Bilirubin Nanoparticles as a Nanomedicine for Anti‐inflammation Therapy. Issue 26 (4th May 2016)

• Record Type: Journal Article
• Authors: Lee, Yonghyun; Kim, Hyungjun; Kang, Sukmo; Lee, Jinju; Park, Jinho; Jon, Sangyong
• Is Part Of: Angewandte Chemie international edition. Volume 55:Issue 26(2016)
• Page Start: 7460
• Page End: 7463
• Publication Date: 2016-05-04
• Subjects: bilirubin -- inflammation therapy -- nanomedicine -- nanoparticles -- self-assembled nanostructures; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201602525
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract: Despite the high potency of bilirubin as an endogenous anti‐inflammatory compound, its clinical translation has been hampered because of its insolubility in water. Bilirubin‐based nanoparticles that may overcome this critical issue are presented. A polyethylene glycol compound (PEG) was covalently attached to bilirubin, yielding PEGylated bilirubin (PEG‐BR). The PEG‐BR self‐assembled into nanoscale particles with a size of approximately 110 nm, termed bilirubin nanoparticles (BRNPs). BRNPs are highly efficient hydrogen peroxide scavengers, thereby protecting cells from H2 O2 ‐induced cytotoxicity. In a murine model of ulcerative colitis, intravenous injection of BRNPs showed preferential accumulation of nanoparticles at the sites of inflammation and significantly inhibited the progression of acute inflammation in the colon. Taken together, BRNPs show potential for use as a therapeutic nanomedicine in various inflammatory diseases. Abstract : Bilirubin, a nanomedicine for inflammatory diseases: Bilirubin, a highly potent anti‐inflammatory but extremely water insoluble compound, is converted into nanoparticles by simply introducing PEG. The resultant bilirubin nanoparticles show potential as a nanomedicine in anti‐inflammation therapy. ROS=reactive oxygen species, BRNP=Bilirubin nanoparticle.