Evaluation of brain-targeting for the nasal delivery of estradiol by the microdialysis method

International Journal of Pharmaceutics
Xiaomei WangXing Tang

Abstract

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.

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Citations

Jul 31, 2013·Drug Delivery and Translational Research·Lipa ShahMansoor Amiji
Dec 19, 2009·Expert Opinion on Drug Delivery·Santosh Pasha, Kshitij Gupta
Aug 28, 2010·Journal of Pharmaceutical Sciences·Kiruba FlorenceMisra Ambikanandan
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Aug 8, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Xiaomei WangXing Tang
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