A multifunctional dendritic nanodevice containing folate (FA) as the targeting molecule and daunorubicin (DNR) as the chemotherapeutic drug has been designed and synthesized. The primary amino groups on the surface of the generation 5 poly(amidoamine) dendrimer (G5 dendrimer) were acetylated partially. FA and DNR were conjugated to the remaining primary amino groups on the G5 dendrimer through amide and ester linkage, respectively, to generate the difunctional dendritic device. The synthetic approach of G5 PAMAM dendrimer containing daunorubicin and folic acid would be useful for targeting the overexpressed membrance-associated folate receptors of KB human carcinoma cell line and discreating them effectively.