Breast cancer is a deadly disease that usually affects women. The nano‐drug delivery system's ligand‐functionalized nanoparticles have great cancer‐treatment potential. This study developed a potential method for drug loading and sustained release of breast cancer model medications 5‐fluorouracil (5‐FU) and Ganoderic acid (GA). CS/Apt/COQ NPs were produced. FT‐IR, XRD, DLS, zeta potentiometer, and SEM analyzed NP's chemical structure, particle size, and shape. In vitro MTT experiments examined MCF‐7 cell viability. Real‐time PCR quantified cell apoptosis. XRD and FTIR showed nanocarrier generation, crystalline structure, and molecular interactions. DLS indicated that nanocarriers contain 250.6 nm NPs with PDI 0.057. Zeta potential and SEM indicated their spherical shape and +37.8 mV surface charge. pH 5.4 released most 5‐FU and GA in 48 h. 5‐FU entrapment efficiency was 84.7 ± 5.2 and GA 80.2% ± 2.3. The 5‐FU‐GA‐CS‐CQD‐Apt group killed the most MCF‐7 cells, 57.9%. 5‐FU and GA in CS‐CQD‐Apt increased flow cytometry‐induced apoptosis. 5‐FU‐GA‐CS‐CQD‐Apt increased Caspase 9 and decreased Bcl2. Thus, pH‐sensitive NPs may release 5‐FU and GA to treat breast cancer.