Abstract: Objective · To engineer a light-induced size-switchable (large to small) nanosystem for doxorubicin (DOX) delivery and characterize its light-induced size change and cytotoxicity. Methods · The poly(ethylene glycol)-polylactide nanoparticles loading DOX (PEG-PLA-DOX) were fabricated with the dropwise addition method. Then the nanoparticles were encapsulated into the inner cavity of liposome (LP), and a photosensitizer (verteporfin, VP) was loaded in the bilayers of the LP to engineer the near-infrared light-sensitive core-shell nanoparticles (PEG-PLA-DOX@LP). The morphology of the nanoparticles was observed under a transmission electron microscope. Dynamic light scattering was used to examine the particle size at each stage. The size-switchable property of the nanoparticles and its influence on viability of murine melanoma B16F10 cells under near-infrared light were evaluated. The stability of the nanoparticles was also investigated. Results · PEG-PLA-DOX@LP, the light-sensitive nanoparticles, were successfully developed. The nanoparticles had a particle size of (194.83±5.70) nm and Zeta potential of (-1.43±0.32) mV. The drug loading was 2.82% for DOX, and 1.16% for VP. The small-sized PEG-PLA-DOX [(37.42±8.67) nm]was quickly released the nanoparticles upon light for enhanced toxicity to B16F10 murine melanoma cells. Conclusion · The particle size of the novel DOX delivery nanosystem rapidly changes large size to small size upon the irradiation of near-infrared light, and thus the cytotoxic effect on tumor cells can be enhanced. [Key words]near-infrared light; doxorubicin; nanoparticle; size-switchable[National Natural Science Foundation of China, 81773274; Foundation of Shanghai Local High Level University (First-class Discipline–Pharmacy) ]。

Key words: near-infrared light, doxorubicin, nanoparticle, size-switchable[National Natural Science Foundation of China, 81773274, Foundation of Shanghai Local High Level University (First-class Discipline&, ndash, Pharmacy) ]。