A Novel Oil-Body Nanoemulsion Formulation of Ginkgolide B: Pharmacokinetics Study and In Vivo Pharmacodynamics Evaluations

被引：16

作者：

Yang, Pengfei ^{[1
,2
,3
]}

Cai, Xiaolei ^{[1
,2
,3
]}

Zhou, Kai ^{[1
,2
,3
]}

Lu, Chuanhua ^{[1
]}

Chen, Weidong ^{[1
]}

机构：

[1] Anhui Univ Chinese Med, Pharmacokinet Lab, Hefei 230038, Anhui, Peoples R China

[2] Anhui Univ Chinese Med, Sch Pharm, Hefei 230038, Anhui, Peoples R China

[3] Anhui Univ Chinese Med, Inst Pharmacokinet, Hefei 230038, Anhui, Peoples R China

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 2014年 / 103卷 / 04期

关键词：

nanoemulsion; Ginkgolide B; Alzheimer's disease; amyloid (25-35); pharmacokinetics; pharmacodynamics; CNS; blood brain barrier; BETA; BIOAVAILABILITY;

D O I：

10.1002/jps.23866

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The goal of this study was to develop a novel oil-body nanoemulsion (ONE) for Ginkgolide B (GB) and to conduct pharmacokinetics and pharmacodynamics evaluations. GB-ONE was prepared by O/O emulsion method. The differences in pharmacokinetics parameters and tissue distribution of rats after oral administrated with GB-ONE were investigated by liquid chromatography-tandem mass spectrometry. Changes in the ethological and pathological characterizations of the Alzheimer's disease rats after treated with GB-ONE were evaluated by Morris water maze (MWM) and pathological section, respectively. Furthermore, choline acetyltransferase (ChAT) and acetylcholinesterase (AchE) activity in hippocampus was analyzed by spectrophotometric method. The results indicated that the AUC of GB in rats' plasma was significantly improved after incorporated into ONE, and GB-ONE was significantly targeted into brain. In MWM experiment, memory improvement of rats with cognition impaired was confirmed after administrated with GB-ONE. Furthermore, GB-ONE significantly inhibited AchE activity and enhanced the activity of ChAT in the hippocampus. The overall results implicated that the novel ONE was effective for improving the drawbacks of GB and showed great potential for clinical application. (c) 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:1075-1084, 2014

引用

页码：1075 / 1084

页数：10

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