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Lanreotide-conjugated PEG-DSPE micelles: an efficient nanocarrier targeting to somatostatin receptor positive tumors
Zheng, Nan1; Dai, Wenbing2; Zhang, Hua2; Wang, Xueqing2; Wang, Jiancheng2; Zhang, Xuan2; Wang, Kun1; Li, Jian1; Zhang, Qiang2
关键词Antitumor Lanreotide Paclitaxel Peg-dspe Micelles Receptor-mediated Delivery Somatostatin Receptor 2
刊名JOURNAL OF DRUG TARGETING
2015
DOI10.3109/1061186X.2014.954118
23期:1页:67-78
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
资助者National Science Foundation ; Ministry of Science and Technology of China ; National Science Foundation ; Ministry of Science and Technology of China
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]POORLY SOLUBLE DRUGS ; LIQUID-CHROMATOGRAPHY ; CREMOPHOR EL ; MOUSE PLASMA ; IN-VITRO ; PACLITAXEL ; DELIVERY ; THERAPY ; CANCER ; PHARMACOKINETICS
英文摘要

Lanreotide is an octapeptide analog of endogenous somatostatin, specifically binding with tumors over-express somatostatin receptor 2 (SSTR2). In this study, we conjugated lanreotide to 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy (poly-(ethylene glycol))-2000] (PEG-DSPE), constructed active targeted micelles (lanreotide-PM), characterized their in vitro and in vivo targeting effect, and explored the receptor mediated transportion. The uptake of lanreotide-PM was found to be related to the expression level of SSTR2 in different cell lines and the competitive inhibition phenomenon indicated that the cellular uptake of lanreotide-PM was via a receptor meditated mechanism. In vivo, more lanreotide-PM accumulated in SSTR2 high expression tumor xenografts, endocytosed by the tumor cells, induced more apoptosis of tumor cells, and suppressed tumor growth efficiently. In conclusion, lanreotide-modified micelles containing antitumor drugs provide a promising strategy for the treatment of SSTR-expressing tumors.

语种英语
所属项目编号81130059 ; 2009CB930300
资助者National Science Foundation ; Ministry of Science and Technology of China ; National Science Foundation ; Ministry of Science and Technology of China
WOS记录号WOS:000346915600006
引用统计
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/50537
专题北京大学药学院
作者单位1.Peking Univ, Canc Hosp & Inst, Good Clin Practice Ctr, Key Lab Carcinogenesis & Translat Res,Minist Educ, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
Zheng, Nan,Dai, Wenbing,Zhang, Hua,et al. Lanreotide-conjugated PEG-DSPE micelles: an efficient nanocarrier targeting to somatostatin receptor positive tumors[J]. JOURNAL OF DRUG TARGETING,2015,23(1):67-78.
APA Zheng, Nan.,Dai, Wenbing.,Zhang, Hua.,Wang, Xueqing.,Wang, Jiancheng.,...&Zhang, Qiang.(2015).Lanreotide-conjugated PEG-DSPE micelles: an efficient nanocarrier targeting to somatostatin receptor positive tumors.JOURNAL OF DRUG TARGETING,23(1),67-78.
MLA Zheng, Nan,et al."Lanreotide-conjugated PEG-DSPE micelles: an efficient nanocarrier targeting to somatostatin receptor positive tumors".JOURNAL OF DRUG TARGETING 23.1(2015):67-78.
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