Abstract

Targeted drug delivery systems have been developed as a promising strategy for targeted delivery of the drugs, genes, and biomolecules to the target tissue. In this study, a drug delivery system based on layered double hydroxide (LDH), as a carrier, and galactose (Gal), as a ligand, was designed for targeted delivery of curcumin (Cur) to hepatocellular carcinoma cells. Gal was conjugated onto Cur/LDH nanohybrid using SiO2 nanodot-coating and amine-functionalization strategy to fabricate a Gal-Cur/LDH delivery system. The physicochemical properties were determined using field emission scanning electron microscopy (FESEM), and transmission electron microscopy (TEM), zeta potential, Fourier transform infrared spectrometry (FTIR) and X-ray powder diffraction (XRD). The cell viability, cellular uptake, and apoptotic effects of the Gal-Cur/LDH nanoparticles for human hepatocellular carcinoma cell line (HepG2 cells) were evaluated. Additionally, in the cell viability test, to investigate the specific targeting efficiency of Gal-Cur/LDH nanoparticles into hepatoma cells, Murine fibrosarcoma L929 cells were utilized as control cells for studying the specific targeting efficiency of Gal-Cur/LDH nanoparticles for HepG2 cells. Results demonstrated the successful synthesis of LDH and the intercalation of Cur in LDH with 31.0 ± 0.0% loading efficiency. According to the cyto assay results, LDH did not significantly induce cytotoxicity in both L929 and HepG2 cells. Gal-Cur/LDH nanoparticles showed higher cytotoxicity effects against HepG2 cells than L929 cells, compared with free Cur and Cur/LDH nanohybrid. Additionally, Gal-Cur/LDH nanoparticles significantly exhibited a higher rate of apoptosis than the other groups, which might be attributed to higher cellular uptake efficiency via ASGP-receptors in HepG2 cells surface. Our findings suggest the Gal-Cur/LDH nanoparticles as an excellent carrier system for targeted delivery of Cur to the hepatocellular carcinoma cells.

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