Abstract
Photodynamic therapy (PDT) is an effective approach for inducing tumor cell death through reactive oxygen species (ROS) generated by light-activated photosensitizers (PSs). Despite its selectivity in tumor treatment, PDT still faces significant challenges in targeting deep-seated tumors due to limitations in tissue penetration and precise localization. Graphene-based nanomaterials, such as graphene oxide (GO), reduced graphene oxide (rGO), graphene quantum dots (GQDs), and graphene nanosheets (GNS), offer innovative solutions by enhancing light penetration, boosting PS activity, and improving tumor-targeting precision. This review highlights how graphene-based nanomaterials address these challenges through functionalization strategies, including receptor-mediated tumor targeting, size-dependent penetration, optical synergy, and hypoxia modulation. Additionally, it explores the synthesis and production challenges associated with these materials. Focusing on four key graphene derivatives-GO, rGO, GQDs, and GNS-this article examines how reaction conditions, catalyst types, and precursor purity influence their structural properties and functional performance in PDT. To facilitate the translation from laboratory research to clinical application, strategies for scaling up production are discussed, emphasizing the need to simplify synthesis processes and improve efficiency for broader biomedical use. This review provides valuable insights into advancing graphene-based nanomaterials for clinical PDT applications, bridging the gap between nanomaterial design and therapeutic precision.