The acute respiratory distress syndrome (ARDS) is a severe form of acute lung injury (ALI). Its pathogenesis is closely linked with reactive oxygen species (ROS). Antioxidation has been considered as an efficient treatment. Besides, liposomes are widely investigated as potential drug carriers due to their ability to protect and carry drug molecules to the target organ such as the lung. The present study was undertaken to investigate whether dipyridamole (DIP), delivered as a liposomal preparation, can ameliorate the lipopolysaccharides (LPS)-induced ALI due to the changes of its biodistribution. First, the liposomes entrapping DIP were prepared by film hydration for treating ARDS. Subsequently, the characterizations including entrapment efficiency, size, span and micrograph of DIP liposomes were measured. The concentration change of DIP in tissues and plasma of mice after intravenous administration of DIP injection and DIP liposomes was determined by RP-HPLC and calculated to lung targeting parameters. To prove the therapeutic efficiency, the effects of DIP liposomes on LPS-induced ALI were studied compared with DIP injection. The results showed DIP liposomes have the relative high entrapment efficiency and satisfying particle size. Compared with DIP injection, the liposomes increased the accumulation of DIP in the lung on a vast scale. Furthermore, DIP liposomes alleviated the ALI induced by LPS significantly. All of the results suggested that DIP liposomes have the potential efficacy in treating ALI/ARDS due to their obvious lung targeting.