聚氧乙烯蓖麻油微乳对血脑屏障通透性的影响

Effect of Cremophor-based Microemulsion on the Permeability of Blood Brain Barrier

目的 :以伊文思蓝为指示剂 ,研究聚氧乙烯蓖麻油 (cremophor)微乳对血脑屏障通透性的影响。方法 :采用甲酰胺提取 紫外分光光度法测定小鼠各脏器中伊文思蓝的浓度 ,比较不同微乳体系中伊文思蓝在小鼠体内的组织分布情况。结果 :伊文思蓝在脑组织中的浓度依次为 :聚氧乙烯蓖麻油微乳、陈皮油微乳、(cre mophor/Tween 80为 1∶1)微乳、Tween 80微乳、胶束、伊文思蓝水溶液。其中聚氧乙烯蓖麻油微乳、陈皮油微乳组脑中伊文思蓝的浓度分别为水溶液组的 5 . 0倍、3 2倍 (P <0 . 0 1) ,胶束组的 3 0倍、1 9倍 (P <0 . 0 5 ) ,脑靶向效果显著。结论 :微乳对血脑屏障通透性有一定的促进作用 ,且聚氧乙烯蓖麻油开放血脑屏障的作用较Tween 80强。

AIM:To study the effect of cremophor-based microemulsion on the permeability of blood brain barrier by using Evens blue as the indicator.METHOD: A formamide extraction-ultraviolet spectrophotometry was employed to determine the concentrations of Evens blue in tissues of rats,and the in vivo distribution of the solution group,micelle group and microemulsion groups containing Evens blue in mice was studied.RESULT: The concentrations of the Evens blue in the brain after each formulation being administered to mice by caudal vein were as follows(from the highest to the lowest):cremophor-based microemulsion group,the tangerine peel oil-based micreomulsion group,cremophor/Tween-80-based microemulson group,Tween-80-based microemulsion group,micelle group and aqueous solution group.The concentrations of Evens blue in the brain in the cremophor-based microemulsion group and the tangerine peel oil-based micreomulsion group were 5.0 times and 3.2 times higher than those in the aqueous solution group while 3.0 times and 1.9 times higher than those in the micelle group respectively.CONCLUSION:The microemulsions might facilitate the transporting of Evens blue across the blood brain barrier.