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CORM-2-entrapped ultradeformable liposomes ameliorate acute skin inflammation in an ear edema model via effective CO delivery

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Acta Pharmaceutica Sinica B 2020年第12期10卷 2362-2373,2440页

作者： Gwan-Yeong Lee Alam Zeb Eun-Hye Kim beomseon suh Young-Jun Shin Donghyun Kim Kyoung-Won Kim Yeong-Hwan Choe Ho-Ik Choi Cheol-Ho Lee Omer Salman Qureshi In-Bo Han Sun-Young Chang Ok-Nam Bae Jin-Ki Kim College of Pharmacy Institute of Pharmaceutical Science and TechnologyHanyang UniversityAnsan 15588Republic of Korea Riphah Institute of Pharmaceutical Sciences Riphah International UniversityIslamabad 44000Pakistan Department of Pharmacy Forman Christian CollegeLahore 54600Pakistan Department of Neurosurgery CHA Bundang Medical CenterSchool of MedicineCHA UniversitySeongnam 13496Republic of Korea College of Pharmacy Ajou UniversitySuwon 16499Republic of Korea

The short release half-life of carbon monoxide(CO)is a major obstacle to the effective therapeutic use of carbon monoxide-releasing molecule-2(CORM-2).The potential of CORM-2-entrapped ultradeformable liposomes(CORM-2-UDLs)to enhance the release half-life of CO and alleviate skin inflammation was investigated in the present ***-2-UDLs were prepared by using soy phosphatidylcholine to form lipid bilayers and Tween 80 as an edge *** deformability of CORM-2-UDLs was measured and compared with that of conventional liposomes by passing formulations through a filter device at a constant *** release profile of CO from CORM-2-UDLs was evaluated by myoglobin *** vitro and in vivo anti-inflammatory effects of CORM-2-UDLs were assessed in lipopolysaccharide-stimulated macrophages and TPA-induced ear edema model,*** deformability of the optimized CORM-2-UDLs was 2.3 times higher than conventional ***-2-UDLs significantly prolonged the release half-life of CO from 30 s in a CORM-2 solution to 21.6 ***-2-UDLs demonstrated in vitro anti-inflammatory activity by decreasing nitrite production and pro-inflammatory cytokine ***,CORM-2-UDLs successfully ameliorated skin inflammation by reducing ear edema,pathological scores,neutrophil accumulation,and inflammatory cytokines *** results demonstrate that CORM-2-UDLs could be used as promising therapeutics against acute skin inflammation.

关键词： Carbon monoxide CORM-2 Anti-inflammatory effect Ultradeformable liposomes Skin inflammation Ear edema

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