Highly Stable, Coordinated Polymeric Nanoparticles Loading Copper(II) Diethyldithiocarbamate for Combinational Chemo/Chemodynamic Therapy of Cancer Xinyu Peng Qingqing Pan Boya Zhang Shiyu Wan Sai Li Kui Luo Yuji Pu Bin He 10.1021/acs.biomac.9b00367.s001 https://acs.figshare.com/articles/journal_contribution/Highly_Stable_Coordinated_Polymeric_Nanoparticles_Loading_Copper_II_Diethyldithiocarbamate_for_Combinational_Chemo_Chemodynamic_Therapy_of_Cancer/8204150 Disulfiram (DSF) has excellent <i>in vitro</i> anticancer activity in the presence of Cu­(II). The anticancer mechanism studies have demonstrated that copper­(II) diethyldithiocarbamate, Cu­(DDC)<sub>2</sub>, is the crucial DSF’s metabolite exhibiting anticancer activity. In this paper, highly stable polymeric nanoparticles were fabricated via a coordination strategy between Cu­(II) and carboxylic groups in poly­(ethylene glycol)-<i>b</i>-poly­(ester-carbonate) (PEC) for efficient loading of Cu­(DDC)<sub>2</sub>, which was generated by the <i>in situ</i> reaction of DSF and Cu­(II). The properties of nanoparticles such as drug loading contents, sizes, and morphologies could be tuned by varying the feeding ratios of DSF, Cu­(II), and PEC. These Cu­(II)/DDC-loaded nanoparticles showed excellent stability in both neutral and weak acidic solutions and under dilution. <i>In vitro</i> anticancer study established that Cu­(II)/DDC-loaded nanoparticles could enable a combination therapy of Cu­(DDC)<sub>2</sub>-based chemotherapy and chemodynamic therapy mediated by bioavailable Cu­(II) that was not in the form of Cu­(DDC)<sub>2</sub>. The <i>in vivo</i> antitumor results demonstrated that the Cu­(II)/DDC-loaded nanoparticles showed superior antitumor efficacy to DSF/Cu­(II). Our study provided a facile and effective strategy of highly stable coordination-mediated polymeric nanoparticles for combinational therapy of cancer. 2019-05-22 00:00:00 nanoparticle anticancer activity DSF vivo antitumor results PEC Cu anticancer mechanism studies drug loading contents