Development of delivery system of Diacerein in animal models for achieving of new antirheumatoid arthritis drug

Abstract

Diacerein is an anthraquinone derivative having antiosteoarthritic activity. Apart from this, newlinevarious literature reveals that it is having protective effects in diabetes, Psoriasis, cancer, newlineepidermolysis bullosa, and in periodontitis. It works primarily by inhibiting the IL-1and#946; newlinebiosynthesis, the key cytokine involved in inflammatory reactions of various disorders. The newlineaqueous solubility of diacerein is low, oral bioavailability is approx. 35 to 56 %. Diacerein newlinemicrospheres were created using the ionotropic gelation technique. 8 different batches were newlineproduced based on the alterations in the ratios of polymer used. FTIR studies were performed newlineto check drug-polymer compatibility. % Yield, swelling index, In-vitro drug release studies, newlineentrapment efficiency of drug, estimation of particle size were performed. From the data of the newlinepreviously mentioned experimental part, the optimized batch was selected and SEM was done newlineto examine the Surface topography of the microspheres. newlineOptimized batch microspheres were subjected to preclinical animal models of rheumatoid newlinearthritis. Various arthritic parameters like paw volume measurement, joint stiffness study, newlinemobility test, gait test, haematological parameters, X-ray examinations of tibiotarsal joints, and newlinehistopathological examinations of cartilages of tibiotarsal joints showed significant newlineimprovements like diacerein API treated group and glucosamine treated group. LPS induced newlinepaw edema model showed diacerein microsphere showed significant sustained release newlinecharacteristics. Further, data from the charcoal meal test showed a significant decrease in newlineintestinal meal transit and peristalsis index in the diacerein microsphere-treated group which newlineresults in a decrease in diarrhoea