通过纳米载体,配方,优化,表征,动物研究和随机双盲临床试验进行皮洛西卡姆的增强性皮肤间传递
Moein Masjedi1,2, Mohammad Ali Helforoush3,4, Katayoun Rohani Rad3,5
1Department of Research and Development, Daroosazan Sorena Exir Pharmaceutical Company, Shiraz, Iran. Masjedi_m@sums.ac.ir.
AAPS PharmSciTech
|March 6, 2025
概括
这项研究开发了一种纳米-尼奥索马尔皮罗西卡姆乳液,用于局部骨关节炎和类风湿性关节炎的疼痛缓解. 在动物和临床试验中,优化的配方证明了增强的皮肤透性和显著的疼痛和炎症减少.
科学领域:
- 药理学和制药学 药理学和制药学
- 药物输送系统 药物输送系统
- 纳米技术在医学中的应用
背景情况:
- 皮罗西卡姆是一种非类固醇抗炎药物 (NSAID),用于局部治疗膝关节骨关节炎和类风湿性关节炎疼痛.
- 传统的局部配方可能在药物透和疗效方面存在局限性.
- 尼奥索姆配方有可能改善药物输送和治疗结果.
研究的目的:
- 为了制定和描述一个优化的纳米-niosomal piroxicam 乳液,以提高局部输送.
- 在炎症和疼痛的动物模型中评估纳米-niosomal piroxicam 乳膜的 in vivo 疗效.
- 在一项随机临床试验中,将纳米尼奥索马尔皮罗西卡姆乳液与常规皮罗西卡姆凝的止痛作用进行比较.
主要方法:
- 纳米尼奥索马尔皮罗西卡姆乳膜的配方,优化了尼奥索马特征 (大小,PDI,泽塔潜力,捕获效率).
- 在体外表征包括药物释放和通过皮肤透的研究.
- 在动物模型中的体内评估 (疼痛评估,前列腺素E2水平,关节胀,组织病理学) 和随机双盲临床试验.
主要成果:
- 经过优化后的体体平均尺寸为142纳米,捕获效率高 (99.48%),药物释放持续.
- 与piroxicam凝相比,尼奥索姆凝显示了通过皮肤透的3.31倍增加.
- 在动物研究中观察到膝关节胀和前列腺素E2水平的显著降低;临床试验显示了比安慰剂和阳性对照更好的止痛效果.
结论:
- 纳米-尼奥索马尔皮罗西卡姆乳液配方显示,皮肤透和积累在突组织中的增强.
- 开发的乳凝在减少疼痛和炎症方面显示出有希望的疗效,并得到动物和人类临床数据的支持.
- 这种配方代表了与骨关节炎和类风湿性关节炎相关的疼痛管理的潜在改善的治疗选择.
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