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

doi:10.1016/j.msec.2016.03.062

NWIPB OpenIR

	Design, preparation and characterization of cyclic RGDfK peptide modified poly(ethylene glycol)-block-poly(lactic acid) micelle for targeted delivery
	Li, Caixia 1,2; Wang, Wenlong 1; Xi, Yuewei 1; Wang, Jiexin 1; Chen, Jian-Feng 1; Yun, Jimmy 3; Le, Yuan 1
	2016-07-01
发表期刊	MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
卷号	64 页码:303-309
文章类型	Article
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.
关键词	Target Drug Delivery Rgdfk Peptide Nano-micelle Docking Calculations
WOS标题词	Science & Technology ; Technology
DOI	10.1016/j.msec.2016.03.062
关键词[WOS]	INTEGRIN ALPHA(V)BETA(3) ; EXTRACELLULAR SEGMENT ; TUMOR ANGIOGENESIS ; CRYSTAL-STRUCTURE ; ALPHA-V-BETA-3 ; RELEASE ; ANTAGONISTS ; DOCKING ; COMPLEX ; CELLS
收录类别	SCI
语种	英语
项目资助者	National Basic Research Program(2015CB932100) ; Program for New Century Excellent Talents University of China(NCET-12-0760) ; National "863" Program of China(2013AA032201)
WOS研究方向	Materials Science
WOS类目	Materials Science, Biomaterials
WOS记录号	WOS:000376547700036
引用统计	被引频次：24[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://210.75.249.4/handle/363003/5758
专题	中国科学院西北高原生物研究所
作者单位	1.Beijing Univ Chem Technol, State Key Lab Organ Inorgan Composites, Beijing 100029, Peoples R China 2.Chinese Acad Sci, Northwest Inst Plateau Biol, Key Lab Tibetan Med Res, Xining 810001, Qinghai, Peoples R China 3.Univ New S Wales, Sch Chem Sci & Engn, Sydney, NSW 2052, Australia
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,2016,64:303-309.
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,64,303-309.
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 64(2016):303-309.