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学科主题: 药学
题名:
Octreotide-Modified Polymeric Micelles as Potential Carriers for Targeted Docetaxel Delivery to Somatostatin Receptor Overexpressing Tumor Cells
作者: 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
发表日期: 2011-05-01
DOI: 10.1007/s11095-011-0381-1
卷: 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
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
项目资助者: Ministry of Science and Technology, PR China
WOS记录号: WOS:000289302000021
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/66978
Appears in Collections:北京大学药学院_期刊论文

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

Recommended Citation:
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.
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