Graphene quantum dots capped in hollow mesoporous silica nanoparticles (GQDs@hMSN) exhibited great potential in medical applications due to its good optical properties and high drug loading capacity. Compared with antibodies, peptide has a better affinity with target proteins. Herein, we demonstrated efficient targeting of triple-negative breast cancer with GQDs@hMSN, which was conjugated to a peptide ligand, F3 against nucleolin, to form GQDs@hMSN-F3. The core/shell GQDs@hMSN and GQDs@hMSN-F3 had diameters of 100 nm and 130 nm, respectively, based on transmission electron microscope (TEM) and dynamic laser scattering (DLS) measurement. Doxorubicin (DOX) was loaded onto GQDs@hMSN with a relatively high loading capacity. Systematic in vitro and in vivo studies were performed to investigate the targeting specificity and tissue distribution of GQDs@hMSN conjugates. Fluorescence microscopy examination and flow cytometry confirmed the targeting specificity of F3-attached GQDs@hMSN conjugates against cell nucleolin. A more potent uptake of GQDs@hMSN-F3 in MDA-MB-231 nodules was witnessed when compared with that of non-targeted GQDs@hMSN. Based on the findings from cellular targeting and in vivo fluorescence imaging, F3-attached GQDs@hMSN conjugates had the potential to serve as an image-guidable, tumor-selective cargo delivery nanoplatform.

盖在空心介孔二氧化硅纳米粒子（GQDs @ hMSN）中的石墨烯量子点因其良好的光学性能和高载药量而在医疗应用中显示出巨大的潜力。与抗体相比，肽与靶蛋白具有更好的亲和力。在本文中，我们证明了GQDs @ hMSN可有效靶向三阴性乳腺癌，GQDs @ hMSN与肽配体F3结合核仁素形成GQDs @ hMSN-F3。基于透射电子显微镜（TEM）和动态激光散射（DLS）测量，核/壳GQDs @ hMSN和GQDs @ hMSN-F3的直径分别为100 nm和130 nm。阿霉素（DOX）以相对较高的装载量装载到GQDs @ hMSN上。进行了系统的体外和体内研究，以研究GQDs @ hMSN共轭物的靶向特异性和组织分布。荧光显微镜检查和流式细胞术证实了F3连接的GQDs @ hMSN缀合物对细胞核蛋白的靶向特异性。与非靶向GQDs @ hMSN相比，MDA-MB-231结节中GQDs @ hMSN-F3的吸收更有效。基于细胞靶向和体内荧光成像的发现，F3连接的GQDs @ hMSN偶联物具有作为图像指导的，对肿瘤有选择性的货物递送纳米平台的潜力。与非靶向GQDs @ hMSN相比，MDA-MB-231结节中GQDs @ hMSN-F3的吸收更有效。基于细胞靶向和体内荧光成像的发现，F3连接的GQDs @ hMSN偶联物具有作为图像指导的，对肿瘤有选择性的货物递送纳米平台的潜力。与非靶向GQDs @ hMSN相比，MDA-MB-231结节中GQDs @ hMSN-F3的吸收更有效。基于细胞靶向和体内荧光成像的发现，F3连接的GQDs @ hMSN偶联物具有作为图像指导的，对肿瘤有选择性的货物递送纳米平台的潜力。