Multistimuli-Responsive Bilirubin Nanoparticles for Anticancer Therapy

Yonghyun Lee, Soyoung Lee, Dong Yun Lee, Byeongjun Yu, Wenjun Miao, Sangyong Jon

Research output: Contribution to journalArticlepeer-review

89 Scopus citations


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.

Original languageEnglish
Pages (from-to)10676-10680
Number of pages5
JournalAngewandte Chemie - International Edition
Issue number36
StatePublished - 26 Aug 2016

Bibliographical note

Publisher Copyright:
© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim


  • anticancer therapy
  • bilirubin
  • drug delivery
  • nanomedicine
  • nanoparticles


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