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Future of nanotherapeutics: Targeting the cellular sub-organelles. Ma Xiaowei,Gong Ningqiang,Zhong Lin,Sun Jiadong,Liang Xing-Jie Biomaterials Many diseases originate from alterations at nanoscale levels. Precise drug delivery should be achieved not only at cell level, but also at organelle level to achieve maximum therapeutic responses as well as avoiding possible toxic side effects of the drugs. However, organelles and subcellular structures are natural barriers that hampering many therapeutics from taking effects. Nanodelivery vehicle is a favorable platform to navigate across physiological barriers and to achieve selective delivery of therapeutic and diagnostic agents to intracellular targets. In this review, we have highlighted recent innovations in organelle-targeted nanomaterials designed to treat a variety of currently challenging diseases. Targeting strategies of four main kinds of organelles: mitochondria, nucleus, lysosomes and endoplasmic reticulum are discussed in detail. This review will help to clarify the intracellular nanomaterial-organelle interactions, and understand the fundamentals of organelle-targeted drug delivery strategies, which is of vital importance for the design and successful biomedical applications of nanomaterials in therapeutic treatments. At the end of this review, challenge and perspectives of organelle-targeted nanotherapy are discussed. 10.1016/j.biomaterials.2016.04.026