Colorectal cancer (CRC), as the third most prevalent cancer and fourth principal cause of cancer death worldwide, is in urgent need of effective treatments. Though chemotherapy is still one of the powerful tools available for cancer therapy, it suffers from some limitations including lack of selectivity, aggregation and low biocompatibility. Therefore, the application of targeted drug delivery systems (DDS) is of greatest importance, among which nanoparticles have attracted considerable attention as carriers. In this study, after Calcium Carbonate (CaCO3) nanoparticles were synthesized via spontaneous precipitation method, the synthesized nanoparticles were characterized by X-ray Diffraction (XRD), Fourier transform infrared (FT-IR)and Field Emission Scanning Electron Microscope (FE-SEM). 5-fluorouracil (5-FU), a common anti CRC therapeutic drug, was loaded on CaCO3 nanoparticles. Then, the cytotoxicity of 5-FU alone and together with CaCO3 nanoparticles were evaluated on the murine colorectal cell line, CT-26, by MTT assay. The successful synthesis of CaCO3 nanoparticles was concluded owing to the crystallinity, purity of CaCO3 nanoparticles and the appearance of the characteristic vibrational bands attributed to the bending and stretching vibrations of CO32- in XRD pattern and FTIR spectrum respectively. Furthermore, after 5-FU loading on CaCO3 nanoparticles, absorption bands which belongs to this drug emerged in its FTIR spectrum. Additionally, FESEM observations revealed the synthesis of oval-shaped CaCO3 nanoparticles. The examination of the cytotoxicity of the drug-loaded nanoparticles on cancer cells showed that although free 5-FU has inhibitory effects on cancer cells with the IC50 value of 1.9±0.1 µg ml-1, the chemotherapeutic drug efficacy is improved when loaded on CaCO3 nanoparticles (IC50: 0.9±0.16 µg ml-1). Based on the findings of this study, 5-FUloaded CaCO3 nanoparticles could be considered as a promising candidate for colorectal cancer therapy.

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