Center for Bionanoengineering and State Key Laboratory of Chemical Engineering, Zhejiang University, Hangzhou 310027, P.R. China.
Adv Mater. 2013 Jul 19;25(27):3670-6. doi: 10.1002/adma.201300929. Epub 2013 Jun 6.
A prodrug forms nanocapsules responsive to tumor GSH/ROS heterogeneity releasing the parent drug SN38 via thiolysis in the presence of GSH (glutathione) or via enhanced hydrolysis due to ROS (reactive oxygen species)-oxidation of the linker, giving rise to high in vitro cytotoxicity and in vivo anticancer therapeutic activity. The nanocapsules are a suitable size for tumor targeting by means of the EPR effect and have a fixed SN38 loading content of 35 wt%, ideal for translational nanomedicine.
前药形成纳米胶囊，可响应肿瘤 GSH/ROS 异质性，在 GSH（谷胱甘肽）存在的情况下通过硫代裂解释放原药 SN38，或通过 ROS（活性氧）引发的连接物增强水解释放原药 SN38，从而产生高体外细胞毒性和体内抗癌治疗活性。纳米胶囊的尺寸适合通过 EPR 效应进行肿瘤靶向，并且具有固定的 35wt%的 SN38 载药含量，非常适合转化纳米医学。
