▎ 摘　　要

Breast cancer is one of the most life-threatening malignancies with high mortality among women. Chemotherapy, radiotherapy, surgical operation, and combination therapy are commonly applied modalities in breast cancer therapy. However, the full treatment of the disease is often failed because of the formation of a permissive milieu, so-called tumor microenvironment (TME). In such a setting, immunosurveillance is impaired and high-pressure tumor interstitial fluid resists drug penetration due to the creation of irregular tumor microvasculature, the initiation of drug resistance mechanisms, the emergence of undesired side effects, and relapse of the disease even after a vigorous treatment. To tackle these pitfalls, smart multifunctional nanosystems (NSs) have been developed based on passive and active targeting mechanisms. Of various NSs, graphene-based nanosystems (GrNSs) offer unique physicochemical features, including functionalization with various targeting and imaging ligands, offering photothermal and photodynamic therapy (PTT and PDT) potentials combined with chemotherapy of the loaded drugs. Multimodal GrNSs, to be transformed into precision medicine, demand rationalized preclinical and clinical studies to examine their pharmacokinetics and pharmacodynamics (PD) properties together with their behaviors in TME. For a successful transformation towards personalized nano-medicine, furthermore, key pivotal patient- and formulation-oriented challenges (e.g., patients' genomic/proteomic profiles and PK/PD properties) must be addressed before any clinical interventions. This review provides comprehensive insights into the smart GrNSs and discusses their applications for the concurrent diagnosis and treatment of solid tumors.