Gold-doxorubicin nanoconjugates for overcoming multidrug resistance

Multidrug resistance (MDR) is a major clinical obstacle to the success of cancer chemotherapy. Here we developed a gold-doxorubicin (DOX) nanoconjugates system to overcome MDR. Gold nanoparticles (AuNPs) were first PEGylated as Au-PEG-NH2, and DOX was then grafted onto AuNPs via a cleavable disulfide linkage (Au-PEG-SS-DOX). Confocal images revealed that the extent of intracellular uptake of Au-PEG-SS-DOX was greater than that of free DOX in the MDR cells, and inductively coupled plasma mass spectroscopy analysis further confirmed that AuNPs significantly increased the level of drug accumulation in MDR cells at a nanoparticles dose greater than 15 μM. The cytotoxicity study demonstrated that the Au-PEG-SS-DOX nanoconjugates system efficiently released the anticancer drug DOX and enhanced its cytotoxicity against MDR cancer cells. This study highlights the potential of using AuNPs for overcoming of MDR in cancer chemotherapy.From the Clinical EditorThis study demonstrates that gold nanoparticles can be successfully applied to overcome MDR in cancer chemotherapy.

Graphical AbstractGold-doxorubicin nanoconjugates were developed by grafting doxorubicin (DOX) onto polyethylene glycol (PEG)-modified gold (Au) nanoparticles (Au-NPs) via cleavable disulfide (SS) linkage. The Au-PEG-SS-DOX nanoconjugates exhibited higher intracellular uptake and greatly enhanced cytotoxicity for multidrug-resistant cells HepG2-R compared to free DOX. This study highlights the potential of using Au-NPs for overcoming multidrug resistance in cancer chemotherapy.Figure optionsDownload high-quality image (174 K)Download as PowerPoint slide