Wang Xiaomei, He Haibing, Leng Wei, Tang Xing
Department of Pharmaceutics, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, China.
Int J Pharm. 2006 Jul 6;317(1):40-6. doi: 10.1016/j.ijpharm.2006.02.055. Epub 2006 Mar 12.
The uptake of estradiol into the cerebrospinal fluid (CSF) after intranasal and intravenous administration in rats was investigated to study whether direct nose-CSF transport of estradiol exits or not. Animals received 0.48 mg kg(-1) estradiol randomly methylated beta-cyclodextrin (RAMEB) inclusion complex intranasally and intravenously. Following nasal delivery, estradiol reached a C(max) value (mean+/-S.D.) in plasma (26.70+/-11.37 ng ml(-1)) and CSF (54.76+/-32.84 ng ml(-1)) after 20 min in each case, while after intravenous infusion, estradiol reached a C(max) value in plasma (170.08+/-64.67 ng ml(-1)) and CSF (26.48+/-11.34 ng ml(-1)) at 5 min and 60 min, respectively. The AUC(CSF)/AUC(plasma) ratio (1.60+/-0.67) after intranasal delivery differed significantly from the ratio (0.61+/-0.16) observed after intravenous infusion (P<0.05). All these results indicate that estradiol is transported into CSF via olfactory neurons, and, hence, there is a direct transport route from the nasal cavity into the CSF for estradiol.
为研究雌二醇是否存在从鼻腔直接运输至脑脊液的途径，对大鼠经鼻内和静脉注射给予雌二醇后其在脑脊液（CSF）中的摄取情况进行了研究。动物分别经鼻内和静脉给予0.48 mg kg(-1) 雌二醇随机甲基化β-环糊精（RAMEB）包合物。经鼻给药后，雌二醇在血浆（26.70±11.37 ng ml(-1)）和脑脊液（54.76±32.84 ng ml(-1)）中的C(max)值在每种情况下均于20分钟后达到，而静脉输注后，雌二醇在血浆（170.08±64.67 ng ml(-1)）和脑脊液（26.48±11.34 ng ml(-1)）中的C(max)值分别在5分钟和60分钟时达到。经鼻给药后的AUC(CSF)/AUC(血浆)比值（1.60±0.67）与静脉输注后观察到的比值（0.61±0.16）有显著差异（P<0.05）。所有这些结果表明，雌二醇通过嗅觉神经元转运至脑脊液，因此，存在一条从鼻腔到脑脊液的雌二醇直接运输途径。
