Science China Materials ( IF 6.8 ) Pub Date : 2019-10-21 , DOI: 10.1007/s40843-019-1183-0 Zhilin Liu , Zhaohui Tang , Dawei Zhang , Jiatan Wu , Xinghui Si , Na Shen , Xuesi Chen
The key to improve the therapeutic efficacy for cancer treatment is to increase the delivery of drugs to tumors. For this purpose, tumor-microenvironment stimuli-responsive materials have great potential. Here, we prepared a new nanomedicine by bonding the conjugate of honokiol (HNK) and 5,6-dimethylxanthenone-4-acetic acid (DMXAA) to a glutathione (GSH)-responsive nanocarrier, poly(α-lipoic acid) polyethylene glycol. The nanomedicine would disintegrate due to the high level of GSH at the tumor sites, achieving the co-delivery of HNK and DMXAA, and realizing the combination therapy through close-range killing by HNK and long-range striking by DMXAA together. In a murine 4T1 breast tumor model, this strategy exhibited high tumor inhibition rate of 93%, and provided a valuable therapeutic choice for cancer therapy.
中文翻译:
与厚朴酚-DMXAA共轭物的新型GSH反应性聚(α-硫辛酸)纳米载体键结合用于联合治疗
改善癌症治疗功效的关键是增加药物对肿瘤的递送。为此,肿瘤微环境刺激应答材料具有巨大的潜力。在这里,我们通过将厚朴酚(HNK)和5,6-二甲基黄体酮-4-乙酸(DMXAA)的共轭物与谷胱甘肽(GSH)响应性纳米载体poly(α-硫辛酸)聚乙二醇。由于在肿瘤部位高水平的谷胱甘肽会分解纳米药物,从而实现HNK和DMXAA的共同递送,并通过HNK的近距离杀伤和DMXAA的远距离打击来实现联合治疗。在小鼠4T1乳腺肿瘤模型中,该策略显示出93%的高肿瘤抑制率,并为癌症治疗提供了有价值的治疗选择。