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

PEGylated nanographene oxide for delivery of water-insoluble cancer drugs.
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DOI:
10.1021/ja803688x
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发表时间:
2008-08-20
影响因子:
15
通讯作者:
Dai, Hongjie
Dai, Hongjie
中科院分区:
化学1区
文献类型:
--
作者:
Liu, Zhuang;Robinson, Joshua T.;Sun, Xiaoming;Dai, Hongjie

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众所周知,许多有效的芳香药物是不溶于水的,这阻碍了它们用于疾病治疗。在这项工作中,我们功能化纳米氧化石墨烯(NGO),一种新型的石墨材料,与支化聚乙二醇(PEG),以获得生物相容性NGO-PEG共轭物稳定在各种生物溶液中,并使用它们连接疏水性芳香族分子,包括喜树碱(CPT)类似物,SN 38通过π-π堆积非共价。所得的NGO-PEG-SN 38复合物表现出优异的水溶性,同时保持其与有机溶剂中的游离SN 38分子类似的高癌细胞杀伤效力。NGO-PEG-SN 38的功效远高于伊立替康(CPT-11),伊立替康是FDA批准的用于治疗结肠癌的水溶性SN 38前药。我们的研究结果表明,石墨烯是一类新型材料,有望用于生物应用,包括未来用各种芳香族低溶解度药物进行体内癌症治疗。
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 nano-graphene 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) analog, SN38 non-covalently via π-π 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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