Biocompatibility targeted magnetic nanocarriers are a promising alternative to conventional chemotherapy. Herein, Fe3O4 magnetic nanoparticles (MNPs) functionalized hyaluronic acid (HA)‐folic acid (FA) was synthesized and piperine (PIP) loaded into MNPs. In vitro release analyses, antioxidant activity, hemolysis assay, and intrinsic cytotoxicity of MNPs were determined. The results revealed that the synthesized MNPs released higher amount of piperine in acidic ambience in comparison with neutral ambience. PIP‐loaded prepared MNPs exhibited higher antioxidant activity in comparison with the carrier. On the other hand, prepared Fe3O4 MNPs is hemocompatible. Also, the synthesized MNPs demonstrated the considerable antiproliferative effects in MCF‐7 cancer cells compared with fibroblast cells. The results suggest that Fe3O4‐NH‐HA‐FA MNPs as novel targeted delivery system can enhance the therapeutic effect of piperine.
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