Increasing efforts are being put into the light-sensitive polymeric micelles that hold great potential for drug/gene/small interfering RNA delivery. However, these polymeric micelles lack highly efficient tumor-targeting properties and near-infrared light sensitivity, and often exhibit an uncontrollable drug-release profile. To address these problems, a new strategy is introduced that combines sugar-triggered targeting (active targeting) and two-photon sensitivity to afford a degradable and dendritic micellar nanocarrier, in which the desired sugar residues and light-responsive groups can be modularly conjugated and/or altered. A clinical anticancer drug, doxorubicin, can be released in a controlled manner by changing the light irradiation time, which is induced by the gradual disruption of micelles in aqueous solution. The glucose- and lactose-coated micelles further demonstrate specific binding with the lectins Concanavalin A and Ricinus communis agglutinin, respectively, which makes them useful as targeted drug-delivery vesicles.