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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Authors | Zhuang Liu, Joshua T Robinson, Xiaoming Sun, Hongjie Dai |
Journal | Journal of the American Chemical Society
(J Am Chem Soc)
Vol. 130
Issue 33
Pg. 10876-7
(Aug 20 2008)
ISSN: 1520-5126 [Electronic] United States |
PMID | 18661992
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Drug Carriers
- Oxides
- Water
- Polyethylene Glycols
- Carbon
- Irinotecan
- Camptothecin
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Topics |
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology)
- Camptothecin
(analogs & derivatives, chemistry, pharmacology)
- Carbon
(chemistry, pharmacokinetics)
- Cell Line, Tumor
- Cell Proliferation
(drug effects)
- Cell Survival
(drug effects)
- Dose-Response Relationship, Drug
- Drug Carriers
(chemical synthesis, chemistry, pharmacokinetics)
- Drug Delivery Systems
(methods)
- Drug Screening Assays, Antitumor
- Humans
- Irinotecan
- Molecular Structure
- Nanostructures
(chemistry)
- Oxides
(chemistry, pharmacokinetics)
- Particle Size
- Polyethylene Glycols
(chemistry, pharmacokinetics)
- Solubility
- Surface Properties
- Water
(chemistry)
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