This article introduces a novel approach to deliver water-insoluble cancer drugs using PEGylated nano-graphene oxide (NGO). Graphene, a 2D material, has shown promise in various applications, but its use in biological systems has been limited. Here, researchers synthesized and functionalized nanoscale graphene oxide (NGO) sheets with branched, biocompatible polyethylene glycol (PEG) to enhance their solubility and stability in physiological solutions. This PEGylated NGO (NGO-PEG) demonstrated a unique ability to attach and deliver aromatic, water-insoluble drugs, such as SN38, a camptothecin (CPT) analog. SN38 is a potent topoisomerase I inhibitor, but its clinical use is hindered by its poor water solubility. The researchers showed that NGO-PEG could complex with SN38 via non-covalent van der Waals interactions, resulting in a highly soluble and potent drug complex. The NGO-PEG-SN38 complex exhibited excellent aqueous solubility and retained the high potency of free SN38. It was also more toxic than the FDA-approved SN38 prodrug, CPT-11, by 2-3 orders of magnitude. The researchers prepared graphene oxide by oxidizing graphite and then functionalized it with PEG to enhance its stability and prevent bio-fouling. The resulting NGO-PEG was stable in various biological solutions and showed efficient loading of SN38. The complex was found to be highly effective in killing cancer cells, with a much higher potency than CPT-11. The study also demonstrated the potential of NGO-PEG for delivering other water-insoluble drugs, highlighting its promise for biological applications. The biocompatible nature of PEGylated nanographene sheets makes them a promising material for drug delivery.This article introduces a novel approach to deliver water-insoluble cancer drugs using PEGylated nano-graphene oxide (NGO). Graphene, a 2D material, has shown promise in various applications, but its use in biological systems has been limited. Here, researchers synthesized and functionalized nanoscale graphene oxide (NGO) sheets with branched, biocompatible polyethylene glycol (PEG) to enhance their solubility and stability in physiological solutions. This PEGylated NGO (NGO-PEG) demonstrated a unique ability to attach and deliver aromatic, water-insoluble drugs, such as SN38, a camptothecin (CPT) analog. SN38 is a potent topoisomerase I inhibitor, but its clinical use is hindered by its poor water solubility. The researchers showed that NGO-PEG could complex with SN38 via non-covalent van der Waals interactions, resulting in a highly soluble and potent drug complex. The NGO-PEG-SN38 complex exhibited excellent aqueous solubility and retained the high potency of free SN38. It was also more toxic than the FDA-approved SN38 prodrug, CPT-11, by 2-3 orders of magnitude. The researchers prepared graphene oxide by oxidizing graphite and then functionalized it with PEG to enhance its stability and prevent bio-fouling. The resulting NGO-PEG was stable in various biological solutions and showed efficient loading of SN38. The complex was found to be highly effective in killing cancer cells, with a much higher potency than CPT-11. The study also demonstrated the potential of NGO-PEG for delivering other water-insoluble drugs, highlighting its promise for biological applications. The biocompatible nature of PEGylated nanographene sheets makes them a promising material for drug delivery.