Regeneration and Repair, Key Laboratory for Neurodegenerative Disease of The Ministry of Education, Capital Medical University, Beijing, People's Republic of China.
School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing, People's Republic of China.
Int J Nanomedicine. 2014 Mar 18;9:1433-42. doi: 10.2147/IJN.S58783. eCollection 2014.
Current chemotherapy for glioma is rarely satisfactory due to low therapeutic efficiency and systemic side effects. We have developed a glioma-targeted drug delivery system based on graphene oxide. Targeted peptide chlorotoxin-conjugated graphene oxide (CTX-GO) sheets were successfully synthesized and characterized. Doxorubicin was loaded onto CTX-GO (CTX-GO/DOX) with high efficiency (570 mg doxorubicin per gram CTX-GO) via noncovalent interactions. Doxorubicin release was pH-dependent and showed sustained-release properties. Cytotoxicity experiments demonstrated that CTX-GO/DOX mediated the highest rate of death of glioma cells compared with free doxorubicin or graphene oxide loaded with doxorubicin only. Further, conjugation with chlorotoxin enhanced accumulation of doxorubicin within glioma cells. These findings indicate that CTX-GO is a promising platform for drug delivery and provide a rationale for developing a glioma-specific drug delivery system.
由于治疗效率低和全身副作用，目前针对神经胶质瘤的化疗很少令人满意。我们已经开发了一种基于氧化石墨烯的神经胶质瘤靶向药物传递系统。成功合成并表征了靶向肽氯毒素偶联氧化石墨烯（CTX-GO）片。通过非共价相互作用，将阿霉素高效地负载到 CTX-GO（CTX-GO/DOX）上（每克 CTX-GO 负载 570mg 阿霉素）。阿霉素的释放具有 pH 依赖性，并表现出持续释放的特性。细胞毒性实验表明，与游离阿霉素或仅负载阿霉素的氧化石墨烯相比，CTX-GO/DOX 介导了神经胶质瘤细胞死亡的最高速率。此外，与氯毒素的缀合增强了阿霉素在神经胶质瘤细胞内的积累。这些发现表明 CTX-GO 是一种很有前途的药物传递平台，并为开发神经胶质瘤特异性药物传递系统提供了依据。
