[Brain targeting of gastrodin nasal in situ gel].
OBJECTIVE
To investigate the biodistribution of gastrodin ion-activated nasal in situ gel in rat blood and brain tissues and to evaluate its brain targeting.


METHODS
Intravenous administration of gastrodin solution or intranasal administration of gastrodin nasal in situ gel were given to 32 rats, respectively. The concentrations of gastrodin in the plasma and gastrodigenin in the brain tissues of the rats were determined by HPLC.


RESULTS
The intranasal administration of the in situ gel of gastrodin produced more significant brain targeting effect than the intravencus administration of gstrodin solution (P < 0.01). The area under curve (AUC) of cerebrum, cerebellum and olfactory bulb increased by 1.16, 0.77 and 3.34 times, with 2.66. 2.18 and 5.34 brain targeting indexes (BTI), respectively. The mean residence time (MRT) increased by nearly four-folds.


CONCLUSIONS
Gastrodin nasal in situ gel can improve the brain targeting of gastrodin and slow its release.
Department of Pharmaceutics, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Zheng
Z
Cai
Shi-Xiang
SX
Hou
Zhao-Xiang
ZX
Yang
Xiang-Rong
XR
Song
Qiu-Hong
QH
Chen
Yuan-Bo
YB
Li
Bin-Bin
BB
Zhao
D000281:Administration, Intranasal; D000818:Animals; D019540:Area Under Curve; D001592:Benzyl Alcohols / Q000008:administration & dosage* / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics; D001921:Brain / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D054022:Cerebrum / Q000378:metabolism; D016503:Drug Delivery Systems; D005260:Female; D005782:Gels; D005960:Glucosides / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D008297:Male; D009830:Olfactory Bulb / Q000378:metabolism; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D001592:Benzyl Alcohols; D005782:Gels; D005960:Glucosides; C018966:4-hydroxybenzyl alcohol; C045345:gastrodin