Tianjin Cancer Institute and Hospital, Research Center of Basic Medical Science, Key Laboratory of Breast Cancer Prevention and Therapy, Ministry of Education, Tianjin Medical University, Tianjin, People's Republic of China.
Nanotechnology. 2012 Sep 7;23(35):355101. doi: 10.1088/0957-4484/23/35/355101. Epub 2012 Aug 8.
This study evaluates the reversal effects of graphene oxide (GO) used as a carrier for adriamycin (ADR) in cancer drug resistance, and provides a preliminary investigation into the reversal mechanism. ADR was loaded onto the GO surface (ADR-GO) by physical mixing and drug loading content was found to be high, up to 93.6%. In vitro releases of ADR from ADR-GO were studied using a dialysis method, and they exhibited a significant pH-sensitive property. Cell experiments showed that GO significantly enhanced the accumulation of ADR in MCF-7/ADR cells (an ADR resistant breast cancer cell line) and exhibited much higher cytotoxicity than free ADR, suggesting that ADR-GO could effectively reverse ADR resistance of MCF-7/ADR, with the reversal index reaching 8.35. Microscopy studies found that GO could effectively carry drug molecules into cells in both endocytosis-dependent and independent manners. In conclusion, use of GO as a carrier for chemotherapeutic agents is favorable for the treatment of drug resistant cancers.
本研究评估了氧化石墨烯（GO）作为阿霉素（ADR）载体在癌症耐药性逆转中的作用，并初步探讨了其逆转机制。ADR 通过物理混合负载到 GO 表面（ADR-GO），载药率高达 93.6%。通过透析法研究了 ADR-GO 体外的 ADR 释放情况，其表现出显著的 pH 敏感性。细胞实验表明，GO 显著增加了 MCF-7/ADR 细胞（一种 ADR 耐药乳腺癌细胞系）中 ADR 的积累，并且表现出比游离 ADR 更高的细胞毒性，表明 ADR-GO 可以有效逆转 MCF-7/ADR 的 ADR 耐药性，逆转指数达到 8.35。显微镜研究发现，GO 可以通过内吞作用依赖和非依赖的方式将药物分子有效带入细胞。总之，使用 GO 作为化疗药物的载体有利于治疗耐药性癌症。
