Predicting skin permeability using liposome electrokinetic chromatography.
Predicting skin permeability using liposome electrokinetic chromatography.
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DOI：
10.1039/b807497f
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发表时间：
2009-02
期刊：
影响因子：
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通讯作者：
Yongjun Wang;Jin Sun;Hongzhuo Liu;Jianfang Liu;Liqiang Zhang;Kai Liu;Zhonggui He
中科院分区：
文献类型：
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作者：
Yongjun Wang;Jin Sun;Hongzhuo Liu;Jianfang Liu;Liqiang Zhang;Kai Liu;Zhonggui He
脂质体电动色谱（LEKC）的潜力，这是用于估计化合物穿透皮肤，在这个报告中进行了评估。利用逐步回归方法（R(2) = 0.902）成功地建立了复合皮肤渗透系数（log K(p)）与保留值（log K）之间的定量保留-活性关系（QRARs），并计算了一些分子描述符。此外，所开发的载体方法被用于比较报道的亲脂性测量尺度和通过皮肤的化合物之间的相似性。这两个结果都表明，化合物进入脂质体膜的运输更类似于其通过皮肤的渗透，而不是进入其他系统，包括辛醇-水系统。总之，LEKC是一种很有前途的预测药物穿透皮肤的简单方法。
The potential of liposome electrokinetic chromatography (LEKC), which is applied to estimate compound penetration through the skin, was evaluated in this report. Quantitative retention-activity relationships (QRARs) were successfully constructed between the compound skin permeability coefficient (log K(p)) and the retention values (log k), as well as some calculated molecular descriptors by the stepwise regression method (R(2) = 0.902). Furthermore, the developed vector method was applied to compare the similarity between the reported lipophilicity measuring scales and compounds through the skin. Both results indicated that the transport of a compound into the liposomal membrane was more similar to its penetration through the skin than that into other systems including the octanol-water system. In a word, LEKC is a promising simple method to predict drug penetration through the skin.