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评价前体脂质体作为优化吡罗昔康经皮传递的替代策略。

Evaluation of proniosomes as an alternative strategy to optimize piroxicam transdermal delivery.

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

J Microencapsul. 2009 May;26(3):272-8. doi: 10.1080/02652040802305618. Epub 2008 Oct 20.

Abstract

The current investigation aims to evaluate the transdermal potential of niosomes bearing a potent non-steroidal anti-inflammatory, piroxicam. Piroxicam-loaded niosomes were prepared and characterized for surface morphology, entrapment efficiency and in vitro permeation across excised rat skin from various proniosome gel formulations using Franz diffusion cells. Various non-ionic surfactants were used to achieve optimum encapsulation efficiency. The prepared proniosomes significantly improved drug permeation and reduced the lag time (p < 0.05). Proniosomes prepared with Span 60 provided a higher piroxicam flux across the skin than did those prepared with Tween 80. Niosomes prepared using Span 60 showed a higher release rate than those prepared using non-ionic surfactants, Span 20 and Span 80, while those prepared from Tween showed higher release rate than formula prepared with Span. This indicates that lipophilicity and hydrophilicity of surfactant has a main role in release rates of piroxicam. Particle size of piroxicam niosomal vesicles formed by proniosome was determined by scanning electron microscopy. The encapsulation efficiency was evaluated by a specific high performance liquid chromatography method. Niosomes formed from using Spans and Tweens exhibited very high encapsulation efficiency. The results are very encouraging and suggest that niosomes can act as promising carriers offering an alternative approach for transdermal delivery of piroxicam.

摘要

当前的研究旨在评估含有一种强效非甾体抗炎药吡罗昔康的类脂体的经皮潜力。制备并表征了载有吡罗昔康的类脂体,用于研究从不同的前体胶束凝胶制剂中通过离体大鼠皮肤的体外渗透,使用 Franz 扩散池。使用各种非离子表面活性剂以实现最佳包封效率。与载药前体胶束相比,所制备的前体胶束显著提高了药物渗透并减少了滞后时间(p < 0.05)。与吐温 80 相比,用 Span 60 制备的前体胶束提供了更高的吡罗昔康跨皮通量。用 Span 60 制备的前体胶束比用非离子表面活性剂、Span 20 和 Span 80 制备的前体胶束具有更高的释放率,而用吐温制备的前体胶束比用 Span 制备的前体胶束具有更高的释放率。这表明表面活性剂的亲脂性和亲水性对吡罗昔康的释放速率有主要作用。扫描电子显微镜用于确定由前体胶束形成的吡罗昔康类脂体囊泡的粒径。通过特定的高效液相色谱法评估包封效率。用 Span 和 Tweens 形成的类脂体表现出非常高的包封效率。这些结果非常令人鼓舞,表明类脂体可以作为有前途的载体,为吡罗昔康的经皮给药提供一种替代方法。

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