Metal-organic frameworks, such as MIL-100, have been recently introduced as promising drug carriers due to their notable characteristics such as stability, biocompatibility and owning large porosity which may admit a broad range of drugs with different molecular sizes. In this study, we firstly proposed an accessible top-down approach using ultrasound method to prepare nanoMIL-100 and secondly, evaluated its potentials as an anticancer nanocarrier. This is the first report that docetaxel (DTX) as a highly hydrophobic anticancer drug was encapsulated in nanoMIL-100 with the drug payload of 57.2 wt%. Characterizations of the prepared nanoMIL-100 and DTX-loaded nanoMIL-100 were performed by PXRD, FT-IR, N adsorption, DLS and FE-SEM. Moreover, the drug loading and release processes were quantified by HPLC. The in vitro release of DTX from the prepared nanocarrier was investigated in two pH values, 7.4 and 5.5. The toxic effect of DTX-loaded nanoMIL-100 was examined on human breast cancer cell line, MCF-7, and a significant decrease was observed in IC value (0.198 μg/mL) at the first 24 h in comparison with the free drug (4.9908 μg/mL). This nanocarrier may, thus offer promising potentials as a novel cytotoxic drug delivery system.