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Platinum-based drugs are used to treat a variety of cancers but have many side effects such as nephrotoxicity and neurotoxicity. A folate-decorated nanoparticles system with a good drug payload can selectively deliver drugs into folate receptor (FR)-overexpressing cancer cells to prevent the shortcomings of platinum-based chemotherapy. Here, folate-decorated and near-infrared (NIR) laser-activated nanoparticles (abbreviated as PtIV-FINPs) were prepared via ultrasonic self-assembling of platinum(IV) prodrug c,c,t-Pt(NH3)2Cl2(OOCCH2CH2COOH)2, folic acid (FA)-functionalized lipid DSPE-PEG-FA and NIR fluorescent dye indocyanine green (ICG). The obtained PtIV-FINPs had almost spherical shape with a mean diameter about 100 nm. In vitro cellular uptake, cytotoxicity assays revealed that upon NIR irradiation, PtIV-FINPs further enhanced cellular uptake and generated higher cytotoxicity against human ovarian carcinoma SKOV3 cells than non-targeted or non-NIR activated nanoparticles. Thus, the multifunctional nanoparticles have potential to be developed as an attractive drug delivery system for effective chemotherapy against FR-overexpressing cells. [ABSTRACT FROM AUTHOR]