用 MUC1 适体功能化的 PLA-PEG 纳米载体靶向肺癌细胞。
Targeting lung cancer cells with MUC1 aptamer-functionalized PLA-PEG nanocarriers.
机构信息
Department of Materials Engineering, Babol Noshirvani University of Technology, Shariati Ave., 47148-71167, Babol, Iran.
Nanobiotechnology Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran.
出版信息
Sci Rep. 2022 Mar 18;12(1):4718. doi: 10.1038/s41598-022-08759-z.
MUC1 aptamer-functionalized PLA-PEG nanocarriers at various w/w ratios (polymer to doxorubicin weight ratio) were prepared by a double emulsion method. Physiochemical properties, encapsulation efficiency (EE), loading content (LC) and in vitro release kinetics of DOX were assessed. Furthermore, cytotoxicity and antitumor activity of prepared PLA-PEG-Apt/DOX NPs at w/w ratio 10:1 were evaluated by MTT assay and flow cytometry against MUC1-overexpressing A-549 cell line. Targeted nanocarriers (PLA-PEG-Apt/DOX NPs at w/w ratio 10:1) induced higher apoptosis rate (36.3 ± 3.44%) for 24 h in MUC1 positive A-549 cancer cells in compare to non-targeted form (PLA-PEG/DOX NPs at w/w ratio 10:1, 11.37 ± 1.65%) and free DOX (4.35 ± 0.81%). In other word, the percentage of cell death in A-549 lung cancer cells treated with PLA-PEG-Apt/DOX NPs at w/w ratio 10:1 is 3.19 and 8.34 fold higher than in non-targeted form and Free DOX treated cancer cells, respectively. Therefore, PLA-PEG-Apt/DOX NPs might be considered a promising drug delivery system for targeted drug delivery towards MUC1-overexpressing tumors cells.
通过复乳法制备了不同 w/w 比（聚合物与阿霉素重量比）的 MUC1 适体功能化 PLA-PEG 纳米载体。评估了 DOX 的物理化学性质、包封效率（EE）、载药量（LC）和体外释放动力学。此外，通过 MTT 分析和流式细胞术，评估了 w/w 比为 10:1 的制备的 PLA-PEG-Apt/DOX NPs 对高表达 MUC1 的 A-549 细胞系的细胞毒性和抗肿瘤活性。与非靶向形式（w/w 比为 10:1 的 PLA-PEG/DOX NPs，11.37±1.65%）和游离 DOX（4.35±0.81%）相比，靶向纳米载体（w/w 比为 10:1 的 PLA-PEG-Apt/DOX NPs）在 24 小时内诱导 MUC1 阳性 A-549 癌细胞的凋亡率更高（36.3±3.44%）。换句话说，w/w 比为 10:1 的 PLA-PEG-Apt/DOX NPs 处理的 A-549 肺癌细胞的细胞死亡率比非靶向形式和游离 DOX 处理的癌细胞分别高 3.19 倍和 8.34 倍。因此，PLA-PEG-Apt/DOX NPs 可以被认为是一种有前途的靶向药物传递系统，用于向高表达 MUC1 的肿瘤细胞进行靶向药物传递。
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