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作者

HOU Xue-qin RONG Cui-ping HAO Ji-fu ZHANG Han-ting

作者单位

Institute of Pharmacology,Taishan Medical University,Shandong,271016,China；Guangxi Key Laboratory of Brain and Cognitive Neuroscience,Guilin Medical University,Guilin,China；Department of Pharmacy,Taishan Medical University,Shandong,271016,China；Departments of Behavioral Medicine&Psychiatry,Physiology&Pharmacology,and Neuroscience,the Rockefeller Neurosciences Institute,West Virginia University Health Sciences Center,Morgantown,WV 26506,USA

刊名

神经药理学报

年份

2018

卷号

第8卷

期号

第4期

页码

101-102

ISSN

2095-1396

关键词

OSTHOLE NANOEMULSIONS Pseudo-ternary phase DIAGRAM NASAL administration CHOLINERGIC nerve circuits

分类号

R73

摘要

Objectives:Fructus Cnidii is the dry ripe fruit of Cnidium monnieri(L.)Cuss.,which belongs to the umbelliferous plant.It has long been used in clinic practice and has been found to have pharmacological activity in the central nervous system.Osthole is the main active component of Fructus Cnidii.However,it shows low bioavailability,fast distribution and elimination,and low concentration in the brain when given orally.In this study,we aimed to develop a new dosage form to increase the osthole conc...更多

Objectives:Fructus Cnidii is the dry ripe fruit of Cnidium monnieri(L.)Cuss.,which belongs to the umbelliferous plant.It has long been used in clinic practice and has been found to have pharmacological activity in the central nervous system.Osthole is the main active component of Fructus Cnidii.However,it shows low bioavailability,fast distribution and elimination,and low concentration in the brain when given orally.In this study,we aimed to develop a new dosage form to increase the osthole concentration in the brain and enhance its pharmacological effects in the central nervous system through reducing the dosage while improving the stability and bioavailability.Thus,microemulsion containing osthole was prepared and the effects of osthole microemulsion were examined in the mouse model of Alzheimer’s disease(AD).Methods:On the basis of pseudo-ternary phase diagram,microemulsion was prepared by using polyoxyethlated Cremophor RH40 as emulsifiers,propylene glycol as assistant emulsifiers and ethyl acetate as the oil phase.The particle size and distribution of osthole microemulsion were detected by laser particle size analyzer and transmission election microscope.The content of osthole was determined by UV spectrophotometry.The effects of osthole microemulsion by nasal administration on the learning and memory abilities in scopolamine-treated mice were assessed by Morris water maze and novel object recognition tests.The superoxide dismutase(SOD)activity,glutathione(GSH)levels and malondialdehyde(MDA)contents in the serum were examined to evaluate the oxidant stress.Choline acetyltransferase(ChAT)and acetylcholinesterase(AChE)expression in the olfactory-basal forebrain pathway were detected by immunohistochemical analysis.We also investigated the acetylcholine(ACh)levels and the histological morphology in the brain.Results:The average particle size of 1μg·μL-1 osthole microemulsion was less than 15 nm.It was characterized as spheres under the transmission electron microscopy,and the osthole was completely encapsu收起

学科

【教育部学科】医学

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