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Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature
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
2011
DOI10.3109/10611861003663531
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
WOS记录号WOS:000285054900003
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:13[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/400002259/68157
专题北京大学药学院
北京大学医学部管理机构_医学部
北京大学药学院_药剂学系
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
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GB/T 7714
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.
APA Yin, Jie,Li, Zaiquan,Yang, Tingyuan,Wang, Jiancheng,Zhang, Xuan,&Zhang, Qiang.(2011).Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature.JOURNAL OF DRUG TARGETING,19(1),25-36.
MLA Yin, Jie,et al."Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature".JOURNAL OF DRUG TARGETING 19.1(2011):25-36.
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