An amphiphilic and bioactive calix[4]arene derivative is designed and successfully synthesized from -butyl calix[4] arene by sequential inverse F-C alkylation, nitration, O-alkylation, esterification, aminolysis, reduction, and acylation reaction. The blank micelles of and doxorubicin (DOX) loaded micelles are prepared subsequently undergoing self-assembly and dialysis of and DSPE-PEG-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, micelles reported in this work was a promising drug delivery vehicle for tumor targeting therapy.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6855266 | PMC |
| http://dx.doi.org/10.3389/fchem.2019.00732 | DOI Listing |
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