Knowledge Management System of Northwest Institute of Plateau Biology, CAS
Design, preparation and characterization of cyclic RGDfK peptide modified poly(ethylene glycol)-block-poly(lactic acid) micelle for targeted delivery | |
Li, Caixia1,2; Wang, Wenlong1; Xi, Yuewei1; Wang, Jiexin1; Chen, Jian-Feng1; Yun, Jimmy3; Le, Yuan1 | |
2016-07-01 | |
发表期刊 | MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
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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 | |
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. |
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