<p>Nanotechnology has opened new horizons in the treatment of diseases by providing a suitable platform for the production of novel drugs and creating the potential for new pharmaceutical interactions. The importance of nanotechnology in targeted drug delivery is clearly evident in its ability to increase the precision, efficacy, and safety of treatments, which ultimately improves the quality of life of patients. <i>Moringa oleifera</i> Lam. contains significant biological compounds that are highly valued due to their anticancer and antioxidant properties. Consequently, the use of nanoparticles for the targeted delivery of medicinal compounds from the Moringa plant can enhance its efficacy and therapeutic properties. In this study, we investigated the effectiveness of polylactic acid (PLA)-polyethylene glycol (PEG)-folic acid (FA)/chitosan-PLA polymeric nanoparticles for the targeted delivery of aqueous extracts from <i>M. oleifera</i> plant tissue and callus and their effects on the growth and survival of the MCF-7 and BT-549 cell lines. The solvent evaporation method was used to prepare the PLA-PEG-FA/PLA-chitosan copolymer nanoparticles, and the physicochemical properties of the nanoparticles were evaluated. After the aqueous extract of the moringa plant, its callus extract, and pure quercetin in the copolymer nanoparticles were encapsulated, their release rates were assessed at 2 different pH values, 5 and 7.4. Finally, the cytotoxicity and IC₅₀ values of the nanoparticles, as well as their efficacy in the targeted delivery of pharmaceutical compounds under in vitro conditions and the level of apoptosis in the mentioned cell lines, were examined via flow cytometry. It was also determined that the synthesized PLA-PEG-FA/PLA-chitosan nanoparticles had a spherical shape with an average size of 230 ± 0.92 nm, a zeta potential of 6.4 ± 0.82 mV, and a PDI value of 0.38 ± 0.12. Spectrophotometric evaluation revealed that drug release was greater at acidic pH values. A water-soluble tetrazolium salt (WST-1) assay revealed the biocompatibility of the drug carriers and their low toxicity. Furthermore, the highest percentage of pre- and postapoptotic cells in the BT-549 cell line treated with PLA-PEG-FA/chitosan-PLA/quercetin nanoparticles was observed (31.2% and 7.15%, respectively). It was concluded that the PLA-chitosan copolymer nanoparticles and PLA-PEG-FA/chitosan-PLA have a high ability for the targeted delivery of quercetin, an anticancer compound found in the aqueous extract of moringa (from plant tissue and callus), to cancer cells.</p> Graphical Abstract <p></p>