An amphiphilic drug-drug nanoparticle for reversing platinum-based anticancer drug resistance in cancer therapy, which is formed through coordination of a histone deacetylase inhibitor with a platinum-based antitumor agent and self-assembly in water. After entering tumor cells, the amphiphilic drug-drug nanoparticle can hydrolyze to release two drug agents. The amphiphilic complex can self-assemble into nanoparticles in water without any carriers, and the complex can realize drug delivery by itself. At the meantime, the amphiphilic drug-drug nanoparticle can effectively enter tumor cells, reduce the blocking effect of sulfur-containing ligands in blood on cisplatin, and decrease the toxic and side effects towards normal cells. It can also be hydrolyzed to release the histone deacetylase inhibitor and platinum-based antitumor active agents, thereby achieving the synergistic effect for reversing platinum-based drug resistance in cancer therapy and the purpose of cancer treatment.
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