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