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Multistimuli‐Responsive Bilirubin Nanoparticles for Anticancer Therapy
Author(s) -
Lee Yonghyun,
Lee Soyoung,
Lee Dong Yun,
Yu Byeongjun,
Miao Wenjun,
Jon Sangyong
Publication year - 2016
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201604858
Subject(s) - doxorubicin , chemistry , bilirubin , drug delivery , drug , nanoparticle , biocompatible material , reactive oxygen species , anticancer drug , nanotechnology , drug carrier , prodrug , biophysics , pharmacology , biochemistry , chemotherapy , materials science , medicine , biomedical engineering , biology , organic chemistry
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.

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