Coelho Sílvia Castro, Reis Daniel Pires, Pereira Maria Carmo, Coelho Manuel A N
LEPABE-Laboratory for Process Engineering, Environment, Biotechnology and Energy, Faculty of Engineering, University of Porto, Rua Dr Roberto Frias, 4200-465 Porto, Portugal.
Pharmaceutics. 2018 Jul 12;10(3):91. doi: 10.3390/pharmaceutics10030091.
Colloidal gold nanoparticles are targeting probes to improve varlitinib delivery into cancer cells. The nanoconjugates were designed by the bioconjugation of pegylated gold nanoparticles with varlitinib via carbodiimide-mediated cross-linking and characterized by infrared and X-ray photoelectron spectroscopy. The drug release response shows an initial delay and a complete drug release after 72 h is detected. In vitro experiments with MIA PaCa-2 cells corroborate that PEGAuNPsVarl conjugates increase the varlitinib toxic effect at very low concentrations (IC50 = 80 nM) if compared with varlitinib alone (IC50 = 259 nM). Our results acknowledge a decrease of drug side effects in normal cells and an enhancement of drug efficacy against to the pancreatic cancer cells reported.
胶体金纳米颗粒是用于改善马来酸瓦利替尼向癌细胞递送的靶向探针。通过碳二亚胺介导的交联将聚乙二醇化金纳米颗粒与马来酸瓦利替尼进行生物共轭设计纳米缀合物，并通过红外和X射线光电子能谱进行表征。药物释放反应显示出初始延迟，并检测到72小时后药物完全释放。与单独使用马来酸瓦利替尼（IC50 = 259 nM）相比，用MIA PaCa-2细胞进行的体外实验证实，PEGAuNPsVarl缀合物在非常低的浓度（IC50 = 80 nM）下会增加马来酸瓦利替尼的毒性作用。我们的结果证实正常细胞中的药物副作用减少，并且所报道的针对胰腺癌细胞的药物疗效增强。
