Department of Pharmaceutics, Nanoformulation Research Lab, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India.
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj,11942, Saudi Arabia.
Curr Drug Deliv. 2020;17(10):885-897. doi: 10.2174/1567201817666200724170203.
The present work aimed to develop an ethosomal gel of naproxen sodium for the amelioration of rheumatoid arthritis.
In the present work, we have explored the potential of ethosomes to deliver naproxen into deeper skin strata. Further, the anti-inflammatory efficacy of naproxen ethosomal formulation was assessed using the carrageenan-induced rat paw edema model.
Naproxen sodium nanoethosomes were prepared using different proportions of lipoid S100 (50mg-200mg), ethanol (20-50%) and water, and were further characterized on the basis of vesicle morphology, entrapment efficiency, zeta potential, in-vitro drug release and ex-vivo permeation studies.
The optimized ethosomal formulation was found to have 129 ± 0.01 nm particle size, 0.295 Polydispersity Index (PDI), -3.29 mV zeta potential, 88% entrapment efficiency and 96.573% drug release in 24 hours. TEM and SEM analysis of the optimized formulation showed slightly smooth spherical structures. The Confocal laser scanning microscopy showed that ethosomes could easily infiltrate into deeper dermal layers (upto 104.9μm) whereas the hydroalcoholic solution of the drug could penetrate up to 74.9μm. Further, the optimized ethosomal formulation was incorporated into 1% carbopol 934 gel base and optimized wherein the transdermal flux was found to be approximately 10 times more than the hydroethanolic solution. Also, the in-vivo pharmacodynamic study of the optimized ethosomal gel exhibited a higher percentage inhibition of swelling paw edema than marketed diclofenac gel.
The ethosomal gel was successfully developed and has shown the potential to be a good option for the replacement of conventional therapies of rheumatoid arthritis.
本工作旨在开发一种萘普生钠的醇质体凝胶,以改善类风湿性关节炎。
在本工作中,我们探索了醇质体将萘普生递送至更深皮肤层的潜力。此外,使用角叉菜胶诱导的大鼠足肿胀模型评估了萘普生醇质体制剂的抗炎功效。
使用不同比例的脂质 S100(50mg-200mg)、乙醇(20-50%)和水制备萘普生钠纳米醇质体,并基于囊泡形态、包封效率、ζ电位、体外药物释放和离体渗透研究对其进行进一步表征。
发现优化的醇质体制剂具有 129±0.01nm 粒径、0.295 多分散指数(PDI)、-3.29mV ζ电位、88%包封效率和 24 小时内 96.573%的药物释放。优化制剂的 TEM 和 SEM 分析显示出略微光滑的球形结构。共聚焦激光扫描显微镜显示,醇质体可以轻易地渗透到更深的真皮层(最多 104.9μm),而药物的水醇溶液只能渗透到 74.9μm。此外,将优化的醇质体制剂掺入 1%卡波姆 934 凝胶基质中并进行优化,发现其透皮通量大约是水醇溶液的 10 倍。此外,优化的醇质体凝胶的体内药效学研究表明,对肿胀足肿胀的抑制百分比高于市售双氯芬酸钠凝胶。
成功开发了醇质体凝胶,并且显示出作为替代传统类风湿关节炎治疗方法的良好选择的潜力。