Introduction: This review aimed to assess the potential use of poly(ethylene glycol)– poly(lactic-co-glycolic acid) (PEG-PLGA) nanoparticles in targeted tumor therapy, specifically focusing on their potential to overcome the limitations of traditional anticancer drug delivery systems, such as drug resistance, lack of tumor selectivity, and systemic toxicity. Methods: The PRISMA 2020 guidelines were used for this systematic literature review. The Pub- Med/MEDLINE, Scopus, Web of Science, and ScienceDirect databases were searched for scientific literature published between 2010 and 2025. We analyzed, selected, and critically assessed papers related to the composition, targeting, pharmacokinetic optimization, and therapeutic efficacy of PEG-PLGA nanoparticles in cancer therapy. Results: The results indicate that PEG-PLGA nanoparticles have the potential to significantly improve the pharmacokinetics, bioavailability, and therapeutic efficacy of bioactive phytoconstituents, gene therapies, and anticancer drugs. Enhanced tumor accumulation and reduced off-target toxicity were achieved through both passive targeting strategies utilizing the enhanced permeability and retention (EPR) effect and active targeting strategies using ligands such as hyaluronic acid, peptides, aptamers, folate, and transferrin. Discussion: The results illustrate the versatility of PEG-PLGA nanoparticles as multi-purpose nanocarriers in cancer therapy. The challenges of large-scale production, stability, immunogenicity, chronic administration, and translational feasibility remain important hurdles for their successful translation into clinical practice, despite the promising preclinical results. Conclusion: The biocompatibility, targeting ability, and versatility of PEG-PLGA nanoparticles make them a promising nanoscale platform for tailored and targeted therapy. It is expected that further advances in nanocarrier technology would increase their therapeutic utility in tailored tumor therapy, despite the existing translational hurdles.
Shahu et al. (Tue,) studied this question.