We designed and synthesized aminated mesoporous silica (MSN-NH2), and functionally grafted alginate oligosaccharides (AOS) on its surface to get MSN-NH2-AOS nanoparticles as a delivery vehicle for the fat-soluble model drug curcumin (Cur). Dynamic light scattering, thermogravimetric analysis, and X-ray photoelectron spectroscopy were used to characterize the structure and performance of MSN-NH2-AOS. The nano-MSN-NH2-AOS preparation process was optimized, and the drug loading and encapsulation efficiencies of nano-MSN-NH2-AOS were investigated. The encapsulation efficiency of the MSN-NH2-Cur-AOS nanoparticles was up to 91.24 ± 1.23%. The pH-sensitive AOS coating made the total release rate of Cur only 28.9 ± 1.6% under neutral conditions and 67.5 ± 1% under acidic conditions. According to the results of in vitro anti-tumor studies conducted by MTT and cellular uptake assays, the MSN-NH2-Cur-AOS nanoparticles were more easily absorbed by colon cancer cells than free Cur, achieving a high tumor cell targeting efficiency. Moreover, when the concentration of Cur reached 50 μg/mL, MSN-NH2-Cur-AOS nanoparticles showed strong cytotoxicity against tumor cells, indicating that MSN-NH2-AOS might be a promising tool as a novel fat-soluble anticancer drug carrier.