BACKGROUND Nanoparticles are proven as a potential tool for treating various disorders. However, efficient nanoparticle delivery of anti-tumor drugs is urgently needed for tumor treatment. This study aimed to generate a drug-delivery nanoparticle with higher efficacy and safety. MATERIAL AND METHODS We developed a poly-(lactide-co-glycolide) (PLGA) nanoparticle (FLGA-Fe₃O₄+PFP) embedded with super-paramagnetic iron oxide (Fe₃O₄) and perfluoropentane (PFP). Characteristics of FLGA-Fe₃O₄+PFP nanoparticles were observed using optical microscopy, scanning electron microscopy, and transmission electron microscopy. HNE1 and HepG2 cells were cultured and used for experiments. MTT was used to evaluate cytotoxic effects of FLGA-Fe₃O₄+PFP nanoparticles on HNE1 and HepG2 cells. Cell engulfment capacity was examined and a cell targeting experiment was conducted to evaluate invasive capability and binding efficiency of PLGA+Fe₃O₄+PFP nanoparticles, respectively. Biological toxicity of PLGA+Fe₃O₄+PFP nanoparticles in rats was evaluated by determining CK, LDH, creatinine, and UA levels, and ALT and AST activities. RESULTS PLGA+Fe₃O₄+PFP nanoparticles demonstrated well-defined spherical and dispersed morphology with smooth surfaces. There were scattered black spots on shells of PLGA+Fe₃O₄+PFP nanoparticles. PLGA+Fe₃O₄+PFP nanoparticles did not trigger obvious effects on cell viability of HNE1 and HepG2 cells. HNE1 and HepG2 cells demonstrated higher engulfment capacity for PLGA+ Fe₃O₄+PFP nanoparticles. PLGA+Fe₃O₄+PFP nanoparticles demonstrated higher targeting CDDP delivery efficacy and promoted binding efficiency of targeting CDDP with cells. PLGA+Fe₃O₄+PFP nanoparticles demonstrated no obvious toxic effects on heart, kidney, liver (without effects on CK, LDH, creatinine, UA levels, and ALT and AST activities). CONCLUSIONS PLGA+Fe₃O₄+PFP nanoparticles were safe, with higher invasive ability and binding efficiency of targeting CDDP with tumor cells. Therefore, PLGA+Fe₃O₄+PFP nanoparticles demonstrated potential anti-tumor effects after transplantation.