Senyiğit Taner, Padula Cristina, Ozer Ozgen, Santi Patrizia
Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Izmir, Turkey.
Int J Pharm. 2009 Oct 1;380(1-2):155-60. doi: 10.1016/j.ijpharm.2009.07.018. Epub 2009 Jul 25.
The aim of this paper was to evaluate the effect of vehicle, chemical enhancer and iontophoresis on the skin accumulation of clobetasol propionate (CP) and mometasone furoate (MF). In vitro permeation experiments were performed using pig ear skin as barrier and HPLC as quantification method. The formulations tested were chitosan gels, sodium-deoxycholate gels and commercial creams of CP and MF. The results obtained indicate that Na-DOC gel had an enhancing effect on the skin accumulation of both active agents. This effect was more evident with CP especially in the stratum corneum and epidermis which are the target sites of topical steroidal treatment. Two terpene derivatives (D-limonene and nerolidol) and Transcutol P were evaluated as chemical penetration enhancers. Nerolidol produced considerable increase in the amount of CP and MF accumulated without any permeation across the skin. The application of electric current (anodal iontophoresis) to the gels improved the accumulation of MF while it did not effect the accumulation of CP. Due to the best accumulation results of nerolidol, the enhancement effect in combination with iontophoresis was also investigated. It was shown that, the combination of anodal iontophoresis and chemical enhancer (nerolidol) produced no further enhancement for both active agents.
本文旨在评估赋形剂、化学增强剂和离子导入对丙酸氯倍他索（CP）和糠酸莫米松（MF）皮肤蓄积的影响。以猪耳皮肤为屏障进行体外渗透实验，采用高效液相色谱法进行定量分析。所测试的制剂为CP和MF的壳聚糖凝胶、脱氧胆酸钠凝胶及市售乳膏。所得结果表明，Na-DOC凝胶对两种活性剂的皮肤蓄积均有增强作用。这种作用在CP上更为明显，尤其是在角质层和表皮，这两个部位是局部甾体治疗的靶位点。评估了两种萜类衍生物（D-柠檬烯和橙花叔醇）和肉豆蔻酸异丙酯作为化学渗透促进剂。橙花叔醇使CP和MF的蓄积量显著增加，且无任何透过皮肤的渗透现象。对凝胶施加电流（阳极离子导入）可提高MF的蓄积量，而对CP的蓄积量无影响。由于橙花叔醇的蓄积效果最佳，还研究了其与离子导入联合使用的增强作用。结果表明，阳极离子导入与化学增强剂（橙花叔醇）联合使用对两种活性剂均未产生进一步的增强作用。
