A variety of targeted nanoparticles were developed for the diagnosis and therapy of orthotopic and metastatic bone tumors during the past decade. This critical review will focus on principles and methods in the design of these bone-targeted nanoparticles. Ligands including bisphosphonates, aspartic acid-rich peptides and synthetic polymers were grafted on nanoparticles such as PLGA nanoparticles, liposomes, dendrimers and inorganic nanoparticles for bone targeting. Besides, other ligands such as monoclonal antibodies, peptides and aptamers targeting biomarkers on tumor/bone cells were identified for targeted diagnosis and therapy. Examples of targeted nanoparticles for the early detection of bone metastatic tumors and the ablation of cancer via chemotherapy, photothermal therapy, gene therapy and combination therapy will be intensively reviewed. The development of multifunctional nanoparticles to break down the “vicious” cycle between tumor cell proliferation and bone resorption, and the challenges and perspectives in this area will be discussed.

在过去的十年中，开发了多种靶向纳米粒子用于原位和转移性骨肿瘤的诊断和治疗。这篇重要的评论将着重于这些靶向骨的纳米颗粒的设计原理和方法。将包括双膦酸酯，富天冬氨酸的肽和合成聚合物在内的配体接枝到纳米颗粒（例如PLGA纳米颗粒，脂质体，树状聚合物和无机纳米颗粒）上，以进行骨靶向。此外，还鉴定了靶向肿瘤/骨细胞上生物标志物的其他配体，例如单克隆抗体，肽和适体，用于靶向诊断和治疗。通过化学疗法，光热疗法，基因疗法和联合疗法，用于骨转移性肿瘤的早期检测和癌症消融的靶向纳米粒子的实例将得到深入研究。