摘要 : In the present study, the tannic acid-modified magnetic hydrotalcite-based MgAl nanoparticles (TA@HT@Fe3O4 NPs) were synthesized and assessed as a novel magnetic-targeted drug delivery system to the estrogen receptor (ER)-expressi... 展开 In the present study, the tannic acid-modified magnetic hydrotalcite-based MgAl nanoparticles (TA@HT@Fe3O4 NPs) were synthesized and assessed as a novel magnetic-targeted drug delivery system to the estrogen receptor (ER)-expressing colorectal cancer cells in vitro. In addition, FT-IR, EDS, DLS, and XRD measurements were employed for confirming the successful loading of doxorubicin (DOX), a widely-used chemotherapeutic agent, on the TA@HT@Fe3O4 NPs. The NPs exhibited a negative zeta potential value due to the presence of negatively charged molecules on their surface. The lading of DOX on the TA@HT@Fe3O4 NPs resulted in reducing their negative charge. TEM and FESEM images exhibited a layered HT structure with irregular edges and a mean size of 70 nm Fe3O4 NPs were visualized as small quasi-spherical particles with a uniform size of 12 nm. The TA@HT@Fe3O4 NPs had higher solubility at acidic pH than that at pH 7.4. Further, the entrapment efficiency of DOX in the TA@HT@Fe3O4 NPs was obtained about 51% at pH 7.4. The in vitro release of the DOX/ TA@HT@Fe3O4 NPs indicated a pH-dependent biphasic and sustained release of DOX as an initial rapid release in the first 24 h, followed by a 120-h sustained release. Furthermore, the safety and biocompatibility of the TA@HT@Fe3O4 NPs were confirmed through using hemolysis and MTT assays. Based on the results of fluorescence microscopy and flow cytometry, a higher DOX cellular uptake was observed in the ER-positive HCT116 and LoVo cells treated with the DOX/TA@HT@Fe3O4 NPs compared to the ER-negative HEK293 ones. Treatment with the DOX/TA@HT@Fe3O4 NPs led to more cytotoxicity than free DOX did and enhanced the DOX-induced reactive oxygen species (ROS) generation and subsequent apoptosis in colorectal cancer cells. Finally, applying a 0.6 T static magnetic field resulted in improving the anti-proliferative activity of the DOX/TA@HT@Fe3O4 NPs in HCT116 cells in a time exposure-dependent manner and enhancing ROS production. In general, the prepared NPs can serve as a promising candidate for the pH-responsive and magnetic-targeted delivery to the ER expressing cells. 收起