In recent years, stimuli-responsive drug delivery systems based on pH, particularly those developed using bio-derived nanocomposite systems, have gained significant attention. In this work, a novel magnetic carrier was designed based on biopolymeric chitosan and metal-organic framework (MOF) for pH-controlling the release of anticancer drugs. To end this, an in-situ green method was performed to form Cu-based MOF in the presence of a magnetic polysaccharide synthesized by precipitation method toward the construction of CS/Fe3O4/Cu-MOF nanocomposite. The nanocomposite was immersed in an aqueous solution of a model anticancer drug, doxorubicin (DOX), and a higher loading capacity (90.1 ± 0.5 %) was achieved. The in-vitro drug release study showed low release rates in simulated physiological environments (pH 7.4, 37 °C, lower than about 20 %), but higher release rates in tumor tissue conditions (pH 4.5, 41 °C, higher than about 60 %) over 96 h, allowing for sustained and extended delivery of DOX. Additionally, the MTT assay demonstrated that the blank and DOX-loaded CS/Fe3O4/Cu-MOF had good cytocompatibility (over 80 % cell viability) and considerable cytotoxicity (lower than 40 % at 16 μg/mL) toward breast cancer (MCF-7) cell line, respectively. These results indicated that the synthesized nanocomposite with suitable pH-sensitivity has potential as a targeted anticancer agent.