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一种三羰基铼衍生物,作为一种模型分子,用于掺入磷脂组装体中,用于皮肤应用。

A rhenium tris-carbonyl derivative as a model molecule for incorporation into phospholipid assemblies for skin applications.

机构信息

Institute of Advanced Chemistry of Catalonia (IQAC-CSIC), Jordi Girona 18-26, 08034 Barcelona, Spain.

Bicosome S.L., Jordi Girona 18-26, 08034 Barcelona, Spain.

出版信息

Colloids Surf B Biointerfaces. 2015 Jul 1;131:102-7. doi: 10.1016/j.colsurfb.2015.04.045. Epub 2015 Apr 28.

DOI:10.1016/j.colsurfb.2015.04.045
PMID:25969419
Abstract

A rhenium tris-carbonyl derivative (fac-[Re(CO)3Cl(2-(1-dodecyl-1H-1,2,3,triazol-4-yl)-pyridine)]) was incorporated into phospholipid assemblies, called bicosomes, and the penetration of this molecule into skin was monitored using Fourier-transform infrared microspectroscopy (FTIR). To evaluate the capacity of bicosomes to promote the penetration of this derivative, the skin penetration of the Re(CO)3 derivative dissolved in dimethyl sulfoxide (DMSO), a typical enhancer, was also studied. Dynamic light scattering results (DLS) showed an increase in the size of the bicosomes with the incorporation of the Re(CO)3 derivative, and the FTIR microspectroscopy showed that the Re(CO)3 derivative incorporated in bicosomes penetrated deeper into the skin than when dissolved in DMSO. When this molecule was applied on the skin using the bicosomes, 60% of the Re(CO)3 derivative was retained in the stratum corneum (SC) and 40% reached the epidermis (Epi). Otherwise, the application of this molecule via DMSO resulted in 95% of the Re(CO)3 derivative being in the SC and only 5% reaching the Epi. Using a Re(CO)3 derivative with a dodecyl-chain as a model molecule, it was possible to determine the distribution of molecules with similar physicochemical characteristics in the skin using bicosomes. This fact makes these nanostructures promising vehicles for the application of lipophilic molecules inside the skin.

摘要

一种三羰基铼配合物(fac-[Re(CO)3Cl(2-(1-十二烷基-1H-1,2,3, 三唑-4-基)-吡啶)])被整合到磷脂组装体中,称为双胞体,并用傅里叶变换红外显微镜(FTIR)监测这种分子进入皮肤的情况。为了评估双胞体促进这种衍生物渗透的能力,还研究了溶解在二甲基亚砜(DMSO)中的 Re(CO)3 衍生物的皮肤渗透情况,DMSO 是一种典型的促进剂。动态光散射结果(DLS)显示,随着 Re(CO)3 衍生物的掺入,双胞体的尺寸增加,FTIR 显微镜显示,双胞体中掺入的 Re(CO)3 衍生物比溶解在 DMSO 中时渗透到皮肤更深。当这种分子用双胞体应用于皮肤时,60%的 Re(CO)3 衍生物保留在角质层(SC)中,40%到达表皮(Epi)。否则,通过 DMSO 应用这种分子导致 95%的 Re(CO)3 衍生物在 SC 中,只有 5%到达 Epi。使用具有十二烷基链的 Re(CO)3 衍生物作为模型分子,可以确定具有相似物理化学特性的分子在皮肤中的分布情况。这一事实使这些纳米结构成为在皮肤内部应用亲脂性分子的有前途的载体。

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