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学科主题: 药学
题名:
Peptide PHSCNK as an integrin alpha(5)beta(1) antagonist targets stealth liposomes to integrin-overexpressing melanoma
作者: Dai, Wenbing; Yang, Tingyuan; Wang, Yiguang; Wang, Xueqing; Wang, Jiancheng; Zhang, Xuan; Zhang, Qiang
关键词: Targeted delivery system ; Liposomes ; Doxorubicin ; PHSCNK ; Integrins
刊名: NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
发表日期: 2012-10-01
DOI: 10.1016/j.nano.2012.01.003
卷: 8, 期:7, 页:1152-1161
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Nanoscience & Nanotechnology ; Medicine, Research & Experimental
研究领域[WOS]: Science & Technology - Other Topics ; Research & Experimental Medicine
关键词[WOS]: STERICALLY STABILIZED LIPOSOMES ; IMPROVED ANTITUMOR EFFICACY ; LOADED LIPOSOMES ; IN-VIVO ; INTRACELLULAR DELIVERY ; TUMOR NEOVASCULATURE ; BREAST-CANCER ; RGD PEPTIDE ; DOXORUBICIN ; CELLS
英文摘要:

As an integrin alpha(5)beta(1) antagonist, N-acetyl-proline-histidine-serine-cysteine-asparagine-amide (Ac-PHSCN-NH2) is currently in phase II trials for various cancer therapies. In this study Ac-PHSCNK-NH2 (PHSCNK) was used as a novel homing peptide to prepare ligand-targeted liposomes loaded with doxorubicin (PHSCNK-PL-DOX), with the hypothesis that the therapy target of integrin alpha(5)beta(1) may also serve as a delivery target. The stealth liposomes loaded with doxorubicin (PL-DOX) were used as the control. PHSCNK-PL-DOX demonstrated an enhanced intracellular uptake and a greater cytotoxicity against melanoma B16F10 cells in comparison with PL-DOX. The novel targeted formulation displayed stronger tumor inhibition and prolonged survival time in comparison with controls in C57BL/6mice bearing B16F10 tumors, and it exhibited less heart toxicity in hematoxylin-eosin (H&E) staining of tissues. Taking the pharmacokinetics and biodistribution results into account, the authors conclude that alpha(5)beta(1) integrin-mediated liposomes might be used as a potential delivery system for targeted tumor therapy.

From the Clinical Editor: Lactosyl-norcantharidin TMC nanoparticles were found superior in comparison with Lac-NCTD and Lac-NCTD chitosan nanoparticles from the standpoint of antitumor activity on murine hepatocarcinoma 22 subcutaneous model. (C) 2012 Elsevier Inc. All rights reserved.

语种: 英语
所属项目编号: 2009CB930300 ; 2009zx09310-001
项目资助者: National Basic Research Program of China ; National Key program of New Drug innovation
WOS记录号: WOS:000309216300013
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65495
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
Dai, Wenbing,Yang, Tingyuan,Wang, Yiguang,et al. Peptide PHSCNK as an integrin alpha(5)beta(1) antagonist targets stealth liposomes to integrin-overexpressing melanoma[J]. NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE,2012,8(7):1152-1161.
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