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However, unlike other traditional QDs, graphene quantum dots (GQDs), nanosized graphene sheets that possess edge effects and quantum confinement along with a collective structural feature of graphene, have shown less toxicity and desirable biocompatibility, making them an appropriate part of the carbon family for use in biomedical applications. This review article highlights the recent advances and roles of GQDs in healthcare, with a particular focus on their applications involving bioimaging and drug delivery. Furthermore, we provide an overview of the different synthesis methods for GQDs, including the top\u2010down and bottom\u2010up approaches, and discuss the modifications that enhance their functionality, such as the incorporation of heteroatoms (e.g., nitrogen, sulfur, and phosphorus) to improve their properties. 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