Nanomedicines overcome the pharmacokinetic limitations of traditional drug formulations and have promising prospect in cancer treatment. However, nanomedicine delivery in vivo is still facing challenges from the complex physiological environment. For the purpose of effective tumor therapy, they should be designed to guarantee the five features principle, including long blood circulation, efficient tumor accumulation, deep matrix penetration, enhanced cell internalization and accurate drug release. To ensure the excellent performance of the designed nanomedicine, it would be better to monitor the drug delivery process as well as the therapeutic effects by real-time imaging. In this review, we summarize strategies in developing nanomedicines for efficiently meeting the five features of drug delivery, and the role of several imaging modalities (fluorescent imaging (FL), magnetic resonance imaging (MRI), computed tomography (CT), photoacoustic imaging (PAI), positron emission tomography (PET), and electron microscopy) in tracing drug delivery and therapeutic effect in vivo based on five features principle.

纳米药物克服了传统药物制剂的药代动力学限制，在癌症治疗中具有广阔的前景。然而，体内纳米药物递送仍然面临着来自复杂生理环境的挑战。为实现有效的肿瘤治疗，其设计应保证血液循环长、肿瘤高效蓄积、基质深入渗透、细胞内化增强和药物释放准确五项原则。为了确保所设计的纳米药物的优异性能，最好通过实时成像监控药物输送过程以及治疗效果。在这篇综述中，我们总结了开发纳米药物以有效满足药物输送的五个特征的策略，以及几种成像方式（荧光成像（FL）、磁共振成像（MRI）、计算机断层扫描（CT）、光声成像（ PAI)、正电子发射断层扫描 (PET)、体内基于五特征原则。