The mesoporous silica nanoparticle (MSN) is a promising carrier as a drug-delivery system. And transferrin has been known as a ligand which binds to a receptor expressed on the surface of most proliferating cells such as tumor cells. In order to further improve the tumor delivery of MSN carrier, transferrin- conjugated MSNs were synthesized and evaluated as a targeting carrier. Fourier transform near infrared data revealed a conjugation of transferrin with MSN, while zeta potential and transmission electron microscopy results showed the nano-characteristics of the MSN in detail. To confirm the optimal conditions for drug encapsulation onto the MSN, two types of dyes (hydrophilic rhodamine B and hydrophobic 5,6-carboxyfluorescein) were loaded. Then, the differences in loading efficiencies and release properties of these dyeloaded MSNs were tested. The cellular uptake of dye-loaded MSNs was greater than dye solution. More importantly, the cellular uptake of transferrin modified MSNs was enhanced in the transferrin receptor-expressing Jurkat cells but not in normal cells. Therefore, these results suggest that transferrin-modified MSN could be applied for therapeutic purposes as a drug-delivery system for targeting specific cancer cells.