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学科主题: 药学
题名:
RGD-based strategies for improving antitumor activity of paclitaxel-loaded liposomes in nude mice xenografted with human ovarian cancer
作者: Zhao, Hui1,2; Wang, Jian-Cheng1; Sun, Qi-Shi2; Luo, Chun-Lei1; Zhang, Qiang1,3
关键词: RGD peptide ; targeting liposomes ; paclitaxel ; antitumor
刊名: JOURNAL OF DRUG TARGETING
发表日期: 2009
DOI: 10.1080/10611860802368966
卷: 17, 期:1, 页:10-18
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]: STERICALLY STABILIZED LIPOSOMES ; TAXOL-CONTAINING LIPOSOMES ; IN-VIVO ; INTRACELLULAR DELIVERY ; CELL-ADHESION ; DOXORUBICIN ; INTEGRINS ; EFFICACY ; FORMULATIONS ; THERAPY
英文摘要:

Tumor-targeting drug delivery systems are being the ideal carrier for systemic administration of antiproliferative drugs. RGD peptide (arginine-glycine-aspartic acid) modified liposomes containing paclitaxel (RGD-SSL-PTX). The arginine-glycineaspartic acid tripeptide (RGD) modified sterically stabilized liposomes (SSL) containing paclitaxel (PTX) (RGD-SSL-PTX), which could increase targeting to tumor by binding with the integrin receptors overexpressed on tumor cells. The encapsulation efficiency was more than 90% and the mean particle size was of 120nm with a narrow size distribution. It was indicated that significant cytotoxicity (3.5 times lower IC(50)) was found in the SKOV-3 human ovarian cancer cells treated with RGD-SSL-PTX preparation, as well as the intracellular uptake of liposomes (a 6.21-fold increase in fluorescence intensity), when compared to those of non-targeted liposomes (SSL). For in vivo antitumor activity, it was shown in the present study thatRGD-SSL-PTX preparation had the strongest tumor growth inhibition among the test formulations (P < 0.05) in BALB/c nude mice xenografted with SKOV-3 solid tumor. Meanwhile, there was no significant change in the body weight of the animals treated with RGD-SSL-PTX for intravenous injection at a dose of 12.5 mg/kg. It was suggested that the RGD-SSL-PTX preparation might have a great advantage over present-day chemotherapy with Taxol (R) in curing those tumors overexpressing integrin receptors.

语种: 英语
所属项目编号: 30430760 ; 30572261 ; 2007CB935801
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China (973 program)
WOS记录号: WOS:000261943900002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/57230
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, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100083, Peoples R China
2.Shenyang Pharmaceut Univ, Dept Tradit Chinese Med, Shenyang 110015, Peoples R China
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Zhao, Hui,Wang, Jian-Cheng,Sun, Qi-Shi,et al. RGD-based strategies for improving antitumor activity of paclitaxel-loaded liposomes in nude mice xenografted with human ovarian cancer[J]. JOURNAL OF DRUG TARGETING,2009,17(1):10-18.
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