Design, preparation and characterization of cyclic RGDfK peptide modified poly(ethylene glycol)-block-poly(lactic acid) micelle for targeted delivery

	Design, preparation and characterization of cyclic RGDfK peptide modified poly(ethylene glycol)-block-poly(lactic acid) micelle for targeted delivery
	Li, Caixia ; Wang, Wenlong ; Xi, Yuewei ; Wang, Jiexin ; Chen, Jian-Feng ; Yun, Jimmy ; Le, Yuan
刊名	MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
	2016-07-01
英文摘要	Molecular targeted cancer therapy is a promising strategy to overcome the lack of specificity of anticancer drug. While the binding of c(RGDfX) (cyclic Arginine-Glycine-Aspartic acid-Phenylalanine-Lysine) to alpha v beta(3) over expressed on tumor cell has been validated, the underlying interaction remains poorly understood. In this work, docking calculation was applied to investigate the interactions between c(RGDfX)/c(RGDfX)-PEG and alpha v beta(3). The calculated results indicated that c(RGDfK) interacted with alpha v beta(3) mainly by electrostatic interaction, stabilization interaction, and hydrophobic interaction. Conjugation of PEG chain to the c(RGDfX) weakened the binding affinity of c(RGDfK) to alpha v beta(3). Accordingly, docetaxel(DTX)-loaded target micelles (c(RGDfX)-PEG-PLA/PEG-PLA/DTX) were designed, characterized and evaluated using HeLa cells. In vitro release studies demonstrated both target and non-target micelles displayed almost the same profiles, which best fit in Ritger-Peppas model. Cellular uptake and MTT studies revealed that the target micelles with the presence of c(RGDfK) were more efficiently taken up by HeLa cells and significantly improved the cytotoxicity compared to that of non-target micelles. Cell inhibition rate of target micelles was improved by 20% after 24 h. Our findings suggest that target micelles may be a potential anticancer drug delivery system in the treatment of integrin alpha v beta(3) over-expressed on tumor cell. (C) 2016 Elsevier B.V. All rights reserved.
内容类型	期刊论文
源URL	[http://ir.nwipb.ac.cn/handle/363003/5758]
专题	西北高原生物研究所_中国科学院西北高原生物研究所
推荐引用方式 GB/T 7714	Li, Caixia,Wang, Wenlong,Xi, Yuewei,et al. Design, preparation and characterization of cyclic RGDfK peptide modified poly(ethylene glycol)-block-poly(lactic acid) micelle for targeted delivery[J]. MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS,2016.
APA	Li, Caixia.,Wang, Wenlong.,Xi, Yuewei.,Wang, Jiexin.,Chen, Jian-Feng.,...&Le, Yuan.(2016).Design, preparation and characterization of cyclic RGDfK peptide modified poly(ethylene glycol)-block-poly(lactic acid) micelle for targeted delivery.MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS.
MLA	Li, Caixia,et al."Design, preparation and characterization of cyclic RGDfK peptide modified poly(ethylene glycol)-block-poly(lactic acid) micelle for targeted delivery".MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS (2016).