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用于透皮渗透和穿透药物递送测定的基于羊毛脂的合成膜

Lanolin-Based Synthetic Membranes for Transdermal Permeation and Penetration Drug Delivery Assays.

作者信息

Alonso Cristina, Collini Ilaria, Martí Meritxell, Barba Clara, Coderch Luisa

机构信息

Surfactants and Nanobiotechnology Department, Institute of Advanced Chemical of Catalonia of CSIC, (IQAC-CSIC), Jordi Girona 18-26, 08034 Barcelona, Spain.

出版信息

Membranes (Basel). 2021 Jun 15;11(6):444. doi: 10.3390/membranes11060444.

Abstract

Due to the high similarity in composition and structure between lanolin and human SC lipids, we will work with two models from wool wax. Two types of lanolin were evaluated: one extracted with water and surfactants (WEL) and the other extracted with organic solvents (SEL). Skin permeation and skin penetration studies were performed with two active compounds to study the feasibility of the use of lanolin-based synthetic membranes as models of mammalian skin. Diclofenac sodium and lidocaine were selected as the active compounds considering that they have different chemical natures and different lipophilicities. In the permeation assay with SEL, a better correlation was obtained with the less permeable compound diclofenac sodium. This assay suggests the feasibility of using artificial membranes with SEL as a model for percutaneous absorption studies, even though the lipophilic barrier should be improved. Penetration profiles of the APIs through the SEL and WEL membranes indicated that the two membranes diminish penetration and can be considered good membrane surrogates for skin permeability studies. However, the WEL membranes, with a pH value similar to that of the skin surface, promoted a higher degree of diminution of the permeability of the two drugs, similar to those found for the skin.

摘要

由于羊毛脂与人体皮肤角质层脂质在组成和结构上高度相似,我们将使用来自羊毛蜡的两种模型。评估了两种类型的羊毛脂:一种用水和表面活性剂提取(WEL),另一种用有机溶剂提取(SEL)。使用两种活性化合物进行了皮肤渗透和皮肤穿透研究,以研究使用基于羊毛脂的合成膜作为哺乳动物皮肤模型的可行性。选择双氯芬酸钠和利多卡因作为活性化合物,是因为它们具有不同的化学性质和不同的亲脂性。在使用SEL的渗透试验中,与渗透性较低的化合物双氯芬酸钠获得了更好的相关性。该试验表明,即使亲脂性屏障有待改善,使用含SEL的人工膜作为经皮吸收研究模型也是可行的。活性药物成分通过SEL和WEL膜的穿透曲线表明,这两种膜都能减少穿透,可被视为皮肤渗透性研究的良好膜替代物。然而,pH值与皮肤表面相似的WEL膜,对两种药物的渗透性降低程度更高,与在皮肤上观察到的情况相似。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4197/8232266/ac349a7a4570/membranes-11-00444-g001.jpg

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