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学科主题药学
Octreotide-Modified Polymeric Micelles as Potential Carriers for Targeted Docetaxel Delivery to Somatostatin Receptor Overexpressing Tumor Cells
Zhang, Yuan; Wang, Xueqing; Wang, Jiancheng; Zhang, Xuan; Zhang, Qiang
关键词antitumor efficacy DTX intracellular delivery octreotide polymeric micelles
刊名PHARMACEUTICAL RESEARCH
2011-05-01
DOI10.1007/s11095-011-0381-1
28期:5页:1167-1178
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
资助者Ministry of Science and Technology, PR China ; Ministry of Science and Technology, PR China
研究领域[WOS]Chemistry ; Pharmacology & Pharmacy
关键词[WOS]BLOCK-COPOLYMER MICELLES ; DRUG-DELIVERY ; BREAST-CANCER ; ANALOGS ; DIAGNOSIS ; RESONANCE ; PEPTIDES ; BINDING ; PROTEIN ; SYSTEM
英文摘要

Somatostatin analogue octreotide (OCT)-modified PEG-b-PLA micelles were constructed to bind to somatostatin receptors (SSTRs) overexpressed on tumor cells for enhanced intracellular drug delivery and improved therapeutic efficacy for malignant tumors.

Copolymers conjugated with octreotide (OCT-PEG(6000)-b-PLA(5000)) were synthesized. The fluorescent probe DiI or docetaxel (DTX)-loaded micelles with or without octreotide modification (OCT-PM-DiI, PM-DiI, OCT-PM-DTX and PM-DTX) were prepared, and their physiochemical properties, intracellular delivery in vitro or anti-tumor activity in vivo were evaluated, respectively.

The CMC of OCT-PEG(6000)-b-PLA(5000) was quite low (< 10(-6) mol/L). All micelles were less than 80 nm with spherical shape and high encapsulation efficiency. DTX molecules were well dispersed in the micelles without chemical interactions with the polymers. Flow cytometry and confocal microscopy results showed that OCT-PM-DiI enhanced intracellular delivery efficiency via receptor-mediated endocytosis in NCI-H446 cells; the optimal modification ratio of OCT on micelle surface was 5%. OCT-PM-DTX exhibited higher retardation of tumor growth after intravenous injections into xenograft NCI-H446 tumor model; octreotide-modified micelles did not show severe toxicity.

SSTRs targeting micelles may serve as promising nanocarriers in tumor treatment for hydrophobic anticancer drugs, such as DTX.

语种英语
所属项目编号2009CB930300 ; 2007AA021811 ; 2009ZX09310-001
资助者Ministry of Science and Technology, PR China ; Ministry of Science and Technology, PR China
WOS记录号WOS:000289302000021
Citation statistics
Cited Times:27[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/66978
Collection北京大学药学院
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
Recommended Citation
GB/T 7714
Zhang, Yuan,Wang, Xueqing,Wang, Jiancheng,et al. Octreotide-Modified Polymeric Micelles as Potential Carriers for Targeted Docetaxel Delivery to Somatostatin Receptor Overexpressing Tumor Cells[J]. PHARMACEUTICAL RESEARCH,2011,28(5):1167-1178.
APA Zhang, Yuan,Wang, Xueqing,Wang, Jiancheng,Zhang, Xuan,&Zhang, Qiang.(2011).Octreotide-Modified Polymeric Micelles as Potential Carriers for Targeted Docetaxel Delivery to Somatostatin Receptor Overexpressing Tumor Cells.PHARMACEUTICAL RESEARCH,28(5),1167-1178.
MLA Zhang, Yuan,et al."Octreotide-Modified Polymeric Micelles as Potential Carriers for Targeted Docetaxel Delivery to Somatostatin Receptor Overexpressing Tumor Cells".PHARMACEUTICAL RESEARCH 28.5(2011):1167-1178.
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