Abstract Ferrocene-containing amphiphilic block copolymers, poly(2-acryloyloxyethyl ferrocenecarboxylate)-block-poly(2-(dimethylamino) ethyl methacrylate) (PAEFc-b-PDMAEMA), were synthesized via sequential ATRP, and self-assembled into globular nanoscaled micelle aggregates. The copolymer micelles exhibited reversible redox on-off switch feature, which was mediated by using H2O2, KMnO4, NaClO and FeCl3 as a model of oxidants and ascorbic acid as a model of reductants. The micelle nanoparticles were used to load and deliver anticancer drug, 10-hydroxycamptothecine, finding that the encapsulated drug was rapidly delivered by selectively responding to redox environments in cancer cells. MTT assays were performed to uncover cytotoxicity of the developed copolymer micelles and potentiality used for cancer therapy.