Mitochondrion, the energy generating organelle of the cell, is a subject of interest for selective targeting of therapeutic molecules, both Drugs and DNA, since it is found to be involved in numerous disorders like diabetes, neurodegenerative disease and cancer etc. Mitochondrial therapy can be made possible if the bioactive molecule is selectively delivered to the mitochondria of correct cell type, using cell specific ligands and mitochondriotropic molecules in designing of cell selective mitochondria specific carrier system. In this present review we will elaborate the role of mitochondria in human disease, cell specific ligands, mitochondriotropic molecules and their utilization in construction of such cell selective and mitochondria specific delivery systems that will make mitochondrial medicine practically possible.