IR@PKUHSC  > 北京大学药学院  > 药剂学系
学科主题药学
Enhanced brain distribution and pharmacodynamics of rivastigmine by liposomes following intranasal administration
Yang, Zhen-Zhen1,2; Zhang, Yan-Qing3; Wang, Zhan-Zhang1,2; Wu, Kai1,2; Lou, Jin-Ning4; Qi, Xian-Rong1,2
关键词Intranasal Administration Liposomes Cell Penetrating Peptide (Cpp) Biodistribution Pharmacodynamics Rivastigmine
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2013-08-16
DOI10.1016/j.ijpharm.2013.05.009
452期:1-2页:344-354
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]CELL-PENETRATING PEPTIDE ; ALZHEIMERS-DISEASE ; CHOLINESTERASE INHIBITOR ; INTRACELLULAR DELIVERY ; IN-VITRO ; RATS ; TRANSPORT ; DRUG ; ABSORPTION ; BARRIER
英文摘要

Alzheimer′s disease (AD) is a common progressive neurodegenerative disorder associated with cholinergic neurons degeneration. The blood-brain barrier (BBB) not only provides protection for the brain but also hinders the treatment and diagnosis of this neurological disease, because the drugs must cross BBB to reach the lesions. The present work was aimed at formulating rivastigmine liposomes (Lp) and cell-penetrating peptide (CPP) modified liposomes (CPP-Lp) to improve rivastigmine distribution in brain and proceed to enhance pharmacodynamics by intranasal (IN) administration and minimize side effects. The results revealed that Lp especially the CPP-Lp can enhance the permeability across the BBB by murine brain microvascular endothelial cells model in vitro. IN administration of rivastigmine solution and rivastigmine liposomes demonstrated the capacity to improve rivastigmine distribution and adequate retention in CNS regions especially in hippocampus and cortex, which were the regions most affected by AD, than that of IV administration. Importantly, the lagging but intense inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities were relative to the extended release, absorption and retention. In addition, there was very mild nasal toxicity of liposomal formulations. The data suggest that rivastigmine liposomes especially CPP-Lp improve the brain delivery and enhance pharmacodynamics which respect to BBB penetration and nasal olfactory pathway into brain after IN administration, and simultaneously decrease the hepatic first pass metabolism and gastrointestinal adverse effects. (C) 2013 Elsevier B. V. All rights reserved.

语种英语
WOS记录号WOS:000321496200041
Citation statistics
Cited Times:41[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/56331
Collection北京大学药学院_药剂学系
作者单位1.Peking Univ, Dept Pharmaceut, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
3.Tianjin Univ Commerce, Dept Pharmaceut Engn, Tianjin 300134, Peoples R China
4.China Japan Friendship Hosp, Inst Clin Med Sci, Beijing 100029, Peoples R China
Recommended Citation
GB/T 7714
Yang, Zhen-Zhen,Zhang, Yan-Qing,Wang, Zhan-Zhang,et al. Enhanced brain distribution and pharmacodynamics of rivastigmine by liposomes following intranasal administration[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2013,452(1-2):344-354.
APA Yang, Zhen-Zhen,Zhang, Yan-Qing,Wang, Zhan-Zhang,Wu, Kai,Lou, Jin-Ning,&Qi, Xian-Rong.(2013).Enhanced brain distribution and pharmacodynamics of rivastigmine by liposomes following intranasal administration.INTERNATIONAL JOURNAL OF PHARMACEUTICS,452(1-2),344-354.
MLA Yang, Zhen-Zhen,et al."Enhanced brain distribution and pharmacodynamics of rivastigmine by liposomes following intranasal administration".INTERNATIONAL JOURNAL OF PHARMACEUTICS 452.1-2(2013):344-354.
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