Cisplatin is a widely used anticancer drug in clinic. However, it may induce drug resistance after a course of treatment and it is difficult to accumulate at tumor site selectively, which result in clinic failure and side effects. We successfully bound cisplatin with vorinostat (a FDA-approved histone deacetylase inhibitor) to form a supramolecular conjugate, which can further self-assemble into nanoparticles. The nanodrug can retain in blood stream for a long time, accumulate in tumor site and hydrolyze to release the two drugs for synergistic therapy. In vivo experiments highlighted the great advantage of the supramolecular nanodrug, because it ensured the two drugs reaching cancer tissue simutaneously. Free cisplatin or cisplatin/vorinostat mixture had negligible or limited effects on A549/DR tumor growth. On the contrary, the tumor inhibitory rate approached 99% with little systemic toxicity if the dose of cisplatin-vorinostat nanodrug reached 10 mg/kg body weight, thus suggesting this supramolecular nanodrug as a promising treatment of drug resistance cancer.

顺铂是临床上广泛使用的抗癌药物。然而，它可能在一个疗程后诱发耐药性，并且难以选择性地在肿瘤部位积聚，这导致临床失败和副作用。我们成功地将顺铂与伏立诺他（美国食品与药物管理局批准的组蛋白脱乙酰基酶抑制剂）结合，形成超分子偶联物，该偶联物可以进一步自组装成纳米颗粒。纳米药物可以在血液中保留很长时间，在肿瘤部位积聚并水解释放出两种药物进行协同治疗。体内实验强调了超分子纳米药物的巨大优势，因为它确保了两种药物同时到达癌症组织。游离的顺铂或顺铂/伏立诺他混合物对A549 / DR肿瘤生长的影响可忽略不计或有限。相反，如果顺铂-伏立诺他纳米药物的剂量达到10 mg / kg体重，则肿瘤抑制率接近99％，几乎没有全身毒性，因此表明这种超分子纳米药物是一种有前途的抗药性癌症治疗方法。