Aim: We aimed to develop nanoemulsions containing phosphodiesterase 4 inhibitor rolipram with different droplet sizes, to evaluate the anti-inflammatory effect against activated neutrophils and a related lung injury. Materials & methods: We prepared nanoemulsions of three different sizes, 68, 133 and 188 nm. Results: The nanoemulsion inhibited the superoxide anion but not elastase release in primary human neutrophils. The large-sized nanoemulsions were mostly internalized by neutrophils, resulting in the reduction of intracellular Ca2+ half-life. The peripheral organ distribution of near-infrared dye-tagged nanoemulsions increased, following the decrease in droplet diameter. Rolipram entrapment into intravenous nanoemulsions ameliorated pulmonary inflammation. The smallest droplet size showed improvement, compared with the largest size. Conclusion: We established a foundation for the development of nanoemulsions against inflamed lung disease.

Chinese Herbal Medicine Research Team Healthy Aging Research Center Chang Gung University Kweishan Taoyuan 333 Taiwan

Department of Anesthesiology Chang Gung Memorial Hospital Kweishan Taoyuan 333 Taiwan

Department of Chemical Engineering Ming Chi University of Technology New Taipei City 243 Taiwan

Graduate Institute of Biomedical Sciences Chang Gung University Kweishan Taoyuan 333 Taiwan

Graduate Institute of Natural Products Chang Gung University Kweishan Taoyuan 333 Taiwan

Institute of Macromolecular Chemistry Czech Academy of Sciences Prague 11720 Czech Republic

Research Center for Food and Cosmetic Safety and Research Center for Chinese Herbal Medicine Chang Gung University of Science and Technology Kweishan Taoyuan 333 Taiwan

School of Medicine College of Medicine Chang Gung University Kweishan Taoyuan 333 Taiwan

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