Poly(epsilon-caprolactone)-Block-poly(ethyl Ethylene Phosphate) Micelles for Brain-Targeting Drug Delivery: In Vitro and In Vivo Valuation

doi:10.1007/s11095-010-0265-9

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第二研究室

	Poly(epsilon-caprolactone)-Block-poly(ethyl Ethylene Phosphate) Micelles for Brain-Targeting Drug Delivery: In Vitro and In Vivo Valuation
	Zhang, Pengcheng1 ; Hu, Luojuan 2; Wang, Yucai 3; Wang, Jun 3; Feng, Linyin2 ; Li, Yaping1
刊名	PHARMACEUTICAL RESEARCH
	2010-12
卷号	27 期号:12 页码:2657-2669
关键词	biodistribution blood-brain barrier (BBB) micelle polyphosphoester
ISSN号	0724-8741
DOI	10.1007/s11095-010-0265-9
文献子类	Article
英文摘要	The purpose of this work was to investigate the potential of poly(epsilon-caprolactone)-block-poly(ethyl ethylene phosphate) (PCL-PEEP) micelles for brain-targeting drug delivery. The coumarin-6-loaded PCL-PEEP micelles (CMs) were prepared and characterized. The cellular uptake of CMs was evaluated on in vitro model of brain-blood barrier (BBB), and the brain biodistribution of CMs in ICR mice was investigated. PCL-PEEP could self-assemble into 20 nm micelles in water with the critical micelle concentration (CMC) 0.51 mu g/ml and high coumarin-6 encapsulation efficiency (92.5 +/- 0.7%), and the micelles were stable in 10% FBS with less than 25% leakage of incorporated coumarin-6 during 24 h incubation at 37A degrees C. The cellular uptake of CMs by BBB model was significantly higher and more efficient than coumarin-6 solution (CS) at 50 ng/ml. Compared with CS, 2.6-fold of coumarin-6 was found in the brains of CM-treated mice, and C-max of CMs was 4.74% of injected dose/g brain. The qualitative investigation on the brain distribution of CMs indicated that CMs were prone to accumulate in hippocampus and striatum. These results suggest that PCL-PEEP micelles could be a promising brain-targeting drug delivery system with low toxicity.
资助项目	National Basic Research Program of China[2007CB935804] ; National Basic Research Program of China[2009CB930304] ; National Natural Science Foundation of China[90713035] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09501-024] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09103-066] ; Shanghai Science and Technology Committee[08DZ1980200]
WOS关键词	80-COATED POLYBUTYLCYANOACRYLATE NANOPARTICLES ; MICROVESSEL ENDOTHELIAL-CELLS ; PARTICLE-SIZE ; CYANOACRYLATE) NANOPARTICLES ; MONOLAYER PERMEABILITY ; GOLD NANOPARTICLES ; BARRIER PROPERTIES ; BLOCK-COPOLYMER ; GROWTH-FACTOR ; TRANSPORT
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	SPRINGER/PLENUM PUBLISHERS
WOS记录号	WOS:000284324200013
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278710]
专题	药理学第二研究室中科院受体结构与功能重点实验室新药研究国家重点实验室药物制剂研究中心
通讯作者	Li, Yaping
作者单位	1.Chinese Acad Sci, Ctr Pharmaceut, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Univ Sci & Technol China, Hefei 230026, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Pengcheng,Hu, Luojuan,Wang, Yucai,et al. Poly(epsilon-caprolactone)-Block-poly(ethyl Ethylene Phosphate) Micelles for Brain-Targeting Drug Delivery: In Vitro and In Vivo Valuation[J]. PHARMACEUTICAL RESEARCH,2010,27(12):2657-2669.
APA	Zhang, Pengcheng,Hu, Luojuan,Wang, Yucai,Wang, Jun,Feng, Linyin,&Li, Yaping.(2010).Poly(epsilon-caprolactone)-Block-poly(ethyl Ethylene Phosphate) Micelles for Brain-Targeting Drug Delivery: In Vitro and In Vivo Valuation.PHARMACEUTICAL RESEARCH,27(12),2657-2669.
MLA	Zhang, Pengcheng,et al."Poly(epsilon-caprolactone)-Block-poly(ethyl Ethylene Phosphate) Micelles for Brain-Targeting Drug Delivery: In Vitro and In Vivo Valuation".PHARMACEUTICAL RESEARCH 27.12(2010):2657-2669.