pH响应的碳量子点负载抑制剂体系构建及应用

Construction and Application of pH-Responsive Carbon Quantum Dots-Loaded Inhibitor System

谷氨酰胺抑制剂(V9302)能够阻止癌细胞吸收必须的营养物质,从而抑制肿瘤的生长,且对正常细胞的影响较小,由此设计了一种基于荧光碳量子点(CD)负载抑制剂的给药体系,以荧光碳点为载体,抑制剂为药物,二者通过静电作用结合,而后用牛血清白蛋白(BSA)进行包覆,构成BSA@CD-V9302给药体系。详细表征了体系的特性,研究了其释放性能和药物追踪能力。实验结果表明:在中性条件下药物的载药率达到86.2%,BSA的最大包覆率为60.38%。载药体系对pH敏感,在体外释放实验中,体系pH=5.0的药物释放量是pH=7.4的7.6倍。在细胞毒性实验中,V9302对胃癌细胞的抑制作用随时间的增加明显增强,对正常细胞的影响较小。此外,该体系可以对细胞的状态和药物摄取进行长时间可视化追踪。

Glutamine inhibitors(V9302)can prevent cancer cells from absorbing essential nutrients,inhibiting the growth of the tumor and having slight effect on normal cells.Thus a drug delivery system based on the fluorescent carbon quantum dots(CDs)for the carrier of the inhibitor V9302 was designed.With the fluorescent CDs as the carrier and the inhibitor as the drug,CDs and V9302 were combined through the electrostatic interaction,and then packaged with the bovine serum albumin(BSA)to form the drug delivery system BSA@CDs-V9302.The characteristics of the system were characterized in detail,and its release performance and drug tracking ability were studied.The experiment results show that the drug loading rate reaches 86.2%and the maximum coverage rate of BSA is 60.38%under neutral conditions.The drug-loading system has good sensitivity to pH.In the in vitro release experiments,the drug release amount of the system at pH=5.0 is 7.6 times of that at pH=7.4.In cytotoxicity experiments,the inhibitory effect of V9302 on gastric cancer cells is significantly enhanced over time,while V9302 has slight effect on normal cells.In addition,the system can visually track the cell status and drug uptake for a long time.