Li N, Je Y J, Yang M, Jiang X H, Ma J H
West China School of Pharmacy, Sichuan University, Chengdu.
Pharmazie. 2011 May;66(5):374-7.
The aim of this study is to determine whether baicalin can be transferred along the olfactory pathway to the brain after nasal administration of baicalin phospholipid (BP) complex to rats, thereby circumventing the blood brain barrier. The concentration of baicalin in plasma and different brain tissues (olfactory bulb, cerebral cortex, striatum and cerebellum) were measured by high-performance liquid chromatography (HPLC). The ratios of the area under the concentration-time curve (AUC) values of intranasal to intravenous administrations were 54.21%, 240.59%, 374.71%, and 114.54% in plasma, cerebral cortex, striatum, and cerebellum, respectively. In the olfactory bulb, the AUC values of intranasal to intravenous administrations were 3355.4 +/- 378.8 microg/g-min versus 0 microg/g x min following intravenous administration. The ratios of AUC values of intranasal to intravenous administrations were72.75 %, 240.59 %, 374.71%, 114.54% in plasma, cortex, striatum, cerebellum respetively. The proportion of baicalin in the brain tissues from the olfactory transfer was also calculated, and the result shows that, following intranasal administration, approximately 52.36%-100% baicalin content at 8 h was transported to the brain via the olfactory pathway. In conclusion, the BP complex is transferred into the olfactory bulb via the olfactory pathway in rats, and the BP complex intranasal delivery is a promising approach to protect against cerebral ischemic injury.
本研究的目的是确定大鼠经鼻腔给予黄芩苷磷脂（BP）复合物后，黄芩苷是否能沿嗅觉通路转运至脑内，从而绕过血脑屏障。采用高效液相色谱法（HPLC）测定血浆和不同脑组织（嗅球、大脑皮层、纹状体和小脑）中黄芩苷的浓度。血浆、大脑皮层、纹状体和小脑中，鼻内给药与静脉给药的浓度-时间曲线下面积（AUC）值之比分别为54.21%、240.59%、374.71%和114.54%。在嗅球中，鼻内给药与静脉给药的AUC值分别为3355.4±378.8μg/g·min和静脉给药后的0μg/g·min。血浆、皮层、纹状体、小脑中鼻内给药与静脉给药的AUC值之比分别为72.75%、240.59%、374.71%、114.54%。还计算了经嗅觉转运至脑组织中的黄芩苷比例，结果表明，鼻内给药后，8小时时约52.36%-100%的黄芩苷含量经嗅觉通路转运至脑内。综上所述，BP复合物在大鼠中经嗅觉通路转运至嗅球，鼻内给予BP复合物是预防脑缺血损伤的一种有前景的方法。
