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

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 study.CORM-2-UDLs were prepared by using soy phosphatidylcholine to form lipid bilayers and Tween 80 as an edge activator.The deformability of CORM-2-UDLs was measured and compared with that of conventional liposomes by passing formulations through a filter device at a constant pressure.The release profile of CO from CORM-2-UDLs was evaluated by myoglobin assay.In vitro and in vivo anti-inflammatory effects of CORM-2-UDLs were assessed in lipopolysaccharide-stimulated macrophages and TPA-induced ear edema model,respectively.The deformability of the optimized CORM-2-UDLs was 2.3 times higher than conventional liposomes.CORM-2-UDLs significantly prolonged the release half-life of CO from 30 s in a CORM-2 solution to 21.6 min.CORM-2-UDLs demonstrated in vitro anti-inflammatory activity by decreasing nitrite production and pro-inflammatory cytokine levels.Furthermore,CORM-2-UDLs successfully ameliorated skin inflammation by reducing ear edema,pathological scores,neutrophil accumulation,and inflammatory cytokines expression.The results demonstrate that CORM-2-UDLs could be used as promising therapeutics against acute skin inflammation.

柔性脂质体的促渗作用研究(英文)

In this article different types of ultradeformable liposomes were designed and the properties of transdermal delivery were studied with sodium salicylate as model drug. These results showed that liposomes with strong hydrophilic surfactant added is a new type of penetration enhancer.