Yazdanian M, Chen E
Animal Formulation Development, Merck Research Laboratories, West Point, PA 19486, USA.
Vet Res Commun. 1995;19(4):309-19. doi: 10.1007/BF01839313.
The effect of diethylene glycol monoethyl ether (DGME; Transcutol) on the permeation of ivermectin, a broad-spectrum antiparasitic agent, through bovine skin was evaluated by in vitro permeation experiments followed by serial sectioning of the skin to assess the amount of ivermectin retained in the skin. Ivermectin permeation through bovine skin was enhanced by DGME and this enhancement was DGME-concentration-dependent. Permeation of ivermectin was effectively enhanced in vehicles with low proportions of DGME, but the magnitude of permeation enhancement decreased as the proportion of DGME increased. The permeation was accompanied by the formation of cutaneous depots of ivermectin. Furthermore, the data indicated that the flux and the cutaneous accumulation of ivermectin were sensitive to the concentration gradient of DGME across the skin. This suggested that ivermectin was permeating with DGME, in which it is very soluble. Hence, the enhancing mechanism involves solubilization of the ivermectin by DGME and the transport of DGME itself across the skin. Based on these results, DGME appears to be a potential vehicle for topical delivery of ivermectin by transport through the skin and through formation of cutaneous depots of ivermectin.
通过体外渗透实验,随后对皮肤进行连续切片以评估伊维菌素在皮肤中的保留量,来评价二甘醇单乙醚(DGME;透皮醇)对广谱抗寄生虫药伊维菌素透过牛皮肤的影响。DGME可增强伊维菌素透过牛皮肤的能力,且这种增强作用依赖于DGME的浓度。在低比例DGME的载体中,伊维菌素的渗透得到有效增强,但随着DGME比例的增加,渗透增强的幅度减小。渗透过程伴随着伊维菌素皮肤贮库的形成。此外,数据表明伊维菌素的通量和皮肤蓄积对DGME跨皮肤的浓度梯度敏感。这表明伊维菌素与DGME一起渗透,伊维菌素在DGME中非常易溶。因此,增强机制涉及DGME对伊维菌素的增溶作用以及DGME自身跨皮肤的转运。基于这些结果,DGME似乎是通过皮肤转运并通过形成伊维菌素皮肤贮库来实现伊维菌素局部给药的潜在载体。