Department of Pharmaceutical Technology, Friedrich-Schiller-Universität Jena, 07743 Jena, Germany.
Department of Pharmaceutical Chemistry, Friedrich-Schiller-Universität Jena, 07743 Jena, Germany.
J Pharm Sci. 2011 Aug;100(8):3105-3113. doi: 10.1002/jps.22549. Epub 2011 Mar 31.
The retention factors of neutral, positively charged, and negatively charged solutes were determined in a liposome electrokinetic chromatography (EKC) system, where cerasome was used as the investigated liposome. The Abraham linear free energy relationship (LFER) for neutral and ionized solutes gave a good account of the retention factors (N = 71, R(2) = 0.814, and SD = 0.29 log units). It was shown that the calculated retention factors for 16 neutral acids were about four times higher than those of the corresponding anions, whereas the calculated retention factors for neutral bases were less than those for the corresponding cations by a factor of 0.36. The LFER equation for neutral species, anions, and cations was compared with those for partition from water into a number of solvents and for n-octanol-water distribution coefficients. It was shown that the cerasome EKC system is substantially different to the other systems and consequently it could be a very useful additional model system, possibly for predicting skin permeation. It was further shown that there are considerable advantages in the use of Abraham LFERs that can encompass not only neutral molecules but also ionic species.
在脂质体电动色谱 (EKC) 系统中，使用神经酰胺作为研究脂质体，确定了中性、正电荷和负电荷溶质的保留因子。中性和离解溶质的 Abraham 线性自由能关系 (LFER) 很好地解释了保留因子 (N = 71, R² = 0.814, SD = 0.29 log 单位)。结果表明，16 种中性酸的计算保留因子约比相应阴离子高四倍，而中性碱基的计算保留因子比相应阳离子低 0.36 倍。中性物质、阴离子和阳离子的 LFER 方程与从水中分配到多种溶剂和正辛醇-水分配系数的方程进行了比较。结果表明，神经酰胺 EKC 系统与其他系统有很大的不同，因此它可能是一个非常有用的附加模型系统，可能可用于预测皮肤渗透。进一步表明，使用 Abraham LFER 具有相当大的优势，不仅可以涵盖中性分子，还可以涵盖离子物种。
