Polycarbonate microspheres containing mitomycin C and magnetic powders as potential hepatic carcinoma therapeutics

The polycarbonate copolymer poly(trimethylene carbonate-co-5,5-dimethyl trimethylene carbonate) (P(TMC-co-DTC)) was synthesized by the polymerization of trimethylene carbonate (TMC) and 5,5-dimethyl trimethylene carbonate (DTC) using tin (II) 2-ethylhexanoate [Sn(Oct)2] as a catalyst. In vitro degradation tests indicated this polycarbonate copolymer degraded slowly in phosphate buffer saline solution (PBS, 0.1 mol/L, at 37 °C). Magnetic polymer microspheres (MMC-PC-M) generated from the P(TMC-co-DTC) copolymer and containing Fe3O4 magnetic ultrafine powders and an anticancer drug, mitomycin C (MMC) were prepared by a solvent evaporation technique. These anticancer magnetic polycarbonate microspheres showed strong magnetic responsiveness and high MMC loading capacity. In vitro drug release studies indicated that these microspheres sustained steady release rates of MMC in PBS. In vitro cytotoxicity assays demonstrated the microspheres were strongly inhibitory to human hepatic carcinoma (Bel-7204) cells. In vivo site-specific therapy in nude mice with human hepatic carcinoma indicated that the microspheres possessed markedly high antitumor activity against human hepatic carcinoma (Bel-7204).

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► Polycarbonate magnetic microspheres containing mitomycin C and Fe3O4 magnetic ultrafine powders as tumor-targeting delivery system.
► A magnet field applied outside the organ drives the accumulation of the microspheres into localized tumors.
► Sustain steady drug release of the microspheres enhances drug efficacy.
► The microspheres possess markedly high antitumor activity against human hepatic carcinoma (Bel-7204) in vivo and in vitro.