载吉非替尼的 DSPE-PEG2000 纳米胶束与 CD133 适体靶向肺癌干细胞。
Gefitinib-loaded DSPE-PEG2000 nanomicelles with CD133 aptamers target lung cancer stem cells.
机构信息
Department of Respiratory Medicine, Wuhan NO. 1 Hospital, 215 Zhongshan Street, Wuhan, 430022, China.
Laboratory Medicine, Third Hubei Provincial People's Hospital, Zhongshan Street, Wuhan, 430022, China.
出版信息
World J Surg Oncol. 2017 Aug 30;15(1):167. doi: 10.1186/s12957-017-1230-4.
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.
背景
肺癌干细胞（CSCs）被认为是肺癌的种子，CD133 是肺癌 CSCs 的标志物。在这里，我们开发了载有 CD133 适体的吉非替尼聚乙二醇 2000-二硬脂酰磷脂酰乙醇胺纳米胶束（M-Gef-CD133），以消除 CD133 肺癌 CSCs。
方法
M-Gef-CD133 是采用脂质膜法制备的。评估了 M-Gef-CD133 对肺癌 CSCs 的靶向性和活性。
结果
M-Gef-CD133 粒径较小（25nm），对 CD133 肺癌 CSCs 的细胞毒性作用明显高于非靶向 M-Gef 和吉非替尼。值得注意的是，M-Gef-CD133 可显著降低肿瘤球形成和 CD133 肺癌 CSCs 的比例，表明其对 CD133 肺癌 CSCs 具有选择性毒性。
结论
CD133 适体与 CD133 的相互作用有望将吉非替尼递送至 CD133 肺癌 CSCs，M-Gef-CD133 是一种有前途的针对肺癌 CSCs 的治疗方法。
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