Department of Pharmaceutics, The Applied Research Center of Medicinal Plants "ARCMP", National Organization for Drug Control and Research "NODCAR", El-Mansouria Road, El-Haram, Giza, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini St, Cairo, 11562, Egypt.
AAPS PharmSciTech. 2017 Nov;18(8):2898-2909. doi: 10.1208/s12249-017-0771-8. Epub 2017 Apr 20.
The aim of this study was to investigate the potential of surfactant-based nanovesicular system (spanlastics) for topical delivery of fenoprofen calcium (FPCa) to eliminate its oral gastrointestinal adverse effects. FPCa-loaded spanlastics were prepared by thin film hydration (TFH) technique according to a full factorial design to investigate the influence of formulation variables on the drug entrapment efficiency (%EE), particle size (PS), deformability index (DI), and the % drug released after 24 h through the cellulose membrane (Q24h) using Design-Expert® software. The optimized formula (composed of Span 60 and Tween 60 as an edge activator at weight ratio of 8: 2 in presence of Transcutol P as a cosolvent in the hydration media) exhibited the highest %EE (49.91 ± 2.60%), PS of 536.1 ± 17.14 nm, DI of 5.07 ± 0.06 g, and Q24h of 61.11 ± 2.70%; it was also characterized for morphology and physical stability. In vitro release study of FPCa-loaded spanlastic gel and conventional FPCa gel through a synthetic membrane and hairless rat skin were evaluated. The skin permeation study revealed that spanlastic gel exhibited both consistent and prolonged action. Finally, the % inhibition of carrageenan-induced rat paw edema of spanlastic gel was three times higher than the conventional FPCa gel after 24 h. In conclusion, spanlastic-based gel could be a great approach for improving topical delivery of fenoprofen calcium, providing both prolonged and enhanced anti-inflammatory activity in the treatment of arthritis.
本研究旨在探讨基于表面活性剂的纳米囊泡系统(spanlastics)在局部递芬诺芬钙(FPCa)以消除其口服胃肠道不良反应方面的潜力。采用薄膜水化(TFH)技术根据完全析因设计制备载 FPCa 的 spanlastics,以研究制剂变量对药物包封效率(%EE)、粒径(PS)、变形指数(DI)和 24 小时后通过纤维素膜释放的药物百分比(Q24h)的影响。使用 Design-Expert®软件。优化配方(由 Span 60 和 Tween 60 组成,作为边缘活性剂,重量比为 8:2,并在水化介质中加入 Transcutol P 作为共溶剂)表现出最高的 %EE(49.91±2.60%)、PS 为 536.1±17.14nm、DI 为 5.07±0.06g 和 Q24h 为 61.11±2.70%;还对其形态和物理稳定性进行了表征。通过合成膜和无毛大鼠皮肤评估了载 FPCa 的 spanlastic 凝胶和常规 FPCa 凝胶的体外释放研究。皮肤渗透研究表明,spanlastic 凝胶表现出一致和持久的作用。最后,在 24 小时后,spanlastic 凝胶对角叉菜胶诱导的大鼠爪肿胀的抑制率是常规 FPCa 凝胶的三倍。总之,基于 spanlastics 的凝胶可以是改善芬诺芬钙局部递送的一种很好的方法,为关节炎的治疗提供了延长和增强的抗炎活性。