| In vivo: |
| Nanomedicine. 2014 Jul;10(5):1031-40. | | Targeting of diacerein loaded lipid nanoparticles to intra-articular cartilage using chondroitin sulfate as homing carrier for treatment of osteoarthritis in rats.[Pubmed: 24512762] | Targeted delivery of antiosteoarthritic drug diacerein to articular tissue could be a major achievement and soluble polysaccharide chondroitin sulfate (ChS) may be a suitable agent for this.
METHODS AND RESULTS:
Therefore, diacerein loaded solid lipid nanoparticles modified with ChS (ChS-DC-SLN) were prepared for synergistic effect of these agents to combat multidimensional pathology of osteoarthritis (OA). Prepared formulation were of size range 396±2.7nm, showed extended release up to 16h and increased bioavailability of diacerein by 2.8 times. ChS-DC-SLN were evaluated for their effect on histopathology of femoro-tibial joint of rat knee and amount of ChS and rhein (an active metabolite of diacerein) at targeted site. Concentration of rhein was significantly higher in case of ChS-DC-SLN (7.8±1.23μg/ml) than that of drug dispersion (2.9±0.45μg/ml). It can be stated that ChS served as homing to articular cartilage for targeting of drug.
CONCLUSIONS:
Thus, ChS-DC-SLN have great potential to enhance the overall efficacy of treatment for OA. | | Clin Ther. 2013 Apr;35(4):431-9. | | The efficacy of diacerein in hand osteoarthritis: a double-blind, randomized, placebo-controlled study.[Pubmed: 23474153] | Diacerein is a drug used in osteoarthritis (OA) that elicits an inhibitory effect on interleukin-1 and metalloproteases. Although Diacerein has shown modest efficacy and safety in the treatment of knee and hip OA, there have been no placebo-controlled clinical trials for hand OA. The aim of the current study was to investigate the efficacy and tolerability of Diacerein in patients with hand OA.
METHODS AND RESULTS:
Patients fulfilling the American College of Rheumatology criteria for hand OA participated in this randomized, double-blind, placebo-controlled study. Eligible patients were >40 years of age, had at least 1 tender joint, and had a joint pain visual analog scale of >30 mm. Patients received Diacerein (50 mg) or placebo BID for 12 weeks. The primary end point was the Australian/Canadian Osteoarthritis Hand Index (AUSCAN) pain score at 4 weeks. Secondary end points were AUSCAN pain score at 12 weeks and AUSCAN physical function and stiffness score, patient and physician global assessment, functional index of hand OA scores, and multidimensional health assessment questionnaire results at 4 weeks and 12 weeks. Eighty-six Korean patients were enrolled (42 Diacerein, 44 placebo). The intention-to-treat and per-protocol analyses revealed no significant differences between the 2 groups in terms of change in AUSCAN pain score at 4 weeks, except for improvement in physician global assessment at 4 weeks (per-protocol analysis, P = 0.004). The safety profile of Diacerein was comparable to placebo, except for frequent discoloration of the urine (88% vs 20%).
CONCLUSIONS:
These results suggest that Diacerein 50 mg BID may be ineffective in controlling the symptoms of hand OA. |
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