Selective Inhibition of Osteosarcoma Cell Functions Induced By Curcumin‐Loaded Self‐assembled Arginine‐Rich‐RGD Nanospheres

Abstract

ObjectivesTo develop a treatment against osteosarcoma with higher selectivity towards osteosarcoma cells and lower cytotoxicity towards normal osteoblast cells.Statement of methodsCurcumin was found to have significant selectivity against osteosarcoma cells in vitro, and the ampiphilic peptide C18GR7RGDS was used as a carrier in aqueous solution. This peptide contains an arginine‐rich and an arginine‐glycine‐aspartic acid (RGD) structure, which may lead to efficient cell penetration and targeting for cancerous cells since RGD sequence can target to the overexpressed ανβ3 integrin. Using a method of co‐dissolution with acetic acid and dialysis tubing, the solubility of curcumin was enhanced and formed a homogeneous solution with the help of amphiphilic nanoparticles (APNPs). The cytotoxicity and cellular uptake of these materials on both osteosarcoma and normal healthy osteoblast cell lines were evaluated by MTT assays and confocal fluorescent microscopyResultsIt was demonstrated for the first time that APNPs formed nanospheres with diameters of 10‐20 nm in water and phosphate buffer saline (PBS), and opened up when the pH value was reduced to 4. The successful encapsulation of curcumin in APNPs was confirmed by Fourier transform infrared (FT‐IR) and X‐ray diffraction (XRD) analysis. The curcumin‐loaded APNPs exhibited a significant selective internalization against the MG‐63 osteosarcoma cell lineimageConclusionsAPNPs can encapsulate hydrophobic curcumin in their hydrophobic cores, and the curcumin‐loaded APNPs could be an innovative candidate for the selective inhibition against osteosarcoma.