Yu Chaosheng, Long Zhen, Qiu Qianhui, Liu Fang, Xu Yiming, Zhang Tao, Guo Rui, Zhong Wen, Huang Shuixian, Chen Shuaijun
Department of Otorhinolaryngology Head and Neck Surgery, Zhujiang Hospital Southern Medical University Guangzhou China.
Guangzhou Red Cross Hospital Jinan University Guangzhou China.
Bioeng Transl Med. 2021 Nov 26;7(2):e10270. doi: 10.1002/btm2.10270. eCollection 2022 May.
One of the main clinical treatments for advanced nasopharyngeal carcinoma is chemotherapy, but systemic administration can cause serious adverse reactions. New type of nanomaterial which can actively targeting, imaging, and treating nasopharyngeal carcinoma at the same time to enhance the effect of chemotherapy, meanwhile monitoring the intracellular drug release process at the level of single cancer cell was urgently needed. GE11, an EGFR antagonist peptide, was used to target nasopharyngeal carcinoma which has positive expression of EGFR on its nucleus. GE11-modified graphene quantum dots (GQDs@GE11) were used as drug carriers for clinical chemotherapeutics cisplatin (CDDP) and doxorubicin (DOX). The emission spectrum of GQDs (460 nm) and the excitation spectrum of DOX (470 nm) have a good overlap, thus the transfer and release process of DOX can be sensitively detected by the fluorescence resonance energy transfer (FRET). CDDP was used to enhance the chemotherapy effect of nanoprobe, and the loading amount of DOX and CDDP on GQDs@GE11 nanoprobe were up to 67 and 50 mg/g, respectively. In vivo experiments have confirmed that GQDs@GE11/CDDP/DOX nanoprobe can be enriched to tumor site through specific targeting effect, and significantly inhibit tumor cell proliferation. This new type of targeted therapy fluorescent probe provides new ideas for the study of drug release process and the treatment of nasopharyngeal carcinoma.
晚期鼻咽癌的主要临床治疗方法之一是化疗，但全身给药会引起严重的不良反应。迫切需要一种新型纳米材料，它能够同时对鼻咽癌进行主动靶向、成像和治疗，以增强化疗效果，同时在单个癌细胞水平监测细胞内药物释放过程。GE11是一种表皮生长因子受体（EGFR）拮抗剂肽，用于靶向细胞核上EGFR呈阳性表达的鼻咽癌。GE11修饰的石墨烯量子点（GQDs@GE11）被用作临床化疗药物顺铂（CDDP）和阿霉素（DOX）的药物载体。石墨烯量子点的发射光谱（460nm）与阿霉素的激发光谱（470nm）有良好的重叠，因此可以通过荧光共振能量转移（FRET）灵敏地检测阿霉素的转移和释放过程。顺铂用于增强纳米探针的化疗效果，阿霉素和顺铂在GQDs@GE11纳米探针上的负载量分别高达67和50mg/g。体内实验证实，GQDs@GE11/CDDP/DOX纳米探针可通过特异性靶向作用富集到肿瘤部位，并显著抑制肿瘤细胞增殖。这种新型靶向治疗荧光探针为药物释放过程研究和鼻咽癌治疗提供了新思路。
