RESUMO
OBJECTIVE: To prepare ovarian cancer targeted photosensitizer albumin nanoconjugates, and investigate their tumor-targeting ability and antitumor response. METHODS: The intracellular uptake and uptake mechanism were investigated by confocal laser scanning microscope, flow cytometry and lysosome labeling. The cytotoxicity was detected by Alamar Blue and Calcein AM/PI staining. The antitumor mechanism of cRGD-PEG-HSA-IR700 was investigated by observing the generation of reactive oxygen species(ROS) and apoptosis. The tumor targeting ability of nanoconjugates was observed by constructing SKOV-3-NIH-3T3/GFP spheroids. RESULTS: The intracellular uptake of cRGD-PEG-HSA-IR700 in integrin overexpressed SKOV-3 cells was 3.8 fold higher than that of PEG-HSA-IR700, and cRGD-PEG-HSA-IR700 mainly distributed in lysosomes after uptake, where as the uptake of PEG-HSA-IR700 and cRGD-PEG-HSA-IR700 in integrin free NIH-3T3 cells was little.No photokilling effect was observed in the IR700, PEG-HSA-IR700 and cRGD-PEG-HSA-IR700 without light irradiation groups, while remarkable cytotoxicity was shown in the cRGD-PEG-HSA-IR700 with light irradiation group owing to the light-induced intracellular ROS generation and apoptosis.CONCLUSION: The tumor-specific nanoconjugates may become a new drug delivery platform for enabling targeted photodynamic therapy of cancer.