Artesunate-loaded porous PLGA microsphere as a pulmonary delivery system for the treatment of non-small cell lung cancer

Abstract Non-small cell lung cancer (NSCLC) has emerged to be a significant cause of cancer mortality worldwide. Artesunate (ART) extracted from Chinese herb Artemisia annua L, has been proven to possess desirable anti-cancer efficacy, especially for the metastatic NSCLC treatment. Moreover, the poly(lactic-co-glycolic acid) (PLGA) microsphere has been considered to be a potential pulmonary delivery system for the sustained drug release to enhance the therapeutic efficacy of lung cancer. Herein, the ART-loaded porous PLGA microsphere was prepared through the emulsion solvent evaporation approach. The microsphere was demonstrated to possess highly porous structure and ideal aerodynamic diameter for the pulmonary administration. Meanwhile, sustained ART release was obtained from the porous microsphere within 8 days. The release solution collected from the microsphere could be effectively uptake by the cells and further induce the cell apoptosis and the cell cycle arrest at G2/M phase to execute the anti-proliferative effect, using human lung adenocarcinoma cell line A549 as a model. Additionally, strong inhibitory effect on the cell migration and invasion could be obtained after the treatment with release solution. Taken together, our results demonstrated that the ART-loaded PLGA porous microsphere could achieve excellent anti-cancer efficacy, providing a potential approach for the NSCLC treatment via the pulmonary administration.