Diacerein, its beneficial impact on chondrocytes and notable new clinical applications

Abstract

Diacerein (DCN) was obtained by diacetylation of an anthraquinone derivative rhein and was approved by FDA in 2008, in the treatment of osteoarthritis due to its inhibitory effect on proinflammatory cytokines, including IL-6 and IL-1β. It was synthesized in 1980s and marketed as a tablet in some European Union and Asian countries from 1994. Along with its great potential in the treatment of osteoarthritis, its other applications are also being explored day by day, such as in the treatment of psoriasis, epidermolysis bullosa, breast cancer, type 2 diabetes and periodontitis. The main aim of this review is to explore mechanism of action, various applications and side effects associated with DCN. This has been reviewed that apart from the risk of diarrhea on long-term administration of DCN, various clinical studies has also shown its modest benefits in treatment of various pathological conditions. Hence, DCN is emerging as a new and potentially safe derivative with maximum therapeutic efficacies and minimum side effects which can results in improving the living status of patients suffering from various inflammatory diseases.

Preparation of solid dispersion systems for enhanced dissolution of poorly water soluble diacerein: In-vitro evaluation, optimization and physiologically based pharmacokinetic modeling

“…In our study, first order and Higuchi diffusion model plots yielded greater R 2 values than plots for zero order model (Table 4). Hence, dissolution profiles of plain DCN and SD (1-5), (8)(9)(10)(11) as well as (15)(16)(17)(18) followed the first order model. The rest the systems followed the Higuchi diffusion model.…”

“…It is poorly soluble, with reported aqueous solubility of 3.197 mg/mL [ 8 ]. As a result, it suffers from poor dissolution properties, reduced oral absorption [ 5 ] and consequently, lowered bioavailability equal to 35–56% [ 9 ].…”

Diacerein: A potential multi-target therapeutic drug for COVID-19

“…The main mechanism of action of DAR is inhibition of the interleukin-1 (IL-1) signalling pathway [8][9][10][12][13][14][15][16][17][18][19][20]. In addition, several studies have described the inhibitory effect of this compound on IL-6 [16,[20][21][22][23][24] and TNF-α [16,21,25,26]. However, no reported studies have addressed the potential therapeutic use of DAR in patients with COVID-19.…”

Development of orally disintegrating tablets containing solid dispersion of a poorly soluble drug for enhanced dissolution: In-vitro optimization/in-vivo evaluation

“…Although DCN is well known for its beneficial capacities in treating OA, it belongs to the Biopharmaceutics Classification System, class II (BCS II) therefore, it suffers from poor aqueous solubility (3.197 mg/mL) [10], which results in its limited dissolution and absorption [9], as well as its reduced oral bioavailability (35-56%) [11,12]. Previous formulation strategies were performed to improve DCN solubility, dissolution properties and consequently its bioavailability.…”