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Purposes Zero-dimensional carbon nanomaterial-based targeting drug delivery system has shown broad application prospects in the field of tumor therapy since the complex is constructed by using carbon nanomaterials with good stability and biocompatibility as drug carries and carries drugs, genes, and targeting components. Methods In this review, the structure of zero-dimensional carbon nanomaterial as drug carriers, the construction of targeting drug delivery systems, and their applications in chemotherapy, gene therapy, and integration of diagnosis and treatment are reviewed. First, the structure of zero-dimensional carbon nanomaterial is classified. Second, the construction strategies of carbon nanomaterial-based targeting drug delivery system are summarized from two aspects: targeting modification and drug loading. Finally, the application advances of zero-dimensional carbon nanomaterial-based targeting drug delivery system is reviewed, and the current problems they face in tumor treatment are presented. Conclusions This work provides some theoretical support and practical experience for the extensive application of zero-dimensional carbon nanomaterial-based targeting drug delivery systems in the biomedical field.