School of Life Science, Zhengzhou University, 100 Science Road, Zhengzhou, 450001, PR China.
School of Materials Science and Engineering & Henan Key Laboratory of Advanced Magnesium Alloy, Zhengzhou University, 100 Science Road, Zhengzhou, 450001, PR China.
Carbohydr Polym. 2021 Jun 1;261:117846. doi: 10.1016/j.carbpol.2021.117846. Epub 2021 Feb 23.
In the clinical treatment of cancer, improving the effectiveness and targeting of drugs has always been a bottleneck problem that needs to be solved. In this contribution, inspired by the targeted inhibition on cancer from combination application of disulfiram and divalent copper ion (Cu), we optimized the concentration of disulfiram and Cu ion for inhibiting esophageal cancer cells, and loaded them in hyaluronic acid (HA)/polyethyleneimine (PEI) nanoparticles with specific scales, in order to improve the effectiveness and targeting of drugs. The in vitro cell experiments demonstrated that more drug loaded HA/PEI nanoparticles accumulated to the esophageal squamous cell carcinoma (Eca109) and promoted higher apoptosis ratio of Eca109. Both in vitro and in vivo biological assessment verified that the disulfiram/Cu loaded HA/PEI nanoparticles promoted the apoptosis of cancer cells and inhibited the tumor proliferation, but had no toxicity on other normal organs.
在癌症的临床治疗中,提高药物的疗效和靶向性一直是一个需要解决的瓶颈问题。在本研究中,受双硫仑与二价铜离子(Cu)联合应用靶向抑制癌症的启发,我们优化了双硫仑和 Cu 离子抑制食管癌细胞的浓度,并将其装载到具有特定比例的透明质酸(HA)/聚乙烯亚胺(PEI)纳米颗粒中,以提高药物的疗效和靶向性。体外细胞实验表明,更多负载药物的 HA/PEI 纳米颗粒聚集到食管鳞状细胞癌(Eca109)细胞中,并促进 Eca109 更高的细胞凋亡率。体外和体内生物评估都验证了负载双硫仑/Cu 的 HA/PEI 纳米颗粒促进了癌细胞的凋亡并抑制了肿瘤的增殖,但对其他正常器官没有毒性。