胶束
赫拉
乙二醇
化学
PEG比率
MTT法
肽
天冬氨酸
体外
细胞毒性
立体化学
生物化学
生物物理学
氨基酸
有机化学
水溶液
生物
经济
财务
作者
Caixia Li,Wenlong Wang,Yang Xi,Jie‐Xin Wang,Jianfeng Chen,Jimmy Yun,Yuan Le
标识
DOI:10.1016/j.msec.2016.03.062
摘要
Molecular targeted cancer therapy is a promising strategy to overcome the lack of specificity of anticancer drug. While the binding of c(RGDfK) (cyclic Arginine-Glycine-Aspartic acid-Phenylalanine-Lysine) to αvβ3 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(RGDfK)/c(RGDfK)-PEG and αvβ3. The calculated results indicated that c(RGDfK) interacted with αvβ3 mainly by electrostatic interaction, stabilization interaction, and hydrophobic interaction. Conjugation of PEG chain to the c(RGDfK) weakened the binding affinity of c(RGDfK) to αvβ3. Accordingly, docetaxel(DTX)-loaded target micelles (c(RGDfK)-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 αvβ3 over-expressed on tumor cell.
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