天麻素鼻用原位凝胶脑靶向性研究

Brain Targeting of Gastrodin Nasal in situ Gel

目的研究天麻素离子敏感鼻用原位凝胶在大鼠体内血液与脑组织中的药物分布,并评价其脑靶向性。方法大鼠静注天麻素溶液或经鼻给予天麻素鼻用原位凝胶后,采用HPLC法分别测定血浆中的天麻素及脑组织中天麻苷元的浓度。结果与静注天麻素溶液组相比,鼻用原位凝胶组大鼠脑组织中的药物分布显著增加(P<0.01),大脑、小脑及嗅球的药时同线下面积分别增加1.16、0.77及3.34倍,脑靶向指数分别为:2.66、2.18及5.34,药物平均滞留时间增加近4倍。结论天麻素鼻用原位凝胶具有一定的脑靶向性与缓释作用。

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. Conclusion Gastrodin nasal in situ gel can improve the brain targeting of gastrodin and slow its release.