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Advances in molecular medicines have led to identification of promising targets on cellular and molecular levels. These targets are located in extracellular and intracellular compartments. The latter include cytosol, nucleus, mitochondrion, Golgi apparatus and endoplasmic reticulum. This report gives an overview on the barriers to delivering nanomedicines to various target sites within a solid tumor, the experimental approaches to overcome such barriers, and the potential utility of nanotechnology.