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学科主题: 药学
题名:
Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature
作者: Yin, Jie1; Li, Zaiquan2; Yang, Tingyuan1; Wang, Jiancheng1; Zhang, Xuan1; Zhang, Qiang1
关键词: Cyclic RGDyK ; polymeric micelles ; intracellular delivery ; integrin ; tumor targeting ; neovasculature
刊名: JOURNAL OF DRUG TARGETING
发表日期: 2011
DOI: 10.3109/10611861003663531
卷: 19, 期:1, 页:25-36
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: BLOCK-COPOLYMER MICELLES ; IN-VIVO EVALUATION ; PHASE-I ; ENCAPSULATED DOXORUBICIN ; ANTITUMOR EFFICACY ; ENDOTHELIAL-CELLS ; TARGETED DELIVERY ; ANTICANCER DRUGS ; SOLID TUMORS ; PACLITAXEL
英文摘要:

On the basis of the fact of the overexpression of integrins in malignant tumor cells and neovasculature, and the advantage of polymeric micelles (PM) as the drug carriers, a cyclic RGD peptide (cRGDyK) was anchored on the surface of polyethylene glycol-b-poly(lactic-co-glycolic acid) (PEG-b-PLGA) micelles as a ligand of integrins in order to enhance the intracellular delivery of encapsulated hydrophobic drug into the tumor cells and its neovasculature. Toward this goal, PEG-b-PLGA micelles without or with cRGDyK conjugation loaded with paclitaxel (PTX) or DiI were prepared and characterized. The results revealed that drug-loaded micelles were stable in solution, with small diameters (<80 nm) and a low critical micelle concentration. Spectrophotofluorometry, confocal microscopy, and flow cytometry showed that cRGDyK-conjugated micelles (TPM) facilitated the cell-specific uptake of DiI into the murine melanoma B16-F10 cells and human umbilical vein endothelial cells (HUVEC) via integrin-mediated endocytosis compared with cRGDyK-free micelles (NPM), and the uptake was proportional to the ratio of cRGDyK modification in certain range. Meanwhile, PTX-loaded TPM displayed higher cytotoxicity and antiproliferation activities against both cells than PTX-loaded NPM. These results suggest that cRGDyK-coupled PEG-b-PLGA micelles may be the promising intracellular targeting carriers for efficient delivery of chemotherapeutic agents into tumor cells and neovasculature.

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:000285054900003
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/68157
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Dept Biochem & Mol Biol, Sch Basic Med Sci, Beijing 100191, Peoples R China

Recommended Citation:
Yin, Jie,Li, Zaiquan,Yang, Tingyuan,et al. Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature[J]. JOURNAL OF DRUG TARGETING,2011,19(1):25-36.
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