Abstract: OBJECTIVE To prepare α-asarone into polyethylene glycol-polylactic acid-α-asarone nanoparticles (PEG-PLA-α-asarone nanoparticles), and investigate the surface properties of PEG-PLA-α-asarone nanoparticles and the nasal cilia toxicity after nasal administration. METHODS α-Asarone was prepared into PEG-PLA-α-asarone nanoparticles by organic solvent evaporation method. PEG-PLA-α-asarone nanoparticles were characterized by nano-particle size locator, transmission electron microscope, differential scanning calorimeter and X-ray diffraction method. In vitro release behavior of PEG-PLA-α-asarone nanoparticles was studied by dialysis method. The rat model was used to investigate the nasal cilia toxicity of PEG-PLA-α-asarone nanoparticles after nasal administration. RESULTS The average particle size of PEG-PLA-α-asarone nanoparticles was 172.3 nm, the PDI index was 0.256, the drug loading was 10.70%, and the entrapment efficiency was 59.36%. The characterization results showed that α-asarone was mainly in the form of molecular dispersion exist in PEG-PLA-α-asarone nanoparticles. In vitro release behavior of α-asarone in PEG-PLA-α-asarone nanoparticles was in accordance with the Ritger-peppas fitting equation. The result of nasal cilia toxicity study showed that PEG-PLA-α-asarone nanoparticles had no apparent toxicity to nasal cilia after nasal administration. CONCLUSION PEG-PLA-α-asarone nanoparticles prepared by volatilization of organic solvents method can be used for nasal administration.