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

  • World J Surg Oncol. 2017 Aug 30;15(1):167. doi: 10.1186/s12957-017-1230-4.
Xiaolong Huang  1 ,  Jingsong Huang  2 ,  Dewen Leng  3 ,  Shuo Yang  4 ,  Qi Yao  5 ,  Jin Sun  6 ,  Jun Hu  7
Affiliations
  • 1. Department of Respiratory Medicine, Wuhan NO. 1 Hospital, 215 Zhongshan Street, Wuhan, 430022, China. [email protected].
  • 2. Laboratory Medicine, Third Hubei Provincial People's Hospital, Zhongshan Street, Wuhan, 430022, China.
  • 3. Department of Critical Care Medicine, Wuhan NO. 1 Hospital, 215 Zhongshan Street, Wuhan, 430022, China.
  • 4. Department of Respiratory Medicine, Wuhan NO. 1 Hospital, 215 Zhongshan Street, Wuhan, 430022, China.
  • 5. Department of Otolaryngology, Wuhan NO. 1 Hospital, 215 Zhongshan Street, Wuhan, 430022, China.
  • 6. Department of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai, 200433, China.
  • 7. Department of Physical examination, Wuhan Hospital for Occupational Disease Prevention and Treatment, 18-20 Jianghanbei Road, Wuhan, 430016, China.
PMID: 28854941 DOI: 10.1186/s12957-017-1230-4
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.

Keywords
CD133; Cancer stem cells; Gefitinib; Lung cancer; Nanomicelles.
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