BACKGROUNDCoaxial electrospray is an emerging technology to produce multilayer micro- and nano-particles (NPs) with well controlled shape and size. ALA-PDT is a fascinating technology used in the treatment for skin and other cancers. In this work, ALA-loaded poly(lactide-co-glycolide) (PLGA) (PLGA-ALA) NPs with high drug loading efficiency were produced via coaxial electrospray and used for the PDT treatment in HSC-3 cells. RESULTSResults showed that 200-1000nm PLGA-ALA NPs with 60-75% ALA loading efficiency were successfully produced. ALA and PLGA were well integrated and no extra chemical reaction occurred during the electrospray. PLGA-ALA NPs displayed a delayed release of ALA in PBS solution up to 7 days. A massive accumulation of PpIX in HSC-3 cells happened after the incubation of PLGA-ALA NPs. With light irradiation, these PLGA-ALA NPs showed a remarkable cytotoxicity against HSC-3 cells, leading to 40-70% cell death depending on the incubation dose. CONCLUSIONSCoaxial electrospraying is a facile method to prepare PLGA-ALA NPs with high drug loading content and efficiency, and PLGA-ALA NPs turned out to be an effective vehicle for delivering ALA to tumor cells. (c) 2015 Society of Chemical Industry