This study aimed to develop an anthelmintic that leaves no residues and is safe and efficient for use in cows. We constructed classical pseudoternary phase diagrams using experimental animal data to optimize and characterize the eprinomectin nanoemulsion formulas. The emulsion samples prepared with ethyl acetate, polysorbate 80, and 1-propanediol as the main components were transparent and uniform when observed under a Hitachi transmission electron microscope (TEM) system. A Mastersizer 3000 laser particle size analyzer was used to determine the particle sizes of the prepared nanoemulsions. The nanoemulsions were homogeneously dispersed, with an average particle size of 12.61 nm and a polydispersity index of (PDI) 0.297. High-performance liquid chromatography confirmed no statistically significant changes in the samples after 24 months at 4 °C, 25 °C, and 37 °C; the samples exhibited long-term stability. The PK/PD studies confirmed that the injection of eprinomectin nanoemulsions at a dose of 0.2 mg/kg body weight was effective, with a withdrawal period of 0 days for dairy cows. The total extermination rate of the nanoemulsions against adult nematodes was 98.40±1.52%. The AUCmilk/plasma ratio was 0.67±0.03. The optimal dose was found to be 0.2 mg/kg body weight.