Department of Medical Biotechnology, College of Biomedical Sciences, Kangwon National University, Chuncheon, 200-701, South Korea.
Department of Marine Bio-Pharmacology, College of Food Science and Technology, Shanghai Ocean University, Shanghai, 201306, China.
Carbohydr Polym. 2020 Oct 1;245:116407. doi: 10.1016/j.carbpol.2020.116407. Epub 2020 May 20.
The present work was developed the pH dependent-aptamer AS1411 (APT) decorated and erlotinib (En) loaded chitosan nanoparticles (CSNPs) for promising non-small-cell lung carcinoma (NSCLC) treatment. The characterization studies revealed that formulated APT-En-CSNPs were spherical in shape with size of 165.95 d. nm and PDI of 0.212. FTIR spectrum recorded molecular chemical interactions with composition of En or En-CSNPs. Cell viability assay, flow cytometry and fluorescent microscopy results revealed that APT-En-CSNPs triggered cancer cell death through pH-sensitive and nucleolin receptor-targeted release of En. The decoration of the APT improved the cellular uptake of En as evidenced by cellular sensing fluorescence and BioTEM assay. The APT-En-CSNPs induced the apoptosis through excessive ROS generation, nucleus damage and Δψm loss in the A549 cells. Hence, the present study revealed that the APT-En-CSNPs improved the therapeutic efficiency of En in NSCLC through the nucleolin targeted drug release.
本工作开发了 pH 响应适体 AS1411（APT）修饰和厄洛替尼（En）负载壳聚糖纳米粒（CSNPs），用于有前景的非小细胞肺癌（NSCLC）治疗。表征研究表明，所制备的 APT-En-CSNPs 呈球形，粒径为 165.95 d。nm 和 PDI 为 0.212。FTIR 光谱记录了分子化学相互作用以及 En 或 En-CSNPs 的组成。细胞活力测定、流式细胞术和荧光显微镜结果表明，APT-En-CSNPs 通过 pH 敏感和核仁素受体靶向释放 En 触发癌细胞死亡。APT 的修饰提高了 En 的细胞摄取，这可以通过细胞感应荧光和 BioTEM 试验证明。APT-En-CSNPs 通过过量 ROS 生成、细胞核损伤和 Δψm 在 A549 细胞中的损失诱导细胞凋亡。因此，本研究表明，APT-En-CSNPs 通过核仁素靶向药物释放提高了 NSCLC 中 En 的治疗效果。
