Center for Nanotechnology in Drug Delivery, Shiraz University of Medical Sciences, Shiraz, Iran.
Department of Chemistry, Isfahan University of Technology, Isfahan, Iran; Department of Chemistry, College of Sciences, Shiraz University, Shiraz, Iran.
Carbohydr Polym. 2018 Dec 1;201:151-161. doi: 10.1016/j.carbpol.2018.08.064. Epub 2018 Aug 17.
To enhance graphene stability, drug loading capacity and biocompatibility, β-cyclodextrin (β-CD) was grafted onto graphene oxide (GO) using L-plenylalanine (Phe) as a linker. The doxorubicin (DOX) loading efficiency and capacity of GO-Phe-CD were 78.7% and 85.2%, respectively. The cone shaped cavity of CD acts as a host for DOX loading through inclusion complex formation. The GO-Phe-CD nanocarrier showed higher release ratio of DOX in acidic milieu of cancer cells. In addition, general cytotoxicity of the nanocarriers was examined by MTT assay and trypan blue dye exclusion in MCF-7 cell lines. It was established that the MTT assay was not an appropriate technique for predicting the cytotoxicity of graphene based nanocarriers due to the spontaneous formation of MTT formazan by these materials; leading to a false high biocompatibility. According to the trypan blue experiment, the GO-Phe-CD had significant cytocompatibility, and the DOX-loaded GO-Phe-CD had outstanding killing capability to MCF-7 cells.
为了提高石墨烯的稳定性、载药能力和生物相容性，利用 L-苯丙氨酸（Phe）作为连接物将β-环糊精（β-CD）接枝到氧化石墨烯（GO）上。GO-Phe-CD 的阿霉素（DOX）载药效率和载药能力分别为 78.7%和 85.2%。CD 的锥形腔作为 DOX 装载的主体，通过包合复合物形成。GO-Phe-CD 纳米载体在癌细胞的酸性环境中显示出更高的 DOX 释放率。此外，通过 MTT 测定法和台盼蓝染料排除试验在 MCF-7 细胞系中检测了纳米载体的一般细胞毒性。结果表明，由于这些材料自发形成 MTT 甲臜，MTT 测定法不是预测基于石墨烯的纳米载体细胞毒性的合适技术；导致假高生物相容性。根据台盼蓝实验，GO-Phe-CD 具有显著的细胞相容性，负载 DOX 的 GO-Phe-CD 对 MCF-7 细胞具有出色的杀伤能力。
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