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      PEGylated nanographene oxide for delivery of water-insoluble cancer drugs.

      Journal of the American Chemical Society

      Antineoplastic Agents, chemical synthesis, chemistry, pharmacology, Camptothecin, analogs & derivatives, Carbon, pharmacokinetics, Cell Line, Tumor, Cell Proliferation, drug effects, Cell Survival, Dose-Response Relationship, Drug, Drug Carriers, Drug Delivery Systems, methods, Drug Screening Assays, Antitumor, Humans, Molecular Structure, Nanostructures, Oxides, Particle Size, Polyethylene Glycols, Solubility, Surface Properties, Water

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          Abstract

          It is known that many potent, often aromatic drugs are water insoluble, which has hampered their use for disease treatment. In this work, we functionalized nanographene oxide (NGO), a novel graphitic material, with branched polyethylene glycol (PEG) to obtain a biocompatible NGO-PEG conjugate stable in various biological solutions, and used them for attaching hydrophobic aromatic molecules including a camptothecin (CPT) analogue, SN38, noncovalently via pi-pi stacking. The resulting NGO-PEG-SN38 complex exhibited excellent water solubility while maintaining its high cancer cell killing potency similar to that of the free SN38 molecules in organic solvents. The efficacy of NGO-PEG-SN38 was far higher than that of irinotecan (CPT-11), a FDA-approved water soluble SN38 prodrug used for the treatment of colon cancer. Our results showed that graphene is a novel class of material promising for biological applications including future in vivo cancer treatment with various aromatic, low-solubility drugs.

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          Author and article information

          Journal
          18661992
          2597374
          10.1021/ja803688x

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