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功能化氧化石墨烯作为铂类抗癌药物的药物传递系统。

Functionalized Graphene Oxide as Drug Delivery Systems for Platinum Anticancer Drugs.

机构信息

Pharmaceutical College, Guangxi Medical University, No. 22 Shuangyong Road, Nanning 530021, Guangxi, China.

Chemistry Department, Frostburg State University, 101 Braddock Rd, Frostburg, MD 21532, USA.

出版信息

J Pharm Sci. 2021 Nov;110(11):3631-3638. doi: 10.1016/j.xphs.2021.07.009. Epub 2021 Jul 23.

Abstract

Graphene Oxide, prepared by the modified Hummer's method, was modified with a series of high polymers (polyethyleneimine, polyethylene glycol, chitosan) and Folic Acid for the delivery of platinum anticancer drugs including Cisplatin, Carboplatin, Oxaliplatin and Eptaplatin. Nanocarriers were successfully prepared and characterized by Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscope. Measurement of drug loading efficiency showed that these nanocarriers had the ability for effective delivery of the platinum anticancer drugs. The Maximum loading ratios of Cisplatin, Carboplatin, Oxaliplatin and Eptaplatin were 25.72, 161.08, 345.21 and 67.80 μg/mg. Drug release experiments in the acid environment showed that the cumulative release rate of platinum anticancer drugs from nanocarriers was higher than that in the neutral environment. The cumulative release of all three nanocarriers in the acid environment reached above 60%. In vitro cytotoxicity assay showed that those nanocarriers had a low toxicity. The cell viability rates were above 80% for all three nanocarriers. Investigation of the anticancer activity in vitro showed that those drug delivery systems had the ability to inhibit the growth of the SKOV3 cell line. These results showed that those nanocarriers were suitable for the delivery of platinum anticancer drugs. Providing preliminary advice on the potential application of the combination of platinum anticancer drugs and the functionalized Graphene Oxide nanocarriers.

摘要

氧化石墨烯经改良的 Hummers 法制备,再用一系列高聚物(聚乙烯亚胺、聚乙二醇、壳聚糖)和叶酸进行修饰,用于递呈顺铂、卡铂、奥沙利铂和伊利替康等铂类抗癌药物。通过傅里叶变换红外光谱、X 射线衍射和扫描电子显微镜对纳米载体进行了成功的制备和表征。载药效率的测量表明,这些纳米载体具有有效递呈铂类抗癌药物的能力。顺铂、卡铂、奥沙利铂和伊利替康的最大载药比分别为 25.72、161.08、345.21 和 67.80μg/mg。在酸性环境下的药物释放实验表明,纳米载体中铂类抗癌药物的累积释放率高于中性环境。在酸性环境下,所有三种纳米载体的累积释放率均超过 60%。体外细胞毒性试验表明,这些纳米载体的毒性较低。对于所有三种纳米载体,细胞存活率均在 80%以上。体外抗癌活性研究表明,这些药物递送系统具有抑制 SKOV3 细胞系生长的能力。这些结果表明,这些纳米载体适合递呈铂类抗癌药物。为铂类抗癌药物与功能化氧化石墨烯纳米载体联合应用的潜在应用提供了初步建议。

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