1. Hydrogen peroxide-activatable polymeric prodrug of curcumin for ultrasound imaging and therapy of acute liver failure.
- Author
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Berwin Singh SV, Jung E, Noh J, Yoo D, Kang C, Hyeon H, Kim GW, Khang G, and Lee D
- Subjects
- Animals, Anti-Inflammatory Agents chemistry, Anti-Inflammatory Agents therapeutic use, Antioxidants chemistry, Antioxidants therapeutic use, Curcumin chemistry, Male, Mice, Mice, Inbred ICR, Prodrugs chemistry, RAW 264.7 Cells, Curcumin therapeutic use, Hydrogen Peroxide chemistry, Liver Failure, Acute diagnostic imaging, Liver Failure, Acute drug therapy, Polymers chemistry, Prodrugs therapeutic use, Ultrasonography methods
- Abstract
Curcumin is a major active phenolic component of turmeric and has gained great attention in pharmaceutics due to its potent antioxidant, anti-inflammatory and anticancer activity. Here, we developed poly(oxalate-co-curcumin) (POC) as a hydrogen peroxide (H
2 O2 )-activatable polymeric prodrug of curcumin by incorporating curcumin in the backbone of H2 O2 -responsive polyoxalate. POC particles effectively scavenged H2 O2 and released curcumin in a H2 O2 -triggered manner. POC particles exhibited excellent antioxidant and anti-inflammatory activity in activated cells. POC particles intravenously administrated into acetaminophen-intoxicated mice remarkably suppressed the level of alanine transaminase and inhibited apoptotic cell death in liver. Interestingly, POC particles could also enhance the ultrasound contrast in the intoxicated liver due to CO2 bubble generation through H2 O2 -triggered oxidation of peroxalate esters. Given their H2 O2 -responsiveness and highly potent antioxidant activity, POC particles hold great translational potential as theranostic agents for H2 O2 -associated diseases., (Copyright © 2018 Elsevier Inc. All rights reserved.)- Published
- 2019
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