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

Abstract

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.

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