He Yeteng, Majid Khadija, Maqbool Maimoona, Hussain Talib, Yousaf Abid Mehmood, Khan Ikram Ullah, Mehmood Yasir, Aleem Ambreen, Arshad Muhammad Sohail, Younus Adnan, Nirwan Jorabar Singh, Ghori Muhammad Usman, Rizvi Syed A A, Shahzad Yasser
Department of Orthopedic Surgery, The First Affiliated Hospital of Shandong First Medical University, Jinan, Shandong Province 250000, China.
Facuty of Pharmacy, University of Central Punjab, Lahore 54000, Pakistan.
Saudi Pharm J. 2020 Aug;28(8):994-1003. doi: 10.1016/j.jsps.2020.06.021. Epub 2020 Jul 3.
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.
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，我们报告了载有氯诺昔康的纤维素微球凝胶制剂，其具有持续的抗炎作用，这对于控制关节炎疼痛是必需的。微球采用准乳液 - 溶剂扩散法制备，使用四种不同的表面活性剂体系，即聚乙烯醇（PVA）、吐温80、Gelucire 48/16和Gelucire 50/13。所有载有氯诺昔康的微球制剂都用各种分析工具进行了广泛表征。然后将优化后的微球制剂转化为凝胶制剂。经质地分析证实，载有氯诺昔康的微球凝胶制剂具有足够的粘度和良好的药学性质，且药物释放遵循超Ⅱ型转运。值得注意的是，我们描述了一种基于纤维素聚合物的新型微球系统的制备，用于氯诺昔康的递送，以在使用角叉菜胶诱导的大鼠足肿胀模型的大鼠中提供快速且持久（持续）的抗炎作用。使用以Transcutol P作为渗透促进剂并借助微针进行皮肤微穿刺的优化透皮凝胶制剂，我们能够在4小时内使炎症减少72%，因此，证明了这种微球凝胶制剂在关节炎治疗中的潜力。
