Malignant tumors are among the primary diseases threatening public health in China, and traditional Chinese medicine has been proven to be an important means of cancer prevention and treatment. However, the strong hydrophobicity, poor stability, low bioavailability, and short half-life of active ingredients of traditional Chinese medicine limit their clinical use. Nanoformulations, as an innovative type of formulation, offer unique advantages in targeted delivery, controlled release, and combination therapy. The combination of nanoformulations with active ingredients of traditional Chinese medicine can improve their bioavailability and biological activity. This article reviews the characteristics and applications of active ingredients of TCM and their nanoformulations in recent years, aiming to provide scientific basis and reference for the development of novel anti-tumor drugs derived from traditional Chinese medicine.