Gefitinib-loaded DSPE-PEG2000 nanomicelles with CD133 aptamers target lung cancer stem cells.

BACKGROUND: Lung cancer stem cells (CSCs) are considered to be the seed of lung cancer, and CD133 is a marker of lung CSCs. Here, we developed gefitinib-loaded poly(ethylene glycol) 2000-distearoylphosphatidylethanolamine nanomicelles with CD133 aptamers (M-Gef-CD133) to eliminate CD133(+) lung CSCs. METHODS: M-Gef-CD133 was prepared using a lipid-film-based approach. The targeting and activity of M-Gef-CD133 towards lung CSCs were evaluated. RESULTS: M-Gef-CD133 were small (25 nm) and showed enhanced cytotoxic effect towards CD133(+) lung CSCs compared with non-targeted M-Gef and gefitinib. Notably, M-Gef-CD133 could significantly reduce tumor sphere formation and the percentage of CD133(+) lung CSCs, indicating that it possesses selective toxicity against CD133(+) lung CSCs. CONCLUSIONS: The interaction of CD133 aptamers and CD133 shows promise in the delivery of gefitinib to CD133(+) lung CSCs, and M-Gef-CD133 represents a promising treatment to target lung CSCs.