Nanoparticulate-based drug carriers have been developed to overcome the problems of conventional anticancer
pharmacotherapy, i.e., the little specificity and low accumulation of the drug into the tumor interstitium, and the extensive biodistribution
leading to severe toxicity. Unfortunately, conventional nanoparticles have been demonstrated to merely accumulate the loaded drug into
organs associated to the reticuloendothelial system, e.g., the liver. Recently, drug delivery strategies involving the use of nanoplatforms
surface decorated with unique biomolecules have demonstrated their potential in concentrating the chemotherapy agent specifically into
the malignant cells. This review will be focused on the analysis of the current state of the art and future perspectives of such passive and
active targeting strategies based on the enhanced permeability and retention effect and on a ligand-mediated transport, respectively.
Special attention will be given to the use of these surface functionalized nanocarriers to overcome multi-drug resistances in cancer cells.
Keywords: Active drug targeting, cancer, EPR effect, ligand-mediated delivery, multi-drug resistance, nanoparticle, passive drug targeting, Nanoparticulate-based, conventional anticancer, pharmacotherapy
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