The effect of diethylene glycol monoethyl ether as a vehicle for topical delivery of ivermectin |
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Authors: | M Yazdanian E Chen |
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Institution: | (1) Merck Research Laboratories, Animal Formulation Development, 19486 West Point, PA, USA;(2) Boehringer Ingelheim Pharm. Inc., 900 Ridgebury Road, PO Box 368, 06877 Ridgefield, CT, USA |
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Abstract: | The effect of diethylene glycol monoethyl ether (DGME; Transcutol) on the permeation of ivermectin, a broad-spectrum antiparasitic agent, through bovine skin was evaluated byin 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.Abbreviations DGME
diethylene glycol monoethyl ether |
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Keywords: | cow ivermectin permeability skin Transcutol transdermal vehicle |
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