Schuetz Yannic B, Naik Aarti, Guy Richard H, Vuaridel Evelyne, Kalia Yogeshvar N
School of Pharmaceutical Sciences, University of Geneva, Geneva CH-1211, Switzerland.
J Pharm Sci. 2005 Oct;94(10):2175-82. doi: 10.1002/jps.20433.
The feasibility of delivering triptorelin ([D-Trp6]LHRH) by transdermal iontophoresis was evaluated in vitro. Peptide electrotransport at different current densities and donor concentrations was measured across porcine ear skin. The concomitant delivery of an electroosmotic marker enabled calculation of the respective contributions of electromigration (EM) and electroosmosis (EO) to iontophoretic delivery. At a given concentration (3 mM), a threefold increase in current density produced a corresponding increase in the cumulative amount of peptide present in the receptor compartment. Conversely, doubling the concentration to 6 mM produced a twofold reduction in the amount of peptide delivered, partly due to a concentration-dependent inhibition of EO. EM was revealed to be the predominant transport mechanism, accounting for 80% of overall delivery. Finally, despite the inhibition of EO, the results indicate that application of an iontophoretic current of 0.8 mA over a relatively small contact area (4 cm2) would provide a delivery rate of 36 microg/h, largely sufficient for therapeutic requirements.
在体外评估了通过经皮离子电渗法递送曲普瑞林（[D - 色氨酸6]促黄体激素释放激素）的可行性。在猪耳皮肤上测量了不同电流密度和供体浓度下的肽电转运。电渗标记物的伴随递送使得能够计算电迁移（EM）和电渗（EO）对离子电渗递送的各自贡献。在给定浓度（3 mM）下，电流密度增加三倍会使受体隔室中存在的肽累积量相应增加。相反，将浓度加倍至6 mM会使递送的肽量减少两倍，部分原因是EO受到浓度依赖性抑制。结果表明EM是主要的转运机制，占总递送量的80%。最后，尽管EO受到抑制，但结果表明在相对较小的接触面积（4 cm²）上施加0.8 mA的离子电流将提供36 μg/h的递送速率，这在很大程度上足以满足治疗需求。
