 Different mechanisms in cancer cells become resistant to one or more chemotherapeutics due to multi-drug resistance, MDR. This hinders chemotherapy efficacy. Factors contributing to MDR include enhanced drug detoxification, decreased drug uptake, increased intracellular nucleophiles levels, enhanced repair of drug-induced DNA damage, over expression of drug transporters such as P-glycoprotein, PGP, multi-drug resistance associated proteins, MRP1, MRP2, and breast cancer resistance protein, BCRP. Currently, nano-assemblies such as polymeric slash solid lipid slash inorganic slash metal nanoparticles, quantum dots, dendrimers, liposomes, micelles have emerged as an innovative, effective and promising platforms for treatment of drug-resistant cancer cells. Nanocarriers have potential to improve drug therapeutic index, ability for multifunctionality, divert ABC transporter mediated drug e-flux mechanism and selective targeting to tumor cells, cancer stem cells, tumor initiating cells or cancer microenvironment. Select. This article was authored by Sonali Ekap's mystery, Theramanlai Govinder, Rohit Ishervastava, and others.