Mudry Blaise, Guy Richard H, Begoña Delgado-Charro M
School of Pharmaceutical Sciences, University of Geneva, 30 Quai Ernest Ansermet, CH-1211 Geneva, Switzerland.
J Control Release. 2006 Apr 10;111(3):362-7. doi: 10.1016/j.jconrel.2005.12.020. Epub 2006 Feb 20.
The objective of this work was to demonstrate that the efficiency of iontophoretic transport across the skin (which is measured in terms of an ion's transport number), either for drug delivery or for therapeutic drug monitoring, depends implicitly on the molar fraction of the species of interest over a wide range of experimental conditions both in vitro and in vivo. Three sets of data from the literature were assessed to establish the direct relationship between transport number and mole fraction. Linear regression between these parameters yielded slopes which correlated with the charge-carrying efficiency of the ion considered. The latter, furthermore, was proportional to the corresponding aqueous mobility and to the transport number of the ion when it is the sole species available for migration from its electrode solution (the so-called "single-carrier" situation). Finally, the principles illustrated here were equally applicable to in vitro experiments and to in vivo data obtained in a clinically relevant study (specifically, the reverse iontophoretic monitoring of lithiemia in bipolar patients). Not only does this validate an in vitro model typically used in iontophoresis research, it also demonstrates the potential of this approach to predict the feasibility of iontophoretic transport across the skin.
这项工作的目的是证明,无论是用于药物递送还是治疗药物监测,离子电渗法透过皮肤的效率(以离子迁移数衡量)在体外和体内的广泛实验条件下都隐含地取决于目标物质的摩尔分数。评估了文献中的三组数据,以建立迁移数与摩尔分数之间的直接关系。这些参数之间的线性回归产生的斜率与所考虑离子的电荷携带效率相关。此外,当该离子是唯一可从其电极溶液迁移的物质时(即所谓的“单载体”情况),后者与相应的水相迁移率和离子迁移数成正比。最后,这里阐述的原理同样适用于体外实验和在临床相关研究中获得的体内数据(具体而言,双相情感障碍患者锂血症的反向离子电渗监测)。这不仅验证了离子电渗研究中通常使用的体外模型,还证明了这种方法预测离子电渗透过皮肤可行性的潜力。