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Zileuton™ loaded in polymer micelles effectively reduce breast cancer circulating tumor cells and intratumoral cancer stem cells.
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 4.2 ) Pub Date : 2019-10-27 , DOI: 10.1016/j.nano.2019.102106
Petra Gener 1 , Sara Montero 2 , Helena Xandri-Monje 1 , Zamira V Díaz-Riascos 3 , Diana Rafael 2 , Fernanda Andrade 4 , Francesc Martínez-Trucharte 1 , Patricia González 2 , Joaquin Seras-Franzoso 1 , Albert Manzano 1 , Diego Arango 5 , Joan Sayós 6 , Ibane Abasolo 7 , Simo Schwartz 2
Affiliation  

Tumor recurrence, metastatic spread and progressive gain of chemo-resistance of advanced cancers are sustained by the presence of cancer stem cells (CSCs) within the tumor. Targeted therapies with the aim to eradicate these cells are thus highly regarded. However, often the use of new anti-cancer therapies is hampered by pharmacokinetic demands. Drug delivery through nanoparticles has great potential to increase efficacy and reduce toxicity and adverse effects. However, its production has to be based on intelligent design. Likewise, we developed polymeric nanoparticles loaded with Zileuton™, a potent inhibitor of cancer stem cells (CSCs), which was chosen based on high throughput screening. Its great potential for CSCs treatment was subsequently demonstrated in in vitro and in in vivo CSC fluorescent models. Encapsulated Zileuton™ reduces amount of CSCs within the tumor and effectively blocks the circulating tumor cells (CTCs) in the blood stream and metastatic spread.

中文翻译:

载于聚合物胶束中的Zileuton™可有效减少乳腺癌循环的肿瘤细胞和肿瘤内癌症干细胞。

肿瘤中存在癌症干细胞(CSC)可维持晚期癌症的肿瘤复发,转移扩散和化学耐药性的逐步提高。因此,高度重视旨在根除这些细胞的靶向疗法。但是,药代动力学需求常常阻碍了新抗癌疗法的使用。通过纳米颗粒的药物输送具有增加功效,减少毒性和不良作用的巨大潜力。但是,其生产必须基于智能设计。同样,我们开发了装载有Zileuton™(一种有效的癌症干细胞抑制剂)的聚合物纳米颗粒,该聚合物是基于高通量筛选而选择的。随后在体外和体内CSC荧光模型中证明了其在CSCs治疗中的巨大潜力。
更新日期:2019-10-27
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