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学科主题: 药学
题名:
A Novel Octreotide Modified Lipid Vesicle Improved the Anticancer Efficacy of Doxorubicin in Somatostatin Receptor 2 Positive Tumor Models
作者: Zhang, Junlin; Jin, Wu; Wang, Xueqing; Wang, Jiancheng; Zhang, Xuan; Zhang, Qiang
关键词: Octreotide ; somatostatin receptors ; sterically stabilized liposomes ; doxorubicin ; antitumor effect
刊名: MOLECULAR PHARMACEUTICS
发表日期: 2010-07-01
DOI: 10.1021/mp1000235
卷: 7, 期:4, 页:1159-1168
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Medicine, Research & Experimental ; Pharmacology & Pharmacy
研究领域[WOS]: Research & Experimental Medicine ; Pharmacology & Pharmacy
关键词[WOS]: PEGYLATED LIPOSOMAL DOXORUBICIN ; LUNG-CANCER CELLS ; IN-VIVO ; CONVENTIONAL DOXORUBICIN ; CYTOTOXIC ANALOGS ; BEARING MICE ; DELIVERY ; PEPTIDE ; BREAST ; PHARMACOKINETICS
英文摘要:

Octreotide (Oct) is a potential ligand due to its high affinity to somatostatin receptors (SSTRs), especially subtype 2 (SSTR2), as many tumor cells specifically overexpress SSTR2. In this study, we conjugated Oct to the PEG end of DSPE-PEG and prepared a novel doxorubicin (DOX)-loaded and Oct-modified sterically stabilized liposomes (Oct-SSL-DOX), in order to facilitate intracellular delivery of chemotherapeutic agent to the related tumor cells through active targeting and finally improve its antitumor activity. Three cells were proved to be different in expression level of SSTR2 and were used as model or control. It was demonstrated by fluorescence spectrophotometry, confocal laser scanning microscopy and flow cytometry that active sterically stabilized liposomes (SSL) increased intracellular delivery of DOX in SSTR2-positive cells, through a mechanism of receptor-mediated endocytosis. Compared to SSL, Oct modification on SSL exhibited little effect on the physicochemical properties of SSL. However, it reduced the circulation time of loaded-DOX to some extent in rats, increased cytotoxicity in SSTR2-positive tumor cells, enhanced drug accumulation in tumor tissue and improved anticancer efficacy in SSTR2-overexpressing tumor model. The correlation was found among intracellular uptake, cytotoxicity, drug distribution in tumor and pharmacodynamics of Oct-SSL-DOX, but not the pharmacokinetics based on plasma drug concentration. In summary, octreotide-modified SSL might be a promising system for the treatment of SSTR2-overexpressing cancers.

语种: 英语
所属项目编号: 2009CB930300 ; 2009ZX09310-001 ; 2007AA021811
项目资助者: National Basic Research Program of China ; State Key Projects ; 863 Project
WOS记录号: WOS:000280448100025
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65366
Appears in Collections:北京大学药学院_期刊论文

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

Recommended Citation:
Zhang, Junlin,Jin, Wu,Wang, Xueqing,et al. A Novel Octreotide Modified Lipid Vesicle Improved the Anticancer Efficacy of Doxorubicin in Somatostatin Receptor 2 Positive Tumor Models[J]. MOLECULAR PHARMACEUTICS,2010,7(4):1159-1168.
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