To achieve highly effective treatment to diseases, successful delivery of drugs with a carrier into

the specific organelles (nucleus, mitochondria, lysosomes, etc.) is of great importance. Targeted

delivery based on nanoparticle (NP)-based drug delivery systems (NDDSs) is mainly focused on

cell-membrane targeting. In this review we summarize researches on organelle-specific drug

delivery with multifunctional NPs. Many effective strategies are introduced for functionalizing

these NPs by altering their chemical composition or by grafting functional groups onto their

surface for improving organelle-targeting ability. Only when the concentration of released drugs

becomes high enough will they interact with molecular targets on specific organelles to induce