Gefitinib-loaded DSPE-PEG2000 nanomicelles with CD133 aptamers target lung cancer stem cells
Xiaolong Huang1, Jingsong Huang2, Dewen Leng3
1Department of Respiratory Medicine, Wuhan NO. 1 Hospital, 215 Zhongshan Street, Wuhan, 430022, China. motolongqd@126.com.
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.
Insights
This study developed targeted nanomicelles loaded with gefitinib to eliminate lung cancer stem cells (CSCs) expressing CD133. The novel M-Gef-CD133 treatment selectively targets and reduces CD133-positive lung CSCs, offering a promising therapeutic strategy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Lung cancer stem cells (CSCs) drive tumor growth, with CD133 identified as a key marker.
- Targeting CD133+ lung CSCs is a critical strategy for effective lung cancer treatment.
Purpose of the Study:
- To develop and evaluate gefitinib-loaded nanomicelles functionalized with CD133 aptamers (M-Gef-CD133) for targeted elimination of CD133+ lung CSCs.
Main Methods:
- Nanomicelles (M-Gef-CD133) were synthesized using a lipid-film-based approach.
- The targeting capability and cytotoxic effects of M-Gef-CD133 on lung CSCs were assessed.
Main Results:
- M-Gef-CD133 nanoparticles (25 nm) demonstrated enhanced cytotoxicity against CD133+ lung CSCs compared to non-targeted gefitinib formulations.
- Significant reduction in tumor sphere formation and CD133+ lung CSC populations was observed, confirming selective toxicity.
Conclusions:
- CD133 aptamer-mediated delivery of gefitinib to CD133+ lung CSCs shows therapeutic potential.
- M-Gef-CD133 nanomicelles represent a promising targeted therapy for lung CSCs, addressing a key challenge in lung cancer treatment.
