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通过用脂质体制剂处理来改变构象皮肤结构及其与阿昔洛韦渗透深度的相关性。

Modification of the conformational skin structure by treatment with liposomal formulations and its correlation to the penetration depth of aciclovir.

机构信息

University of Vienna, Department of Pharmaceutical Technology and Biopharmaceutics, Vienna, Austria.

出版信息

Eur J Pharm Biopharm. 2011 Sep;79(1):76-81. doi: 10.1016/j.ejpb.2011.01.018. Epub 2011 Feb 15.

Abstract

The stratum corneum (SC), top layer of the epidermis, is comprised mostly of lipids that are responsible for the permeability properties of the SC and which protect the body from external agents. Changes in these skin microconstituents can be understood by instrumental methods such as attenuated total reflectance Fourier-transform infrared (ATR-FTIR) spectroscopy. The present work shows that different types of analyzed skin, dermatomed abdominal porcine skin, pig ear skin, and human heat separated skin, influenced both the shape and the intensity of recorded spectra. The typical FTIR spectral bands of the conformation of the lipid aliphatic chains in the skin samples were altered after treatment with pure DPPC liposomes and chitosan (CS) coated DPPC liposomes, but not with aqueous CS-solution. The conformational change could be the reason for the variable permeability of the skin. This was confirmed by tape stripping on pig ear skin (imitating in vivo studies): the amount of aciclovir penetrating from polymer coated and polymer free liposomes was significantly higher under the skin surface in comparison with the aqueous CS-solution. Moreover, the addition of the polymer to liposomes induced a higher skin penetration than pure liposomes. One explanation might be the CS's stronger adhesion to the skin.

摘要

表皮的最外层是角质层(SC),主要由脂质组成,这些脂质决定了 SC 的渗透性,并保护身体免受外部因素的侵害。可以通过仪器方法(如衰减全反射傅里叶变换红外(ATR-FTIR)光谱法)来理解这些皮肤微成分的变化。本工作表明,不同类型的分析皮肤,即腹部猪皮、猪耳皮和人热分离皮,既影响记录光谱的形状,也影响其强度。在使用纯 DPPC 脂质体和壳聚糖(CS)包裹的 DPPC 脂质体处理后,皮肤样品中脂质脂肪链构象的典型 FTIR 光谱带发生了改变,但用纯 CS 溶液处理则没有。这种构象变化可能是皮肤渗透性变化的原因。这在猪耳皮的胶带剥离实验中得到了证实(模拟体内研究):与 CS 水溶液相比,聚合物包裹和无聚合物的脂质体中阿昔洛韦从聚合物包裹的脂质体和无聚合物的脂质体中穿透的量明显更高。此外,与纯脂质体相比,聚合物的添加诱导了更高的皮肤穿透性。一种解释可能是 CS 与皮肤的粘附更强。

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