College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai 201620, PR China.
School of Science, Engineering and Technology, Kydd Building, Abertay University, Dundee DD1 1HG, Scotland, UK.
Carbohydr Polym. 2016 Jan 1;135:72-8. doi: 10.1016/j.carbpol.2015.08.058. Epub 2015 Aug 22.
In order to enhance the efficiency and specificity of anticancer drug delivery and realize intelligently controlled release, a new drug carrier was developed. Graphene oxide (GO) was first modified with carboxymethyl chitosan (CMC), followed by conjugation of hyaluronic acid (HA) and fluorescein isothiocyanate (FI). The resulting GO-CMC-FI-HA conjugate was characterized and used as a carrier to encapsulate the anticancer drug doxorubicin (DOX) to study in vitro release behavior. The drug loading capacity is as high as 95% and the drug release rate under tumor cell microenvironment of pH 5.8 is significantly higher than that under physiological conditions of pH 7.4. Cell uptake studies show that the GO-CMC-FI-HA/DOX complex can specifically target cancer cells, which are over-expressing CD44 receptors and effectively inhibit their growth. The above results suggest that the functionalized graphene-based material has potential applications for targeted delivery and controlled release of anticancer drugs.
为了提高抗癌药物递送的效率和特异性,并实现智能控制释放,开发了一种新的药物载体。首先用羧甲基壳聚糖(CMC)对氧化石墨烯(GO)进行修饰,然后接枝透明质酸(HA)和异硫氰酸荧光素(FI)。对所得的 GO-CMC-FI-HA 缀合物进行了表征,并用作载体来包封抗癌药物阿霉素(DOX)以研究体外释放行为。载药率高达 95%,在 pH 5.8 的肿瘤细胞微环境下的药物释放率明显高于 pH 7.4 的生理条件下的药物释放率。细胞摄取研究表明,GO-CMC-FI-HA/DOX 复合物可以特异性靶向过表达 CD44 受体的癌细胞,并有效抑制其生长。上述结果表明,功能化的基于石墨烯的材料在抗癌药物的靶向递送和控制释放方面具有潜在的应用。