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A Novel Octreotide Modified Lipid Vesicle Improved the Anticancer Efficacy of Doxorubicin in Somatostatin Receptor 2 Positive Tumor Models
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
2010-07-01
DOI10.1021/mp1000235
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
WOS记录号WOS:000280448100025
项目编号2009CB930300 ; 2009ZX09310-001 ; 2007AA021811
资助机构National Basic Research Program of China ; State Key Projects ; 863 Project
引用统计
被引频次:63[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/65366
专题北京大学药学院
作者单位Peking Univ, Dept Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
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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.
APA Zhang, Junlin,Jin, Wu,Wang, Xueqing,Wang, Jiancheng,Zhang, Xuan,&Zhang, Qiang.(2010).A Novel Octreotide Modified Lipid Vesicle Improved the Anticancer Efficacy of Doxorubicin in Somatostatin Receptor 2 Positive Tumor Models.MOLECULAR PHARMACEUTICS,7(4),1159-1168.
MLA Zhang, Junlin,et al."A Novel Octreotide Modified Lipid Vesicle Improved the Anticancer Efficacy of Doxorubicin in Somatostatin Receptor 2 Positive Tumor Models".MOLECULAR PHARMACEUTICS 7.4(2010):1159-1168.
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