Trends in the development of modern medicine necessitate the efficient delivery of therapeutics to achieve the desired treatment outcomes through precise spatiotemporal accumulation of therapeutics at the disease site. Bioresponsive nanomedicine is a promising platform for this purpose. Dynamic covalent bonds (DCBs) have attracted much attention in studies of the fabrication of bioresponsive nanomedicines with an abundance of combinations of therapeutic modules and carrier function units. DCB-based nanomedicines could be designed to maintain biological friendly synthesis and site-specific release for optimal therapeutic effects, allowing the complex to retain an integrated structure before accumulating at the disease site, but disassembling into individual active components without compromising function in the targeted organs or tissues. In this review, we focus on responsive nanomedicines containing dynamic chemical bonds that can be cleaved by various specific stimuli, enabling achievement of targeted drug release for optimal therapy in various diseases.