Mitochondria are the fulcrum for regulating cellular metabolism as well as apoptosis. The multi-lamellar vesicles (MLVs) liposome targeted against mitochondria can be formulated to disrupt mitochondrial integrity to attain programmed cell death of cancer stem cells (CSCs). The gold nanoparticles (GNPs) and a steroid nucleus (cyclopentanoperhydrophenanthrene ring) are encapsulated within MLV liposome that targets specifically to the CD44 receptor of the CSCs. Entering cytosol, it would bind distinctively to the malate-aspartate shuttle through a specifically designed ligand. Liposome fuses with the mito-membrane after associating with shuttle, thereby releasing both the components. The steroid disrupts mito-membrane's integrity facilitating release of cytochrome c. Thus, GNPs enter into the mitosol and interact with the mitochondrial complexes to cease cellular respiration. Since the solid nano-based pharmaceutics has shown a lot of promises as a potent anticancer therapy, the role of MLV liposome can be proved to be a better weapon to terminate malignancy. © 2013 Springer Science+Business Media New York.