Cyclodextrin-based gefitinib nanobubbles for synergistic apoptosis in lung cancer

Abstract

The present research work aimed to develop and characterize nanobubbles (NBs) for synergistic action in human cell line A549 using gefitinib and oxygen. NBs were prepared by loading oxygen in β-cyclodextrin-based inclusion complex (IC), whereas in nanosponges by polymer condensation method. Initially, the amino-functionalization was performed using (3-aminopropyl) triethoxysilane and then, underwent PEGylation to achieve site-specific action. The loading capacities of PEGylated and non-PEGylated NBs of gefitinib were found to be 85.11 ± 2.31% and 86.14±1.24%, respectively, whereas oxygen levels were found to be 2.8mg/L and 6.9mg/L, respectively. The synergistic effect of gefitinib NBs was observed by flow cytometry due to apoptosis of cell line A549 (with apoptotic rate ranged from 35.2±2.15% to 73.6±1.57%) by inhibiting EGFR pathway and further confirmed using western blotting technique. Dual delivery of gefitinib and oxygen from β-cyclodextrin-based nanosponges showed that NBs act as a novel therapy in the treatment of non-small cell lung cancer.

Graphical Abstract

KEYWORDS:

• Β-cyclodextrin
• oxygen
• cancer
• gefitinib
• nanosponges

Disclosure statement

No potential conflict of interest was reported by the author(s).