Dahlizar Sabrina, Futaki Mika, Okada Akie, Yatomi Chihiro, Todo Hiroaki, Sugibayashi Kenji
Graduate School of Pharmaceutical Sciences, Josai University, Saitama 350-0295, Japan.
Department of Pharmacy, Faculty of Health Science, Syarif Hidayatullah State Islamic University Jakarta, Banten 15419, Indonesia.
Pharmaceutics. 2018 Sep 20;10(4):163. doi: 10.3390/pharmaceutics10040163.
-Palmitoyl-Glycine-Histidine (Pal-GH) is a novel low molecular weight gelator. In our previous report, ivermectin, a lipophilic drug, was effectively delivered to skin tissue after topical application with Pal-GH as a spray gel formulation, and a much higher skin concentration was confirmed than with the administration of a conventional oral formulation. The objective of this study was to increase the skin permeation of metronidazole (MTZ), a hydrophilic drug, after the topical application of Pal-GH gel. An evaluation of the combined effect of chemical penetration enhancers (CPEs), such as isopropyl myristate (IPM), propylene glycol (PG), ethanol, diethylene glycol monoethyl ether, and dimethyl sulfoxide (DMSO), on skin permeation was also conducted. We found that a 5% Pal-GH gel containing 1% MTZ (F5) exhibited a 2.7-fold higher MTZ permeation through excised hairless rat skin than its solution. Furthermore, F5 and F5 further increased the skin permeation of MTZ when compared to F5 Interestingly, F5 enhanced the skin penetration of MTZ, although no enhancement effect was observed for an MTZ solution containing PG. Thus, a Pal-GH formulation containing PG and IPM may enhance the skin permeation of MTZ.
棕榈酰甘氨酸-组氨酸（Pal-GH）是一种新型低分子量凝胶剂。在我们之前的报告中，亲脂性药物伊维菌素以喷雾凝胶制剂的形式与Pal-GH一起局部应用后，有效地输送到了皮肤组织中，并且证实其皮肤浓度比传统口服制剂给药时高得多。本研究的目的是在局部应用Pal-GH凝胶后提高亲水性药物甲硝唑（MTZ）的皮肤渗透性。还评估了肉豆蔻酸异丙酯（IPM）、丙二醇（PG）、乙醇、二甘醇单乙醚和二甲亚砜（DMSO）等化学渗透促进剂（CPEs）对皮肤渗透的联合作用。我们发现，含有1%MTZ的5%Pal-GH凝胶（F5）通过切除的无毛大鼠皮肤的MTZ渗透量比其溶液高2.7倍。此外，与F5相比，F5和F5进一步提高了MTZ的皮肤渗透性。有趣的是，F5增强了MTZ的皮肤渗透，尽管对于含有PG的MTZ溶液未观察到增强作用。因此，含有PG和IPM的Pal-GH制剂可能会增强MTZ的皮肤渗透。
