<p> Dendrimers are nanoscale-building blocks, have attracted avid interest of researchers across the globe on account of their well-defined size and derivatisable terminal groups. In this, surface modification of dendrimer is considered in order to solve some issues like drug resistance, in cancer-targeted research. Thus, developed the ferulic acid (FA)-conjugated 4.0 G PAMAM dendrimer for targeted and antioxidant therapy for breast cancer. The ferulic acid (FA) was conjugated with 4.0 G PAMAM dendrimer by divergent growth method and characterized analytically (<i>λ</i>_max, FTIR, and NMR). Hemolysis as well as cytotoxicity studies of dendrimer conjugates were carried out against rat RBC and MCF-7 cell lines, respectively. <i>In vivo</i> anticancer activity is performed in 4T1 tumor-grafted female Balb/c mice model. FTIR represents appearance, disappearance, and then reappearance of peaks which proof the progress of reaction and conjugation. The NMR spectra and chemical shift value of conjugated dendrimer as compared to plain dendrimer provide the proof of conjugation of FA with 4.0 G PAMAM dendrimer. Hemolytic data indicate that conjugation reduces heamolysis of 4.0 G PAMAM dendrimers while cytotoxicity data revealed that conjugate acts synergistically against MCF-7 cell lines and IC₅₀ values were found to be 15&#xa0;μg/mL for 4.0G PAMAM-FA Conjugate. The increased potency of the PAMAM-FA conjugate relative to FA alone suggests the delivery or efficacy of FA in targeting cancer cells. <i>In vivo</i> anticancer results indicated that tumor growth proliferation rates (around 24 ± 2%) were reduced in FA-conjugated 4.0 G PAMAM dendrimer, and tumor growth was significantly slower around 198mm³, after 28&#xa0;days. As a result, developed FA-conjugated 4.0 G PAMAM dendrimer can be applied as potential carrier for delivery of FA as chemotherapeutics at tumor site.</p> Graphical abstract <p></p>