Donepezil nanosuspension intended for nose to brain targeting: In vitro and in vivo safety evaluation
Donepezil nanosuspension intended for nose to brain targeting: In vitro and in vivo safety evaluation
复制标题
DOI：
10.1016/j.ijbiomac.2014.03.022
复制
发表时间：
2014-06-01
影响因子：
8.2
通讯作者：
Ali, Javed
中科院分区：
文献类型：
--
作者：
Bhavna;Md, Shadab;Ali, Javed
本研究旨在开发用于直接嗅觉给药的多奈哌齐纳米混悬液，其到达大脑并确定Sprague-Dawley大鼠的安全性。采用离子交联法制备纳米混悬剂。在套管（尺寸18/20）的帮助下，将开发的纳米混悬液鼻内滴注到大鼠的鼻孔中，使得药物通过鼻-脑途径直接到达脑中。纳米悬浮液的平均尺寸为150-200 nm，多分散指数为0.341。使用HPLC法估计脑匀浆中的多奈哌齐浓度。梭显示多奈哌齐在脑和血浆中的浓度分别为7.2 +/-0.86和82.8 +/-5.42 ng/ml，对于药物悬浮液，多奈哌齐在脑和血浆中的浓度分别为147.54 +/-25.08和183.451 +/-13.45 ng/ml，对于鼻内给药时相同剂量0.5 mg/ml的纳米混悬液（p
The present study was to develop donepezil loaded nanosuspension for direct olfactory administration which reaches the brain and determining safety profile in Sprague-Dawley rats. Nanosuspension was prepared by ionic-crosslinking method. The developed nanosuspension was intranasally instilled into the nostrils of rats with the help of cannula (size 18/20) so that drug reached into the brain directly via nose to brain pathway. The nanosuspension had an average size of 150-200 nm with a polydispersity index of 0.341. The donepezil concentration was estimated in the brain homogenate using HPLC method. The C. showed concentration of donepezil in brain and plasma as 7.2 +/- 0.86 and 82.8 +/- 5.42 ng/ml, respectively, for drug suspension and concentration of donepezil in brain and plasma as 147.54 +/- 25.08 and 183.451 +/- 13.45 ng/ml, respectively, for nanosuspension at same dose of 0.5 mg/ml when administered intranasally (p