A dual-targeting nanocarrier based on poly(amidoamine) dendrimers   conjugated with transferrin and tamoxifen for treating brain gliomas

doi:10.1016/j.biomaterials.2012.02.004

CORC > 北京大学 > 化学与分子工程学院

	A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas
	Li, Yan ; He, Hai ; Jia, Xinru ; Lu, Wan-Liang ; Lou, Jinning ; Wei, Yen
刊名	biomaterials
	2012
关键词	Blood-brain barrier (BBB) PAMAM Dual-targeting PH-sensitive Gliomas DRUG-DELIVERY BIOLOGICAL APPLICATIONS MULTIDRUG-RESISTANCE IN-VITRO CANCER DOXORUBICIN LIPOSOMES RECEPTOR TUMORS NANOPARTICLES
DOI	10.1016/j.biomaterials.2012.02.004
英文摘要	A pH-sensitive dual-targeting drug carrier (G4-DOX-PEG-Tf-TAM) was synthesized with transferrin (TO conjugated on the exterior and Tamoxifen (TAM) in the interior of the fourth generation PAMAM dendrimers for enhancing the blood-brain barrier (BBB) transportation and improving the drug accumulation in the glioma cells. It was found that, on average, 7 doxorubicine (DOX) molecules, over 30 PEG(1000) and PEG(2000) chains and one Tf group were bonded on the periphery of each G4 PAMAM dendrimer, while 29 TAM molecules were encapsulated into the interior of per dendrimer. The pH-triggered DOX release was 32% at pH 4.5 and 6% at pH 7.4, indicating a comparatively fast drug release at weak acidic condition and stable state of the carrier at physiological environment. The in vitro assay of the drug transport across the BBB model showed that G4-DOX-PEG-Tf-TAM exhibited higher BBB transportation ability with the transporting ratio of 6.06% in 3 h. The carrier was internalized into C6 glioma cells upon crossing the BBB model by the coactions of TfR-mediated endocytosis and the inhibition effect of TAM to the drug efflux transports. Moreover, it also displayed the in vitro accumulation of DOX in the avascular C6 glioma spheroids made the tumor volume effectively reduced. (C) 2012 Elsevier Ltd. All rights reserved.; Engineering, Biomedical; Materials Science, Biomaterials; SCI(E); EI; PubMed; 67; ARTICLE; 15; 3899-3908; 33
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/149916]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	Li, Yan,He, Hai,Jia, Xinru,et al. A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas[J]. biomaterials,2012.
APA	Li, Yan,He, Hai,Jia, Xinru,Lu, Wan-Liang,Lou, Jinning,&Wei, Yen.(2012).A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas.biomaterials.
MLA	Li, Yan,et al."A dual-targeting nanocarrier based on poly(amidoamine) dendrimers conjugated with transferrin and tamoxifen for treating brain gliomas".biomaterials (2012).