Multistimuli‐Responsive Bilirubin Nanoparticles for Anticancer Therapy

作者：Yonghyun Lee, Soyoung Lee, Dong Yun Lee, Byeongjun Yu, Wenjun Miao, Sangyong Jon · 发表于：Angewandte Chemie International Edition · 年份：2016 · DOI：10.1002/anie.201604858 · 被引用次数：107 · 研究领域：Heme Oxygenase-1 and Carbon Monoxide、Neonatal Health and Biochemistry、Hemoglobin structure and function

Although stimuli-responsive materials hold potential for use as drug-delivery carriers for treating cancers, their clinical translation has been limited. Ideally, materials used for the purpose should be biocompatible and nontoxic, provide "on-demand" drug release in response to internal or external stimuli, allow large-scale manufacturing, and exhibit intrinsic anticancer efficacy. We present multistimuli-responsive nanoparticles formed from bilirubin, a potent endogenous antioxidant that possesses intrinsic anticancer and anti-inflammatory activity. Exposure of the bilirubin nanoparticles (BRNPs) to either reactive oxygen species (ROS) or external laser light causes rapid disruption of the BRNP nanostructure as a result of a switch in bilirubin solubility, thereby releasing encapsulated drugs. In a xenograft tumor model, BRNPs loaded with the anticancer drug doxorubicin (DOX@BRNPs), when combined with laser irradiation of 650 nm, significantly inhibited tumor growth. This study suggests that BRNPs may be used as a drug-delivery carrier as well as a companion medicine for effectively treating cancers.