结合
内化
体内
材料科学
共轭体系
体外
纳米颗粒
连接器
癌症研究
靶向治疗
肽
两亲性
活性氧
癌细胞
生物物理学
癌症
纳米技术
化学
生物化学
医学
受体
生物
共聚物
生物技术
复合材料
数学分析
内科学
计算机科学
数学
聚合物
操作系统
作者
Xi Xia,Xiaoyuan Yang,Ping Huang,Deyue Yan
标识
DOI:10.1021/acsami.0c00650
摘要
The targeted nanoagents have shown great potential clinically for cancer therapy. Traditional targeted nanodrugs are usually prepared through surface postmodification. Herein, a nanodrug is self-assembled from the amphiphilic precursor of targeting peptide RGD conjugated with cytotoxin epothilone B (Epo B) through a linker containing the thioketal (tk) group that is sensitive to reactive oxygen species (ROS). The obtained RGD–tk–Epo B conjugate nanoparticles (RECNs) are stable and uniform, which facilitates improving tumor-targeting capacity and accumulation of the drug because of the large number of RGD on the surface of the RECN. After internalization by cancer cells, the blood-inert tk group between RGD and Epo B can be cleaved in the presence of high level of ROS to release Epo B, exhibiting a markedly tumor selectivity and excellent anticancer efficiency in vitro and in vivo.
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