Having achieved a significant bioavailability of curcumin by its incorporation into SLNs (C-SLNs) during pharmacokinetic (32-155 times) and pharmacodynamic (3-4 times) studies, our intent was to proof their targeting to brain. Hence, fluorescent/confocal microscopy, biodistribution and gamma scintigraphy techniques were explored to observe the presence of C-SLNs in the brain. 1h post p.o administration of C-SLNs/free curcumin (C-S) to rats, blood was withdrawn, following which the animals were sacrificed and their harvested brains were frozen at -80°C. The obtained plasma and brain cryosections were observed for fluorescence under fluorescent/confocal microscope. Biodistribution study was performed using (99m)Tc-labeled C-SLNs and C-S in Balb/c mice after p.o. and i.v. administration and % radioactivity/g organ was recorded. Subsequent to this gamma scintigraphs of the New Zealand rabbits following similar treatments were performed. Presence of yellow fluorescent particles in plasma and brain indicated effective delivery of C-SLNs across the gut wall and the BBB. (Blood)AUCoral value for C-SLNs was 8.135 times greater than that for C-S, confirming a prolonged circulation of former. The ratio of blood AUCi.v. C-SLN/C-S in blood is ≤1 while the ratio in brain promisingly indicates 30 times higher preferential distribution of C-SLNs into brain confirming their direct delivery.

译文

通过在药代动力学(32-155倍)和药效动力学(3-4倍)研究中将姜黄素掺入SLNs(C-SLNs)中,从而获得了显着的生物利用度,我们的目的是证明其针对大脑的作用。因此,探索了荧光/共聚焦显微镜,生物分布和伽玛闪烁显像技术,以观察脑中C-SLN的存在。向大鼠口服C-SLNs /游离姜黄素(C-S)1小时后,抽血,然后处死动物,将其收获的大脑冷冻在-80°C。在荧光/共聚焦显微镜下观察获得的血浆和脑冷冻切片的荧光。口服后在Balb / c小鼠中使用(99m)Tc标记的C-SLN和C-S进行生物分布研究。和i.v.记录给药和放射性%/ g器官。此后,对新西兰兔进行类似的处理后进行了伽玛闪烁显像。血浆和脑中黄色荧光颗粒的存在表明C-SLNs可以有效地穿过肠壁和血脑屏障。 C-SLNs的AUCoral值比C-S大8.135倍,证实前者的循环时间长。血液AUCi.v.的比例血液中的C-SLN / C-S≤1,而脑中的比例有希望表明C-SLNs在脑中的优先分布高出30倍,从而证实了它们的直接递送。

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