叶酸修饰的氧化石墨烯作为载体制备替莫唑胺
Folate-modified Graphene Oxide as the Drug Delivery System to Load Temozolomide.
机构信息
Institute of Applied Chemistry, Hebei North University, Zhangjiakou 075000, China.
Drug Support Center, Peoples Liberation Army General Hospital, Beijing 100853, China.
出版信息
Curr Pharm Biotechnol. 2020;21(11):1088-1098. doi: 10.2174/1389201021666200226122742.
OBJECTIVE
The folate-modified graphene oxide (GO-FA), which had good stability and biocompatibility on rat glioma cells was successfully prepared.
METHODS
The formation and composition of GO-FA were confirmed by Scanning Electron Microscope (SEM), Transmission Electron Microscope (TEM), Fourier Transform Infrared Spectrum (FT-IR), Raman spectra and X-ray Photoelectron Spectroscopy (XPS spectra). The cell experiment suggested good biocompatibility of GO-FA on rat glioma cells.
RESULTS
The experiment of GO-FA loading with Temozolomide (TMZ) showed that the maximum drug loading of GO-FA was 8.05 ± 0.20 mg/mg, with the drug loading rate of 89.52 ± 0.19 %. When TMZ was released from the folate-modified graphene oxide loading with temozolomide (GO-FATMZ), its release behavior in vitro showed strong pH dependence and sustained release property. The growth of rat glioma cells can be effectively inhibited by GO-FA-TMZ, with the cell inhibition rate as high as 91.72 ± 0.13 % at the concentration of 600 μg/mL and time of 72 h.
CONCLUSION
According to the above experimental results, this composite carrier has potential applications in drug delivery and cancer therapy.
目的
成功制备了叶酸修饰氧化石墨烯（GO-FA），其在大鼠神经胶质瘤细胞上具有良好的稳定性和生物相容性。
方法
通过扫描电子显微镜（SEM）、透射电子显微镜（TEM）、傅里叶变换红外光谱（FT-IR）、拉曼光谱和 X 射线光电子能谱（XPS 谱）证实了 GO-FA 的形成和组成。细胞实验表明 GO-FA 对大鼠神经胶质瘤细胞具有良好的生物相容性。
结果
GO-FA 载药实验表明，GO-FA 的最大载药量为 8.05±0.20mg/mg，载药率为 89.52±0.19%。当 TMZ 从载有替莫唑胺的叶酸修饰氧化石墨烯（GO-FATMZ）中释放出来时，其体外释放行为表现出强烈的 pH 依赖性和持续释放特性。GO-FA-TMZ 能有效抑制大鼠神经胶质瘤细胞的生长，在浓度为 600μg/mL、时间为 72h 时，细胞抑制率高达 91.72±0.13%。
结论
根据上述实验结果，该复合载体在药物传递和癌症治疗方面具有潜在的应用价值。
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