用于治疗骨关节炎的载药透皮贴剂的制备与评估

Kajal, D. Sharma, Vinay Pandit, M. Ashawat
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引用次数: 0

摘要

骨关节炎(OA)是一种退行性关节疾病,由关节软骨和下层骨质破坏引起。骨关节炎最常见的症状是关节疼痛和僵硬。治疗骨关节炎的主要障碍是口服非甾体抗炎药(洛诺昔康)会产生副作用,如消化道副作用、心血管问题、肝脏问题或肾脏问题。因此,有必要开发一种透皮给药系统来运输药物,这种系统可以减少副作用,而且与口服给药相比具有多种益处,还可以开发一种新型给药系统来增强药物的渗透性,缓解骨关节炎的症状。本研究涉及用于治疗骨关节炎的含糖透皮贴片的制备和评估。为找到优化配方,进行了初步评估和表征研究。对体内释放和体外渗透研究进行了调查。制备的 Niosomes 悬浮液(F2)的粒径为 320.2 nm,Zetapotential 为 23.9 mV,药物夹带率为 79 ± 0.32%。优化配方的体外药物释放研究显示,24 小时药物释放率为 96.44 ± 0.34%。然后,将优化的 Niosome 制剂(F2)装入透皮贴片。对 Niosomal 负载透皮贴剂 F1(NLXTP)进行了体外渗透研究,结果表明其渗透性高于普通药物透皮贴剂。F1 (NLXTP) 遵循零阶释放动力学模型,显示了一种非镰刀型控制释放扩散机制。优化配方 F1(NLXTP)的体外药物释放研究表明,8 小时内药物渗透量为 2.79 ± 0.76(微克/毫升),通量值为 0.35 ± 0.55,药物保留率为 5.67%。稳定性研究表明,贴片在不同的大气条件下可稳定使用 90 天。研究发现,洛诺昔康负载的 Niosomal 透皮贴片是一种很有前景的纳米给药替代品,它在骨关节炎的日常治疗中显示出更好的夹持和释放效果,并具有良好的渗透性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Evaluation of Niosomal Loaded Transdermal Patches for the Treatment of Osteoarthritis
Osteoarthritis (OA) is a degenerative joint disease resulting from the breakdown of joint cartilage and underlying bone. The most common symptoms of osteoarthritis are joint pain and stiffness. The major hurdle in its treatment is that the oral administration of NSAIDs (Lornoxicam) causes side effects like GI side effects, cardiovascular problems, liver issues, or renal problems. Thus, there is a need to develop a Transdermal drug delivery system for the transport of drugs, which reduces side effects and has several benefits over oral delivery, and a Novel drug delivery system to enhance the permeation of drugs and give relief from symptoms of OA. This work deals with the formulation and evaluation of niosomal-loaded Transdermal Patches for the treatment of Osteoarthritis. The Niosomes were prepared using the thin film hydration method, and Niosomalloaded Transdermal patches were prepared using the Solvent Casting method. The preliminary evaluation and characterization studies were conducted to find the optimized formulation. The invitro release and ex-vivo permeation studies were investigated. Stability studies were also assessed. The prepared Niosomes suspension (F2) was found to have particle size 320.2 nm, Zeta potential 23.9 mV, and Drug entrapment 79 ± 0.32%. The in-vitro drug release studies of optimized formulation show 96.44 ± 0.34 % drug release for 24 hours. Then, the optimized Niosome formulation (F2) was loaded into the transdermal patches. The in-vitro permeation studies of Niosomal-loaded transdermal patch F1 (NLXTP) were performed, which showed a higher permeability than plain drug-loaded transdermal patch. F1 (NLXTP) followed Zero order release kinetic model, which shows a non-fickian controlled release diffusion mechanism. The ex-vivo drug release studies of optimized formulation F1 (NLXTP) show 2.79 ± 0.76 (µg/ml) drug permeated for 8 hours with a flux value of 0.35 ± 0.55, and the percentage of drug retention was found to be 5.67%. The stability studies showed that patches were stable over 90 days in different atmospheric conditions. The Lornoxicam-loaded Niosomal transdermal patch was found to be a promising nano-drug-delivery alternative that showed better entrapment and release with a permeation profile for the daily management of osteoarthritis.
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