Abstract
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.
Highlights
Malignant tumors are one of the most severe diseases currently threatening human health
In an effort to resolve the limitation of DOX clinically and in continuation of our previous work, we report on a novel DOX delivery system based on bioactive amphlic calix[4]arene polymer micelles (Figure 1)
According to the previous research results of our group (An et al, 2016), amphiphilic calixarene 8 was synthesized by a series of derivatizations using p-tert-butylphenol as raw material
Summary
Malignant tumors are one of the most severe diseases currently threatening human health. During administration, severe toxic side effects on healthy tissues lead to various complications (Livshits et al, 2014; Makin, 2014). Chemotherapy is subject to problems such as poor solubility, poor long-circulation, low bioavailability and lackness of specificity (Corot et al, 2006; Guo et al, 2013; Qi et al, 2013; Shah et al, 2014), which have limited its clinical applications. A large number of clinical trial results have successful approved that the ideal drug carriers can comprehensively overcome various biological obstacles during system administration and achieve optimal anti-tumor effect (Whitehead et al, 2009; Gomes-da-Silva et al, 2012; Zhang et al, 2012): (a) Blood barrier: the drug carrier need to maintain a long cycle time in the blood circulation; (b) Tumor targeting: specific
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