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功能化氧化石墨烯作为纳米载体,用于混合抗癌药物的控制加载和靶向递送。

Functional graphene oxide as a nanocarrier for controlled loading and targeted delivery of mixed anticancer drugs.

机构信息

Suzhou Institute of Nano-tech and Nano-bionics, Chinese Academy of Sciences, 398 Ruoshui Road, Dushu Lake Higher Education Town, Suzhou Industrial Park, Suzhou 215125, P. R. China.

出版信息

Small. 2010 Feb 22;6(4):537-44. doi: 10.1002/smll.200901680.

Abstract

A simple synthetic route for the preparation of functional nanoscale graphene oxide (NGO), a novel nanocarrier for the loading and targeted delivery of anticancer drugs, is reported. The NGO is functionalized with sulfonic acid groups, which render it stable in physiological solution, followed by covalent binding of folic acid (FA) molecules to the NGO, thus allowing it to specifically target MCF-7 cells, human breast cancer cells with FA receptors. Furthermore, controlled loading of two anticancer drugs, doxorubicin (DOX) and camptothecin (CPT), onto the FA-conjugated NGO (FA-NGO) via pi-pi stacking and hydrophobic interactions is investigated. It is demonstrated that FA-NGO loaded with the two anticancer drugs shows specific targeting to MCF-7 cells, and remarkably high cytotoxicity compared to NGO loaded with either DOX or CPT only. Considering that the combined use of two or more drugs, a widely adopted clinical practice, often displays much better therapeutic efficacy than that of a single drug, the controlled loading and targeted delivery of mixed anticancer drugs using these graphene-based nanocarriers may find widespread application in biomedicine.

摘要

报道了一种简单的合成路线,用于制备功能化纳米氧化石墨烯(NGO),这是一种新型纳米载体,可用于负载和靶向输送抗癌药物。NGO 经磺酸基团功能化,使其在生理溶液中稳定,然后通过共价键将叶酸(FA)分子结合到 NGO 上,从而使其能够特异性地靶向 MCF-7 细胞,即具有 FA 受体的人乳腺癌细胞。此外,通过π-π 堆积和疏水相互作用,研究了将两种抗癌药物,阿霉素(DOX)和喜树碱(CPT)负载到 FA 接枝 NGO(FA-NGO)上。结果表明,负载两种抗癌药物的 FA-NGO 对 MCF-7 细胞具有特异性靶向作用,与仅负载 DOX 或 CPT 的 NGO 相比,显示出显著更高的细胞毒性。考虑到两种或多种药物的联合使用,这是一种广泛采用的临床实践,通常比单一药物显示出更好的治疗效果,因此,使用这些基于石墨烯的纳米载体来控制负载和靶向输送混合抗癌药物可能会在生物医学中得到广泛应用。

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