title: In vitro dermal disposition of abamectin (avermectin B(1)) in livestock.
abstract: Many avermectins are approved for topical application in domestic animals. However, extralabel use may result in significant dermal absorption and consequently the potential for adverse effects or violative residues. The primary aim of this study was to assess dermal disposition of abamectin in vitro in bovine, caprine, ovine, and porcine skin dosed in 100% isopropanol, commercial alcohol-based (Ivomec), or oil-based (Eprinex) formulations. Skin sections were perfused in a flow-through diffusion cell system for 8 h, and the disposition of radiolabel abamectin was determined from perfusate and skin samples. Abamectin absorption ranged from 0.09% to 0.20% dose and there were no significant differences between formulations in each species. Isopropanol significantly increased skin deposition in all species when compared to the oil formulation. Absorption was significantly greater in bovine skin than in porcine skin for the isopropanol-containing formulations, but there were no significant species differences for the oil formulation. While significant levels (11.69-50.23% dose) remained on the skin surface, the highest levels deposited in viable skin were observed in caprine skin (28.09% dose) and the lowest levels were in porcine skin (1.50% dose) which could lead to systemic absorption. In summary, these 8-h experiments demonstrated that the alcohol-based formulations compared to oil-based formulations enhanced abamectin absorption and skin deposition in several animal species, and this effect is more likely to be observed in ruminant species than in porcine species.
authors.affiliation: Center for Chemical Toxicology Research and Pharmacokinetics, College of Veterinary Medicine, North Carolina State University, 4700 Hillsborough Street, Raleigh, NC 27606, USA. ronald_baynes@ncsu.edu
authors.forename: Ronald E
authors.initials: RE
authors.lastname: Baynes
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002417:Cattle / Q000378:metabolism*; D006041:Goats / Q000378:metabolism*; D066298:In Vitro Techniques; D007306:Insecticides / Q000493:pharmacokinetics*; D007559:Ivermectin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D012756:Sheep / Q000378:metabolism*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000502:physiology; D013552:Swine / Q000378:metabolism*
chemical_list: D007306:Insecticides; C048324:abamectin; D007559:Ivermectin