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beta-Cyclodextrin modified graphene oxide-magnetic nanocomposite for targeted delivery and pH-sensitive release of stereoisomeric anti-cancer drugs

机译:β-环糊精修饰的氧化石墨烯-磁性纳米复合材料,用于立体异构抗癌药物的靶向递送和pH敏感释放

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beta-Cyclodextrin modified graphene oxide-magnetic (MGC) nanocomposite as an innovative drug carrier was the first to be developed via an effective layer-by-layer-assembly method. Doxorubicin hydrochloride (DOX) and epirubicin hydrochloride (EPI) as model drugs were loaded onto the MGC via p-p stacking, hydrogen bonding and hydrophobic interactions. The MGC exhibits remarkably higher loading capacity for DOX (909.09 mg g(-1)) and EPI (781.25 mg g(-1)) than magnetic graphene oxide (MG). The release profiles of the drugs are pH-sensitive which would control the release in the acidic cytoplasm of cancer cells. Furthermore, cellular uptake using fluorescein isothiocyanate (FITC) labeled MGC proves successful internalization of MGC into the cytoplasm of MCF-7 cells. The fluorescence images demonstrate that MGC/DOX, to a certain extent, displays a more excellent delivery and superior release than MGC/EPI, due to the chiral selective function of beta-cyclodextrin (beta-CD). The pure MGC shows no obvious cytotoxicity while drug loaded MGC reveals significantly high potency for killing MCF-7 breast cancer cells, suggesting that multi-functionalized MGC is an efficient nanoplatform for targeted delivery and controlled release of stereoisomeric anticancer drugs for biomedical applications.
机译:β-环糊精修饰的氧化石墨烯-磁性(MGC)纳米复合材料是一种创新的药物载体,是第一种通过有效的逐层组装方法开发的产品。通过p-p堆积,氢键和疏水相互作用将作为模型药物的盐酸阿霉素(DOX)和盐酸表柔比星(EPI)加载到MGC上。 MGC对DOX(909.09 mg g(-1))和EPI(781.25 mg g(-1))的负载能力比氧化石墨烯(MG)高得多。药物的释放曲线对pH敏感,可控制癌细胞在酸性细胞质中的释放。此外,使用异硫氰酸荧光素(FITC)标记的MGC的细胞摄取证明了MGC成功内化到MCF-7细胞的细胞质中。荧光图像表明,由于β-环糊精(β-CD)的手性选择性作用,MGC / DOX在一定程度上显示出比MGC / EPI更出色的释放和更好的释放。纯MGC没有明显的细胞毒性,而载药的MGC显示出杀死MCF-7乳腺癌细胞的显着高效力,这表明多功能化MGC是用于生物医学应用的立体异构抗癌药物的靶向递送和控释的有效纳米平台。

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