Amphiphilic Rhomboidal Organoplatinum(II) Metallacycles with Encapsulated Doxorubicin for Synergistic Cancer Therapy.

Synergistic therapy with nanocarriers is a promising strategy for effective cancer treatment. Here, we synthesized an amphiphilic rhomboidal metallacycle M, in which a glucose-modified pyridine ligand was used to improve water-solubility and an organoplatinum(II) receptor acted as a platinum-based anticancer agent. Moreover, because of the amphiphilic properties, M self-assembled into micelles or nanobelts at different concentrations, and a drug delivery system (DDS) was developed by encapsulating the anticancer drug doxorubicin (DOX) into the micelles. The morphology, cell uptake, cytotoxicity, internalization, and antitumor effect of the DDS were investigated. Under low intracellular pH conditions, the DDS disassembled to release the loaded DOX in situ. The designed DDS exhibited good biocompatibility, synergistic antitumor efficacy, and negligible adverse effects in a U87 tumor-bearing mice model.