The rapid advancement of nanotechnology, when integrated with traditional Chinese medicine (TCM), is not only expanding the application scope of TCM but also driving its modernization. This chapter focuses on exploring the potential of combining nano-delivery systems with traditional Chinese herbal medicines and TCM theories for tumor treatment. First, it will elaborate on the antitumor properties of TCM and the underlying mechanisms. Second, it emphasizes the synergistic effects between nano-delivery systems and traditional herbal remedies, with a particular focus on their role in boosting therapeutic efficacy. Furthermore, this chapter discusses how such integration can facilitate the modernization of herbal medicines and enhance their global accessibility. Finally, it analyzes the current challenges and future research directions in this emerging interdisciplinary field. Overall, the application of nanotechnology in TCM offers a promising strategy for advancing tumor therapy and reinforcing the relevance of TCM in contemporary medical practice.