Metal-organic frameworks (MOFs) are regarded as promising drug delivery systems (DDSs) for cancer treatment because of their unique porous structures and controlled drug release properties. Herein, we designed and constructed a new multifunctional drug carrier 5-FU/UiO-67-(NH)₂-FAM/PMT (FUFP) with 5-FU/UiO-67-(NH)₂ as the nanocarriers, FAM as a fluorescence imaging agent and PMT as both FA target and anti-tumor drug (5-FAM = 5-carboxyfluorescein, 5-FU = 5-fluorouracil and PMT = pemetrexed). The drug carrier exhibited several functions, including co-loading drugs, targeted delivery and fluorescence imaging to enhance antitumor cytotoxicity for cancer therapy. Through fluorescence imaging and flow cytometry experiments, FUFP presented excellent fluorescence imaging and folate targeted properties to the high expression of folate receptor KB cell compared with low expression A549 cell and moderate expression HeLa cell. Meanwhile, FUFP exhibited superior anti-tumor activity compared single 5-FU and PMT group by the in vitro and vivo experiments. The biocompatibility test of FUFP indicated reasonable biosafety as no evidence of persistent toxicity in vivo was observed. FUFP has unique biological abilities in terms of pH-responsiveness, antitumor efficacy, biocompatibility, and simultaneously release hydrophobic and hydrophilic drug at the tumor site, indicating that this composite is a potential and promising carrier, in which provides a new strategy to co-deliver drugs for MOFs.

金属有机框架（MOF）由于其独特的多孔结构和受控的药物释放特性，被认为是用于癌症治疗的有前途的药物传递系统（DDS）。在这里，我们设计并构建了一种新型的多功能药物载体5-FU / UiO-67-（NH）₂ -FAM / PMT（FUFP）与5-FU / UiO-67-（NH）₂作为纳米载体，FAM作为荧光显像剂，PMT作为FA靶标和抗肿瘤药物（5-FAM = 5-羧基荧光素，5-FU = 5-氟尿嘧啶，PMT =培美曲塞）。药物载体表现出多种功能，包括共同装载药物，靶向递送和荧光成像，以增强针对癌症治疗的抗肿瘤细胞毒性。通过荧光成像和流式细胞术实验，与低表达的A549细胞和中等表达的HeLa细胞相比，FUFP对高表达的叶酸受体KB细胞表现出出色的荧光成像和叶酸靶向特性。同时，相比于单个5-FU和PMT组，FUFP在体外和体内均表现出优异的抗肿瘤活性。实验。FUFP的生物相容性测试表明合理的生物安全性，因为未观察到体内持续毒性的证据。FUFP在pH响应性，抗肿瘤功效，生物相容性方面具有独特的生物学能力，并同时在肿瘤部位释放疏水性和亲水性药物，这表明该复合物是潜在且有前途的载体，在其中提供了共同递送的新策略财政部药品。