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Formulation and characterization of lornoxicam-loaded cellulosic-microsponge gel for possible applications in arthritis.
Saudi Pharmaceutical Journal ( IF 3.0 ) Pub Date : 2020-07-03 , DOI: 10.1016/j.jsps.2020.06.021
Yeteng He 1 , Khadija Majid 2 , Maimoona Maqbool 2 , Talib Hussain 3 , Abid Mehmood Yousaf 3 , Ikram Ullah Khan 4 , Yasir Mehmood 5 , Ambreen Aleem 6 , Muhammad Sohail Arshad 7 , Adnan Younus 8 , Jorabar Singh Nirwan 9 , Muhammad Usman Ghori 9 , Syed A A Rizvi 10 , Yasser Shahzad 3
Affiliation  

Rheumatoid arthritis (RA) is an autoimmune disease associated with severe joint pain. Herein, we report lornoxicam loaded cellulosic microsponge gel formulation with sustained anti-inflammatory effects that are required to manage arthritic pain. The microsponges were formulated using quasi emulsion-solvent diffusion method employing four different surfactant systems, namely polyvinyl alcohol (PVA), Tween80, Gelucire 48/16 and Gelucire 50/13. All the lornoxicam loaded microsponge formulations were extensively characterized with a variety of analytical tools. The optimized microsponge formulation was then converted into gel formulation. The lornoxicam loaded microsponge gel formulation had adequate viscosity and sufficient pharmaceutical properties as confirmed by the texture analysis and the drug release followed Super case II transport. It is noteworthy that we described the preparation of a new cellulosic polymers based microsponge system for delivery of lornoxicam to provide quick as well as lasting (sustained) anti-inflammatory effects in rats using carrageenan induced rat paw edema model. We were able to demonstrate a 72% reduction in inflammation within 4 h using the optimize transdermal gel formulation utilizing Transcutol P as permeation enhancer and with the aid of skin micro-piercing by microneedles, hence, demonstrating the potential of this microsponge gel formulation in arthritis management.



中文翻译:

装载氯诺昔康的纤维素微海绵凝胶的配方和表征可能在关节炎中的应用。

类风湿性关节炎 (RA) 是一种与严重关节疼痛相关的自身免疫性疾病。在此,我们报告了负载氯诺昔康的纤维素微海绵凝胶制剂,具有控制关节炎疼痛所需的持续抗炎作用。使用准乳液-溶剂扩散法配制微海绵,使用四种不同的表面活性剂系统,即聚乙烯醇 (PVA)、Tween80、Gelucire 48/16 和 Gelucire 50/13。所有负载氯诺昔康的微海绵制剂都用各种分析工具进行了广泛的表征。然后将优化的微海绵配方转化为凝胶配方。经质地分析证实,装载氯诺昔康的微海绵凝胶制剂具有足够的粘度和足够的药物特性,药物释放遵循 Super case II 运输。值得注意的是,我们描述了一种新的基于纤维素聚合物的微海绵系统的制备,该系统用于递送氯诺昔康,以在使用角叉菜胶诱导的大鼠爪水肿模型的大鼠中提供快速和持久的(持续)抗炎作用。我们能够证明在 4 小时内使用优化的透皮凝胶制剂,利用 Transcutol P 作为渗透增强剂并借助微针微刺穿皮肤,炎症减少了 72%,因此,证明了这种微海绵凝胶制剂在关节炎中的潜力管理。

更新日期:2020-07-03
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