AUTHOR=An Lin , Wang Jia-wei , Liu Jia-dong , Zhao Zi-ming , Song Yuan-jian 

TITLE=Design, Preparation, and Characterization of Novel Calix[4]arene Bioactive Carrier for Antitumor Drug Delivery

JOURNAL=Frontiers in Chemistry

VOLUME=7

YEAR=2019

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2019.00732

DOI=10.3389/fchem.2019.00732

ISSN=2296-2646

ABSTRACT=<p>An amphiphilic and bioactive calix[4]arene derivative <bold>8 (CA)</bold> is designed and successfully synthesized from <italic>tert</italic>-butyl calix[4] arene <bold>1</bold> by sequential inverse F-C alkylation, nitration, O-alkylation, esterification, aminolysis, reduction, and acylation reaction. The blank micelles of <bold>FA-CA</bold> and doxorubicin (DOX) loaded micelles <bold>FA-CA-DOX</bold> are prepared subsequently undergoing self-assembly and dialysis of <bold>CA</bold> and DSPE-PEG<sub>2000</sub>-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, <bold>FA-CA</bold> micelles reported in this work was a promising drug delivery vehicle for tumor targeting therapy.</p>