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酮洛芬在棕榈油酯纳米乳中的抗炎和镇痛作用

Anti-inflammatory and analgesic effects of ketoprofen in palm oil esters nanoemulsion.

作者信息

Sakeena M H F, Yam M F, Elrashid S M, Munavvar A S, Azmin M N

机构信息

Department of Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains Malaysia.

出版信息

J Oleo Sci. 2010;59(12):667-71. doi: 10.5650/jos.59.667.

Abstract

Ketoprofen is a potent non-steroidal anti-inflammatory drug has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of ketoprofen produces serious gastrointestinal adverse effects. One of the promising methods to overcome these adverse effects is to administer the drug through the skin. The aim of the present work is to evaluate the anti-inflammatory and analgesic effects from topically applied ketoprofen entrapped palm oil esters (POEs) based nanoemulsion and to compare with market ketoprofen product, Fastum(®) gel. The novelty of this study is, use of POEs for the oil phase of nanoemulsion. The anti-inflammatory and analgesic studies were performed on rats by carrageenan-induced rat hind paw edema test and carrageenan-induced hyperalgesia pain threshold test to compare the ketoprofen entrapped POEs based nanoemulsion formulation and market formulation. Results indicated that there are no significant different between ketoprofen entrapped POEs nanoemulsion and market formulation in carrageenan-induced rat hind paw edema study and carrageenan-induced hyperalgesia pain threshold study. However, it shows a significant different between POEs nanoemulsion formulation and control group in these studies at p<0.05. From these results it was concluded that the developed nanoemulsion have great potential for topical application of ketoprofen.

摘要

酮洛芬是一种强效非甾体抗炎药,已用于治疗各种疼痛、炎症和关节炎。然而,口服酮洛芬会产生严重的胃肠道不良反应。克服这些不良反应的一种有前景的方法是通过皮肤给药。本研究的目的是评估基于棕榈油酯(POEs)包裹酮洛芬的纳米乳剂局部应用的抗炎和镇痛效果,并与市售酮洛芬产品法斯通(Fastum)凝胶进行比较。本研究的新颖之处在于,将POEs用于纳米乳剂的油相。通过角叉菜胶诱导的大鼠后爪水肿试验和角叉菜胶诱导的痛觉过敏疼痛阈值试验,在大鼠身上进行抗炎和镇痛研究,以比较基于POEs包裹酮洛芬的纳米乳剂配方和市售配方。结果表明,在角叉菜胶诱导的大鼠后爪水肿研究和角叉菜胶诱导的痛觉过敏疼痛阈值研究中,基于POEs包裹酮洛芬的纳米乳剂与市售配方之间没有显著差异。然而,在这些研究中,POEs纳米乳剂配方与对照组在p<0.05时有显著差异。从这些结果可以得出结论,所开发的纳米乳剂在酮洛芬局部应用方面具有巨大潜力。

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