Controlled Release of an Anti-inflammatory Drug Using an Ultrasensitive ROS-Responsive Gas-Generating Carrier for Localized Inflammation Inhibition

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• 作者：Ming-Fan Chung ; Wei-Tso Chia ; Wei-Lin Wan ; Yu-Jung Lin ; Hsing-Wen Sung
• 刊名：Journal of the American Chemical Society
• 出版年：2015
• 出版时间：October 7, 2015
• 年：2015
• 卷：137
• 期：39
• 页码：12462-12465
• 全文大小：318K
• ISSN：1520-5126

文摘

Inflammation is associated with many diseases, in which activated inflammatory cells produce various reactive oxygen species (ROS), including H₂O₂. This work proposes an ultrasensitive ROS-responsive hollow microsphere (HM) carrier that contains an anti-inflammatory drug, an acid precursor consisting of ethanol and FeCl₂, and sodium bicarbonate (SBC) as a bubble-generating agent. In cases of inflamed osteoarthritis, the H₂O₂ at low concentration diffuses through the HMs to oxidize their encapsulated ethanol in the presence of Fe²⁺ by the Fenton reaction, establishing an acidic milieu. In acid, SBC decomposes to form CO₂ bubbles, disrupting the shell wall of the HMs and releasing the anti-inflammatory drug to the problematic site, eventually protecting against joint destruction. These results reveal that the proposed HMs may uniquely exploit biologically relevant concentrations of H₂O₂ and thus be used for the site-specific delivery of therapeutics in inflamed tissues.