Today Cancer still remains a major cause of mortality and death worldwide, in humans. Chemotherapy a key treatment strategy have major obstacles is the recurrence of chemo- resistance in cancer, which is inherent unresponsiveness or acquired upon exposure to chemotherapeutics. 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 failure of chemo- therapeutics. MDR is primarily based on the over-expression of drug efflux pumps in the cellular membrane, which belong to the ATP-binding cassette (ABC) superfamily of proteins, are Pgp (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 limitation of MDR and various advantages of the present medical science nanotechnology with intracellular delivery aspects for overcoming significant potential for improving the treatment of MDR malignancies.
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