Xing Enyun, Du Yingying, Yin Juanjuan, Chen Minghui, Zhu Mengyao, Wen Xiaona, Xu Jialiang, Feng Yaqing, Meng Shuxian
School of Chemical Engineering and Technology, Tianjin University, Tianjin, 300050, P.R. China.
Department of Pharmacy, The Third Central Hospital of Tianjin, Tianjin Key Laboratory of Extracorporeal Life Support for Critical Diseases, Artificial Cell Engineering Technology Research Center, Tianjin Institute of Hepatobiliary Disease, Tianjin, 300170, China.
Adv Healthc Mater. 2021 Apr;10(8):e2001874. doi: 10.1002/adhm.202001874. Epub 2021 Jan 14.
Targeted synergistic therapy has broad prospects in tumor treatments. Here, a multi-functional nanodrug GDYO-CDDP/DOX@DSPE-PEG-MTX (GCDM) based on three traditional anticancer drugs (doxorubicin (DOX), cisplatin (CDDP) and methotrexate (MTX)) modified graphdiyne oxide (GDYO) is described, for diagnosis and targeted cancer photo-chemo synergetic therapy. In this system, for the first time, these three traditional anti-cancer drugs have played new roles and can reduce multidrug resistance through synergistic anti-tumor effects. Cisplatin can be hybridized with GDYO to form a multifunctional and well-dispersed three-dimensional framework, which can not only be used as nano-drug carriers to achieve high drug loading rates (40.3%), but also exhibit excellent photothermal conversion efficiency (47%) and good photodynamic effects under NIR irradiation. Doxorubicin (DOX) is loaded onto GDYO-CDDP through π-π stacking, which is used as an anticancer drug and as a fluorescent probe for nanodrug detection. Methotrexate (MTX) can be applied in tumor targeting and play a role in synergistic chemotherapy with DOX and CDDP. The synthesized multi-functional nanodrug GCDM has good biocompatibility, active targeting, long-term retention, sustained drug release, excellent fluorescence imaging capabilities, and remarkable photo-chemo synergistic therapeutic effects.
靶向协同治疗在肿瘤治疗中具有广阔前景。在此，描述了一种基于三种传统抗癌药物（阿霉素（DOX）、顺铂（CDDP）和甲氨蝶呤（MTX））修饰的氧化石墨烯（GDYO）的多功能纳米药物GDYO-CDDP/DOX@DSPE-PEG-MTX（GCDM），用于癌症的诊断和靶向光化学协同治疗。在该体系中，这三种传统抗癌药物首次发挥了新作用，并可通过协同抗肿瘤作用降低多药耐药性。顺铂可与GDYO杂交形成多功能且分散良好的三维框架，其不仅可作为纳米药物载体实现高载药率（40.3%），还在近红外照射下表现出优异的光热转换效率（47%）和良好的光动力效应。阿霉素（DOX）通过π-π堆积负载于GDYO-CDDP上，其既用作抗癌药物，又作为纳米药物检测的荧光探针。甲氨蝶呤（MTX）可用于肿瘤靶向，并在与DOX和CDDP的协同化疗中发挥作用。合成的多功能纳米药物GCDM具有良好的生物相容性、主动靶向性、长期保留性、药物缓释性、优异的荧光成像能力以及显著的光化学协同治疗效果。
