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Structural Transformative Antioxidants for Dual‐Responsive Anti‐Inflammatory Delivery and Photoacoustic Inflammation Imaging
Author(s) -
Zhao Caiyan,
Chen Jingxiao,
Ye Jiamin,
Li Zhi,
Su Lichao,
Wang Junqing,
Zhang Ye,
Chen Jinghua,
Yang Huanghao,
Shi Jinjun,
Song Jibin
Publication year - 2021
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.202100873
Subject(s) - phenylboronic acid , chemistry , inflammation , oxidative stress , in vivo , biophysics , biochemistry , immunology , medicine , microbiology and biotechnology , biology , catalysis
We have synthesized a PEGylated, phenylboronic acid modified L‐DOPA pro‐antioxidant (pPAD) that can self‐assemble into nanoparticles (pPADN) for the loading of a model glucocorticoid dexamethasone (Dex) through 1,3‐diol/phenylboronic acid chemistry and hydrophobic interactions for more effective treatment of inflammation. Upon exposure to ROS, pPADN convert into the active form of L‐DOPA, and a cascade of oxidative reactions transform it into antioxidative melanin‐like materials. Concomitantly, the structural transformation of pPADN triggers the specific release of Dex, along with the acidic pH of inflammatory tissue. In a rat model of osteoarthritis, Dex‐loaded pPADN markedly mitigate synovial inflammation, suppress joint destruction and cartilage matrix degradation, with negligible in vivo toxicity. Moreover, in situ structural transformation makes pPADN suitable for noninvasive monitoring of therapeutic effects as a photoacoustic imaging contrast agent.

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