Ce(IV) doped anatase TiO2nanoparticles (CDTs) were prepared and the underlying mechanism by which CDT nanoparticle enters into cell and its cytotoxicity were investigated in a human hepatocellular line L02 cell. The results showed that CDTs can enter into cytoplasm of L02 cell via endocytosis and nonendocytic ways. Large aggregation of CDTs went into cell by endocytosis and finally formed an endocytic vesicle with membrane boundary. Tiny aggregation of CDTs entered into cell cytoplasm via channels similar to that for lung-blood substance exchange in the alveolar-airway barrier. In addition, tiny aggregation of CDTs was observed in nucleus, and maybe CDTs could pass through the nucleus envelope via the channels provided by nuclear pore complexes (NPCs). Results from MTT assay, fluorescence microscope, and TEM observations showed that the cell viability, cell morphology, cell growth, and cell division periods could not be obviously impaired when cells were exposed to CDTs of different concentration from 30 to 150 μg mL−1without UV irradiation. However, large vacuoles containing CDTs were found in cytoplasm, some structure changes were observed in mitochondria, and smooth envelope around the nucleus was shrank and deformed.