%A An,Lin %A Wang,Jia-wei %A Liu,Jia-dong %A Zhao,Zi-ming %A Song,Yuan-jian %D 2019 %J Frontiers in Chemistry %C %F %G English %K amphiphilic calixarene, bioactive carrier, drug delivery, self-assembly, doxorubicin,amphiphilic calixarene,Bioactive carrier,Drug delivery,self-assembly,Doxorubicin %Q %R 10.3389/fchem.2019.00732 %W %L %M %P %7 %8 2019-November-07 %9 Original Research %# %! Anticancer Effect of Calixarene Micelles %* %< %T Design, Preparation, and Characterization of Novel Calix[4]arene Bioactive Carrier for Antitumor Drug Delivery %U https://www.frontiersin.org/articles/10.3389/fchem.2019.00732 %V 7 %0 JOURNAL ARTICLE %@ 2296-2646 %X An amphiphilic and bioactive calix[4]arene derivative 8 (CA) is designed and successfully synthesized from tert-butyl calix[4] arene 1 by sequential inverse F-C alkylation, nitration, O-alkylation, esterification, aminolysis, reduction, and acylation reaction. The blank micelles of FA-CA and doxorubicin (DOX) loaded micelles FA-CA-DOX are prepared subsequently undergoing self-assembly and dialysis of CA and DSPE-PEG2000-FA. The drug release kinetics curve of the encapsulated-DOX micelle demonstrates a rapid release under mild conditions, indicating the good pH-responsive ability. Furthermore, the cytotoxicity of DOX-loaded micelle respect to the blank micelle against seven different human carcinoma (A549, HeLa, HepG2, HCT116, MCF-7, MDA-MB231, and SW480) cells has been also investigated. The results confirm the more significant inhibitory effect of DOX-loaded micelle than those of DOX and the blank micelles. The CDI calculations show a synergistic effect between blank micelles and DOX in inducing tumor cell death. In conclusion, FA-CA micelles reported in this work was a promising drug delivery vehicle for tumor targeting therapy.