title: Microdialysis pharmacokinetic study of scopolamine in plasma, olfactory bulb and vestibule after intranasal administration.
abstract: The purpose of this study was to investigate the microdialysis pharmacokinetic of scopolamine in plasma, olfactory bulb and vestibule after intranasal administration. The pharmacokinetic study of subcutaneous and oral administration was also performed in rats. From the in vivo results, scopolamine intranasal administration can avoid hepatic first-pass effect. Tmax plasma samples after intranasal administration were significantly faster than oral administration and subcutaneous injection. The relative bioavailability of intranasal administrations was 51.8-70% when compared with subcutaneous injection. Moreover, one can see that in comparison with scopolamine subcutaneous administration, scopolamine intranasal gel and solutions can increased drug target index (DTI) with olfactory bulb 1.69 and 2.05, vestibule 1.80 and 2.15, respectively. The results indicated that scopolamine can be absorbed directly through the olfactory mucosa into the olfactory bulb, and then transported to various brain tissue after intranasal administration, with the characteristics of brain drug delivery.
authors.affiliation: a Department of Pharmaceutics, School of Pharmacy , Fudan University , Shanghai , China .
authors.forename: Yan
authors.initials: Y
authors.lastname: Wei
authors.affiliation: b Department of Oncology, Changhai Hospital , Second Military Medical University , China .
authors.forename: Mingzhen
authors.initials: M
authors.lastname: Ying
authors.affiliation: b Department of Oncology, Changhai Hospital , Second Military Medical University , China .
authors.forename: Shuai
authors.initials: S
authors.lastname: Xu
authors.affiliation: c Shanghai Institute of Pharmaceutical Industry , Shanghai , China , and.
authors.forename: Feng
authors.initials: F
authors.lastname: Wang
authors.affiliation: d Department of Pharmaceutics , Yangtze river Pharmaceutical Group , Taizhou , China.
authors.forename: Aifeng
authors.initials: A
authors.lastname: Zou
authors.affiliation: a Department of Pharmaceutics, School of Pharmacy , Fudan University , Shanghai , China .
authors.forename: Shilei
authors.initials: S
authors.lastname: Cao
authors.affiliation: a Department of Pharmaceutics, School of Pharmacy , Fudan University , Shanghai , China .
authors.forename: Xinguo
authors.initials: X
authors.lastname: Jiang
authors.affiliation: b Department of Oncology, Changhai Hospital , Second Military Medical University , China .
authors.forename: Yajie
authors.initials: Y
authors.lastname: Wang
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001682:Biological Availability; D016503:Drug Delivery Systems; D017551:Microdialysis; D009830:Olfactory Bulb / Q000378:metabolism*; D009831:Olfactory Mucosa / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D012601:Scopolamine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D014722:Vestibule, Labyrinth / Q000378:metabolism*
chemical_list: D000932:Antiemetics; D012601:Scopolamine
keywords: Intranasal drug delivery; microdialysis; motion sickness; pharmacokinetics; scopolamine