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首页> 外文期刊>Journal of drug delivery science and technology >Gelified reverse micellar dispersions as percutaneous formulations
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Gelified reverse micellar dispersions as percutaneous formulations

机译:凝胶状逆胶束分散体,经皮制剂

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This study describes the use of lecithin organogels (LO) as versatile vehicles for percutaneous administration of methyl nicotinate (MN), fenretinide (4HPR) and curcumin (CUR). LO are able to increase the solubility of poor water-soluble molecules probably due to the formation of a short-range hexagonal organization of the lecithin cylindrical reverse micelles. After six months from production, no phase separation and an almost absence of aggregates was observed. LO exhibited similar viscosities and rheological behaviour both in the absence and in the presence of drug. The in vitro drug diffusion from LO studied by Franz cell showed that higher viscous vehicles result in lower diffusion coefficient. The microscopic investigation of human skin displayed no significant alterations after treatment with LO and with PBS. In vivo topical activity on erythema after cutaneous application of LO showed that LO-MN induce a strong erythema, while LO-CUR inhibit skin erythema due to CUR anti-inflammatory activity. Tape-stripping experiments performed on skin after topical administration of LO showed a decrease in the amount of CUR in the stratum corneum after 1 h from the occlusion. Shelf life stability studies demonstrated the higher stability of LO-HPR as compared to the others drugs. (C) 2015 Elsevier B.V. All rights reserved.
机译:这项研究描述了卵磷脂有机凝胶(LO)用作经皮施用烟酸甲酯(MN),芬维A胺(4HPR)和姜黄素(CUR)的多功能载体。 LO能够增加不良水溶性分子的溶解度,这可能是由于卵磷脂圆柱状反胶束的短程六角形组织的形成。生产六个月后,没有观察到相分离,几乎没有聚集体。在不存在和存在药物的情况下,LO都表现出相似的粘度和流变行为。 Franz细胞研究了LO在体外的药物扩散,结果表明,较高的粘性载体导致较低的扩散系数。人体皮肤的显微镜检查显示,用LO和PBS处理后,皮肤无明显变化。皮肤应用LO后,体内对红斑的局部活性显示LO-MN诱导强烈的红斑,而LO-CUR由于CUR的抗炎活性而抑制皮肤红斑。 LO局部给药后在皮肤上进行的胶带剥离实验显示,从闭塞1小时后,角质层中CUR的量减少。保质期稳定性研究表明,与其他药物相比,LO-HPR的稳定性更高。 (C)2015 Elsevier B.V.保留所有权利。

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