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学科主题: 药学
题名:
The antitumor activity of a doxorubicin loaded, iRGD-modified sterically-stabilized liposome on B16-F10 melanoma cells: in vitro and in vivo evaluation
作者: Yu, Ke-Fu1; Zhang, Wei-Qiang1; Luo, Li-Min1; Song, Ping1; Li, Dan1; Du, Ruo1; Ren, Wei1; Huang, Dan1; Lu, Wan-Liang1,2; Zhang, Xuan1; Zhang, Qiang1,2
关键词: tumor-targeting and tumor-penetrating ; integrin receptor ; NRP-1 ; iRGD ; liposome ; doxorubicin
刊名: INTERNATIONAL JOURNAL OF NANOMEDICINE
发表日期: 2013
DOI: 10.2147/IJN.S46962
卷: 8, 页:2473-2485
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Nanoscience & Nanotechnology ; Pharmacology & Pharmacy
研究领域[WOS]: Science & Technology - Other Topics ; Pharmacology & Pharmacy
关键词[WOS]: DRUG-DELIVERY ; TARGETED NANOPARTICLES ; COMBINATION THERAPY ; POLYMERIC MICELLES ; TUMOR-CELLS ; PACLITAXEL ; CANCER ; NEUROPILINS ; INTEGRINS
英文摘要:

Considering the fact that iRGD (tumor-homing peptide) demonstrates tumor-targeting and tumor-penetrating activity, and that B16-F10 (murine melanoma) cells overexpress both alpha v integrin receptor and neuropilin-1 (NRP-1), the purpose of this study was to prepare a novel doxorubicin (DOX)-loaded, iRGD-modified, sterically-stabilized liposome (SSL) (iRGD-SSL-DOX) in order to evaluate its antitumor activity on B16-F10 melanoma cells in vitro and in vivo. The iRGD-SSL-DOX was prepared using a thin-film hydration method. The characteristics of iRGD-SSL-DOX were evaluated. The in vitro leakage of DOX from iRGD-SSL-DOX was tested. The in vitro tumor-targeting and tumor-penetrating characteristics of iRGD-modified liposomes on B16-F10 cells were investigated. The in vivo tumor-targeting and tumor-penetrating activities of iRGD-modified liposomes were performed in B16-F10 tumor-bearing nude mice. The antitumor effect of iRGD-SSL-DOX was evaluated in B16-F10 tumor-bearing C57BL/6 mice in vivo. The average particle size of the iRGD-SSL-DOX was found to be 91 nm with a polydispersity index (PDI) of 0.16. The entrapment efficiency of iRGD-SSL-DOX was 98.36%. The leakage of DOX from iRGD-SSL-DOX at the 24-hour time point was only 7.5%. The results obtained from the in vitro flow cytometry and confocal microscopy, as well as in vivo biodistribution and confocal immunofluorescence microscopy experiments, indicate that the tumor-targeting and tumor-penetrating activity of the iRGD-modified SSL was higher than that of unmodified SSL. In vivo antitumor activity results showed that the antitumor effect of iRGD-SSL-DOX against melanoma tumors was higher than that of SSL-DOX in B16-F10 tumor-bearing mice. In conclusion, the iRGD-SSL-DOX is a tumor-targeting and tumor-penetrating peptide modified liposome which has significant antitumor activity against melanoma tumors.

语种: 英语
所属项目编号: 81172992 ; 2009CB930300 ; 2013CB932501 ; BMU20110263
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China (973 Program) ; Ministry of Education of China
WOS记录号: WOS:000321711300001
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64617
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 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
Yu, Ke-Fu,Zhang, Wei-Qiang,Luo, Li-Min,et al. The antitumor activity of a doxorubicin loaded, iRGD-modified sterically-stabilized liposome on B16-F10 melanoma cells: in vitro and in vivo evaluation[J]. INTERNATIONAL JOURNAL OF NANOMEDICINE,2013,8:2473-2485.
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