Targeted delivery via surface receptors can signi cantly improve the therapeutic e cacy and reduce the adverse drug reactions. The protein nanocarrier system offers many advantages, such as encapsulation in various drugs and molecules and prolonged circulation. Here, the folate receptor-targeted folic acidconjugated retinoic acid-loaded glutenin nanoparticles (FA-RA-Glu NPs) were successfully synthesised for enhanced delivery of retinoic acid to breast cancer cells (MCF-7). After a complete physico-chemical characterisation of FA-RA-Glu NPs, stability, drug release, release kinetics, cytotoxicity, apoptosis, cell death, and nucleic acid fragmentation were analysed. The results showed that FA-RA-Glu NPs were 185 nm in size, predominantly spherical in shape, crystalline in nature and had a zeta potential of − 3 mV. The RA encapsulation e ciency and loading capacity of Glu NPs were 83.537% ± 3.32% and 9.917 ± 1.68%, respectively. The effects of FA-RA-Glu NPs against MCF-7 cells signi cantly reduced the number of viable cells and the induction of apoptosis. The cellular uptake study showed that the FA-RA-Glu NPs had facilitated endocytosis and delivered RA into MCF-7 cells. After treatment with FA-RA-Glu NPs, contracted nuclei and deformed membrane bodies were observed as typical apoptotic morphological changes. The released RA also targeted the mitochondria of MCF-7 cells, which signi cantly increased the levels of reactive oxygen species and contributed to the damage of mitochondrial membrane integrity. These results suggest that FA-RA-Glu NPs with facilitated endocytosis and targeted delivery of RA into MCF-7 cells may have signi cant therapeutic potential for the treatment of breast cancer.