Nanotechnology-based therapeutics is an important tool in our armamentarium for improving efficacy and safety of cancer treatments. Key benefits from using nanotechnology-based therapeutics in cancer therapy accrue from improved drug solubility, stability, site-specificity and reduced multidrug resistance. Polymeric micelles, one of the several nanotechnology-based drug carriers, are an attractive and efficient approach to deliver poorly watersoluble anticancer drugs, improve drug stability and site-specificity leading to enhance therapeutic efficacy. The hydrophobic core functions as a repository for hydrophobic anticancer drugs. Stealth properties associated with the hydrophilic corona of polymeric micelles prevent opsonization by the reticuloendothelial system (RES) and hence reduces elimination of micelles from the bloodstream resulting in increased circulation times. Also, the small size ensures selective distribution to tumor cells via the enhanced permeability and retention (EPR) effect.