformation gives them unique properties for specific drug delivery at targeted sites, avoidance of degradation by enzymes and sustained release of the drug. Nanopharmaceuticals have demonstrated better anti-inflammatory capacity, enhanced immunomodulation and lower rates of progression of the disease. Our objective was to evaluate the activity of a Lipid core nanocapsule of Diclofenac (DIC-LNC) in an experimental model of adjuvant-induced arthritis, using stereological analysis. We applied quantitative morphological analysis to measure the volume, density and cellular profile count of the metatarsophalangeal articulation of the second digit. Our results demonstrated that DIC-LNC managed to reduce the volume of the joint in a more effective way than the Diclofenac solution. DIC-LNC preserved the synovial space and diminished synovitis of the arthritic joints. Our results suggest that Diclofenac lipid-core nanocapsules are effective at reducing joint inflammation.