Platinum-based combined chemo-radiotherapy is the most commonly used approach against Nasopharyngeal carcinoma (NPC). However, off target effect and poor efficiency are the two main concerns regarding this approach. Therefore, it is an urgent need to explore novel therapeutic modalities to meet clinically standards. In this work we have established a new anti-cancer drug delivery system, composed of cisplatin (CDDP)-loaded magnetic iron oxide nanoparticles (Fe₃O₄), further functionalized with surface modification of folic acid (FA) and intracellular aggregation ability peptide (Cys(StBu)-Lys-CBT), named as (FA-MNP-CDDP-CBT). FA-MNP-CDDP-CBT was much more effective on the reversal of CDDP resistance with an average reduction in half maximal inhibitory concentration (IC 50) of 40.9% and 59.1% in HNE-1 cells and HNE-1/DDP resistant cells respectively compared to CDDP alone. Moreover, FA-MNP-CDDP-CBT had also shown a superior targeted uptake effect and higher ROS generation. Convincingly, we observed a remarkable increase in the apoptosis rate of NPC cells by using western blot and flow cytometry. Thus, this newly design nano-system provides a facile approach to enhance the antitumor activity by reducing the side effects of chemotherapy, minimizing systemic toxicity, and reversing CDDP treatment resistance, which could be proposed for NPC patients with primary or secondary chemo-resistance in the future.

铂类联合放化疗是治疗鼻咽癌 (NPC) 最常用的方法。然而，脱靶效应和低效率是这种方法的两个主要问题。因此，迫切需要探索新的治疗方式以满足临床标准。在这项工作中，我们建立了一种新的抗癌药物递送系统，由负载顺铂 (CDDP) 的磁性氧化铁纳米粒子 (Fe ₃ O ₄），通过叶酸（FA）和细胞内聚集能力肽（Cys（StBu）-Lys-CBT）的表面修饰进一步功能化，命名为（FA-MNP-CDDP-CBT）。FA-MNP-CDDP-CBT 在逆转 CDDP 耐药性方面更有效，HNE-1 细胞和 HNE-1/DDP 耐药细胞的半数最大抑制浓度 (IC 50) 平均降低 40.9% 和 59.1%与单独的 CDDP 相比。此外，FA-MNP-CDDP-CBT 还显示出优异的靶向摄取效果和更高的 ROS 生成。令人信服的是，我们通过使用蛋白质印迹和流式细胞术观察到 NPC 细胞的凋亡率显着增加。因此，这种新设计的纳米系统提供了一种简便的方法，通过减少化疗的副作用、最小化全身毒性和逆转 CDDP 治疗耐药性来增强抗肿瘤活性，