Abstract

Nanoparticles can act on tumor cells at the nanoscale, causing biological therapeutic responses. In the current work, magnetic nanoparticles (MNPs) were obtained by means of a co-precipitation method and functionalized with dextran (D) and crocin, a saffron metabolite with potential antiproliferative properties. These MNPs were characterized using X-ray diffraction (XRD), transmission electron microscopy (TEM), field emission-scanning electron microscopy (FESEM), and Fourier transform infrared (FTIR) techniques. The crystalline structure of the functionalized MNPs was confirmed by XRD with a crystallite size of ca. 12 nm. The successful coating of MNPs surface with dextran and crocin was confirmed by FTIR spectroscopy. The functionalized MNPs were then used in order to elucidate their antiproliferative and apoptosis-inducing activities in the MCF-7 breast tumor cell line using the tetrazolium-based colorimetric (MTT) and Annexin V/PI flow cytometric assays, respectively. Real time-PCR analysis was used to determine the mRNA levels of VEGF as a marker of tumor angiogenesis. The antitumoral effects of crocin-coated D-MNPs were significantly higher than those of free crocin after 24 (P = 0.01) and 48 h (P < 0.0001) of incubation. Results of Annexin V/PI staining indicated that the rate of early apoptosis in MCF-7 cells treated with crocin-coated D-MNPs was higher than the cell fraction undergoing late apoptosis after 6 (P = 0.002), 12 (P < 0.0001), 24 (P < 0.0001), and 48 h (P < 0.0001) of incubation when compared to administration of free crocin. These results indicate that crocin-coated D-MNPs are a much successful drug nanocarrier with enhanced therapeutic effects than the free administration of the bioactive compound, crocin, becoming an attractive alternative option for the therapeutic use of this class of bioactive principles.

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