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学科主题: 药学
题名:
Enhanced brain distribution and pharmacodynamics of rivastigmine by liposomes following intranasal administration
作者: 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
发表日期: 2013-08-16
DOI: 10.1016/j.ijpharm.2013.05.009
卷: 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
所属项目编号: 2013CB932501 ; 2009CB930303 ; 30970785 ; 81273454 ; 7132113 ; 20100001110056 ; BMU20110263
项目资助者: National Basic Research Program ; NSFC ; Beijing NSF ; Doctoral Foundation of the Ministry of Education ; Innovation Team of Ministry of Education
WOS记录号: WOS:000321496200041
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56331
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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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:
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.
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