Today Cancer still remains a major cause of mortality and death worldwide, in humans.
Chemotherapy, a key treatment strategy in cancer, has significant hurdles such as the occurrence of
chemoresistance in cancer, which is inherent unresponsiveness or acquired upon exposure to chemotherapeutics.
The resistance of cancer cells to an antineoplastic agent accompanied to other chemotherapeutic
drugs with different structures and mechanisms of action called multi-drug resistance
(MDR) plays an important role in the failure of chemo- therapeutics. MDR is primarily based on the
overexpression of drug efflux pumps in the cellular membrane, which belongs to the ATP-binding cassette
(ABC) superfamily of proteins, are P-gp (P-glycoprotein) and multidrug resistance-associated
protein (MRP). Over the years, various strategies have been evaluated to overcome MDR, based not only
on the use of MDR modulators but also on the implementation an innovative approach and advanced
nanosized drug delivery systems. Nanomedicine is an emerging tool of chemotherapy that focuses on alternative
drug delivery for improvement of the treatment efficacy and reducing side effects to normal tissues.
This review aims to focus on the details biology, reversal strategies option with the limitation of
MDR and various advantages of the present medical science nanotechnology with intracellular delivery
aspects for overcoming the significant potential for improving the treatment of MDR malignancies.