Objective　To explore the biological effect of drug-loaded nanoparticles from Ershiwuwei Shanhu’Pill.　Methods　The ESP drug-loaded nanoparticles were incubated with SH-SY5Y cells for 8hrs. Cellular uptake and intracellular distribution was observed by immunofluorescent staining assays. Intracellular translocation was tracked by transmission electron microscopy (TEM). Rats were randomly divided into a model group and an ESP-treated group, being injected with normal water or drug-loaded nanoparticles through tail vein, respectively. HE staining was used to observe liver pathological change. Changes of excitatory was assessed by open field test. SH-SY5Y development on the ESP insoluble components were measured by scanning electron microscope (SEM).    Results    The drug-loaded nanoparticles could fill the whole cells and the cellular nucleus was fragmentized. In vivo experiments, the liver cells in the treatment group had liquefactive necrosis. Compared with the model group, total distance was significantly improved in ESP-treated group (P＜0.05). Cells regularly growing on the insoluble component exsited in ESP. Conclusion　Drug-loaded nanoparticles from ESP may lead to anxiety and strongliver toxicity of rats.