Citation: Haitong Shi, Xiaoye Zhao, Jushan Gao, Zhongwen Liu, Zhaotie Liu, Ke Wang, Jinqiang Jiang. Acid-resistant ROS-responsive hyperbranched polythioether micelles for ulcerative colitis therapy[J]. Chinese Chemical Letters, ;2020, 31(12): 3102-3106. doi: 10.1016/j.cclet.2020.03.039 shu

Acid-resistant ROS-responsive hyperbranched polythioether micelles for ulcerative colitis therapy

Haitong Shi ^{a, 1} ,
Xiaoye Zhao ^{b, 1} ,
Jushan Gao ^b ,
Zhongwen Liu ^a ,
Zhaotie Liu ^a ,
Ke Wang ^{b, *,} ,
Jinqiang Jiang ^{a, *,}

a.
Key Laboratory of Syngas Conversion of Shaanxi Province, Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education, School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an 710062, China
b.
School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China

perpetual1003@mail.xjtu.edu.cn

jiangjq@snnu.edu.cn

Received Date: 23 February 2020
Revised Date: 13 March 2020
Accepted Date: 14 March 2020
Available Online: 17 March 2020

Figures(6)

Drug-loaded micelles for oral administration are desired for its convenience, low cost and flexibility, but current designs rely on introducing pH responsiveness, leaving problems like drug leakage and low accuracy of targeted delivery un-solved. Herein, we reported an acid-resistant ROS-responsive hyperbranched polythioether which can self-assemble into micellar structure and pass through the gastrointestinal tract without leaking drugs. At the inflammatory lesions, the thioester bonds are oxidized to sulphone groups to significantly increase the hydrophilicity in response to accumulated ROS species and efficiently release the encapsulated drugs. Animal experiments, including the evaluation of bodyweight, colon length, MPO activity, spleen index, histology and quantitative reverse transcription PCR, evidenced that the drug-loaded micelles have improved therapeutic efficiency compared to bare drug administration for the treatment of DSS-induced colitis in mice. This study provides an example of oral administrated micellar system can be extended for the treatment of other intestinal tract diseases.
- Hyperbranched micelle,
- Acid-resistant,
- ROS responsive,
- Bud,
- Colon-targeting,
- PCR
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