Suppr超能文献

水合杨梅素尼欧体的配方、表征和药代动力学研究,该尼欧体由各种非离子表面活性剂制备而成。

Formulation, characterization and pharmacokinetics of Morin hydrate niosomes prepared from various non-ionic surfactants.

机构信息

Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Department of Pharmaceutics, Faculty of Pharmacy, University of Gezira, Wad Medani P.O. Box 20, Sudan.

出版信息

Int J Pharm. 2013 Nov 18;456(2):446-58. doi: 10.1016/j.ijpharm.2013.08.040. Epub 2013 Aug 30.

Abstract

Morin hydrate (MH), a bioflavonoid with antioxidant and anticancer activity as well as the ability to improve the bioavailability of other drugs on their concurrent use. Three differently optimized niosomal formulations using three different non-ionic surfactants (Span 60, Span 80 and Tween 60) were achieved by (L9 (3(4))) Taguchi orthogonal array (TOA). The analysis of TOA revealed that Tween 60 Niosomes had the highest entrapment efficiency (93.4%) compared to other optimized Niosomal formulations (71-79%). In terms of MH remaining %, Tween 60 Niosomes were found to be the most stable (89%) at 4 °C over one month compared to Span 60 (56%) and Span 80 (57%) Niosomes. The release pattern in all Niosomal formulations was found to follow the Weibull model and Tween 60 Niosomes had the highest release rate. The molecular modeling simulation explained the binding of MH to the human serum albumin (HSA) by hydrogen bonds during the in vitro release process. As for the bioavailability, the AUC0-8 showed 1.3-2.7 fold increase compared to the MH solution. Ex vivo images of the excised organs showed that MH could accumulate in brain which indicates that MH-Tween 60 Niosomes might be a possible candidate to deliver hydrophobic drugs and overcome the blood-brain barrier (BBB) penetration.

摘要

甘露水合物(MH)是一种具有抗氧化和抗癌活性的生物类黄酮,能够提高同时使用的其他药物的生物利用度。使用三种不同的非离子表面活性剂(Span 60、Span 80 和 Tween 60)通过(L9(3(4)))Taguchi 正交数组(TOA)实现了三种不同优化的囊泡制剂。TOA 的分析表明,与其他优化的囊泡制剂(71-79%)相比,Tween 60 囊泡具有最高的包封效率(93.4%)。就 MH 剩余百分比而言,与 Span 60(56%)和 Span 80(57%)囊泡相比,Tween 60 囊泡在 4°C 下一个月内是最稳定的(89%)。所有囊泡制剂的释放模式均发现符合 Weibull 模型,并且 Tween 60 囊泡具有最高的释放速率。分子建模模拟解释了 MH 在体外释放过程中通过氢键与人血清白蛋白(HSA)结合。至于生物利用度,AUC0-8 与 MH 溶液相比增加了 1.3-2.7 倍。切除器官的体外图像显示 MH 可以在大脑中积累,这表明 MH-Tween 60 囊泡可能是一种潜在的候选药物,可用于输送疏水性药物并克服血脑屏障(BBB)渗透。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验