A comparative study of oral diacerein and transdermal diacerein as Novasomal gel in a model of MIA induced Osteoarthritis in rats

IF 1.1 Q4 PHARMACOLOGY & PHARMACY
N. Fareed, H. Kassab
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Abstract

Background: Osteoarthritis is a chronic pathology of the joints causing disability and morbidity. Diacerein is a disease-modifying agent indicated for osteoarthritis management with enhanced performance and have much lower side effects profile than conventional non-steroidal anti-inflammatory drugs. Oral administration of Diacerein is associated with a laxative effect , thus causing treatment discontinuation. Aim: This study aimed to evaluate the activity of Diacerein novasome-based transdermal gel compared with standard oral treatment in the management of induced osteoarthritis in a rat model. Materials and methods: A single intra-articular injection of monosodium iodoacetate was administered to the left knee joint, resulting in the development of Osteoarthritis. Disease progression and the effect of both routes of Diacerein treatment were evaluated by morphological, biochemical, histological, and radiological studies. Results: Osteoarthritis was successfully induced in rats’ knee joints. Morphological studies revealed that both Diacerein treatments significantly reduced joint swelling as compared to the untreated group. The serum TNF-α and IL-1β levels were significantly lower in both Diacerein treatment groups as compared to the untreated group throughout the course of the study. Histological and radiological findings confirmed that transdermal Diacerein treatment protects against cartilage degradation like oral treatment. Conclusion: Novasomal technology proved its efficacy as a carrier for the transdermal delivery of Diacerein. The in-vivo study on an animal model of osteoarthritis showed that Diacerein transdermal gels provided sufficient pharmacological activity for the attenuation of the disease. This finding could support its use as an alternative to the standard oral treatment to avoid side effects.
在 MIA 诱导的大鼠骨关节炎模型中口服迪卡瑞林与透皮迪卡瑞林(Novasomal 凝胶)的比较研究
背景:骨关节炎是一种慢性关节病变,会导致残疾和发病。与传统的非甾体抗炎药物相比,Diacerein 是一种可改善骨关节炎症状的药物,具有更强的疗效和更低的副作用。口服双醋瑞因具有通便作用,因此会导致治疗中断。 目的:本研究旨在评估基于新生物体的透皮凝胶与标准口服治疗相比,在大鼠模型中治疗诱发骨关节炎的活性。 材料与方法在左膝关节内注射一次碘乙酸钠,导致骨关节炎的发生。通过形态学、生物化学、组织学和放射学研究评估了疾病的进展以及两种双醋瑞因治疗途径的效果。 结果显示大鼠膝关节成功诱发了骨关节炎。形态学研究表明,与未处理组相比,两种 Diacerein 处理方法都能明显减轻关节肿胀。在整个研究过程中,与未处理组相比,两种双醋瑞因处理组的血清 TNF-α 和 IL-1β 水平均明显降低。组织学和放射学研究结果证实,透皮泻肝素治疗与口服治疗一样能防止软骨退化。 结论Novasomal 技术证明了其作为透皮给药载体的功效。对骨关节炎动物模型进行的体内研究表明,透皮 Diacerein 凝胶具有足够的药理活性,可减轻骨关节炎。这一发现支持将其用作标准口服治疗的替代品,以避免副作用。
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来源期刊
Pharmacia
Pharmacia PHARMACOLOGY & PHARMACY-
CiteScore
2.30
自引率
27.30%
发文量
114
审稿时长
12 weeks
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