Stinecipher J, Shah J
Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston 29425, USA.
J Toxicol Environ Health. 1997 Oct 10;52(2):119-35. doi: 10.1080/00984109708984056.
N,N-Diethyl-m-toluamide (DEET), the active ingredient in many commercial mosquito repellents, is thought to be responsible for a wide range of local and systemic adverse reactions following its use. Many investigators have studied the dermal absorption of pure DEET; however, there is only one report in the literature on the absorption of DEET from commercial mosquito repellents and the effect of concentration of DEET on its absorption through skin. The first objective of the present study was to evaluate the permeation characteristics of DEET from four commercial products, Everglades (95%), Repel Deerhunters (52.25%), Off Skintastic (6.65%), and Skedaddle (6.2%), as compared to pure DEET (approximately 100%). The second objective was to study the effects of ethanol, the solvent for DEET, on the permeation of DEET and investigate its potential for enhancing the dermal absorption of DEET. Permeation studies of DEET from commercial mosquito repellents and from solutions containing various percentages of ethanol were conducted across human skin using an infinite dose technique with a Franz diffusion cell. Permeation parameters such as steady-state flux (Jss), lag time (tL), diffusion coefficient (D), permeability (P), and skin/ vehicle partition coefficient (K) were obtained from the permeation profiles in each case. The cumulative amount of DEET permeated can be ranked according to the following order: neat DEET (100%) = Everglades (95%) > Repel (52.25%) > Skedaddle (6.2%) = Off Skintastic (6.65%). Pure DEET exhibited the highest flux value of 63.20 +/- 24.52 micrograms/cm2-h, while Off Skintastic had the lowest value of 21.12 +/- 14.75 micrograms/cm2-h. The tL and D values for each of the products were similar to that of pure DEET. The total amount of DEET permeated from 30-45% ethanolic solutions at the end of 36 h was significantly higher than that from pure DEET and from the 60-90% ethanolic solutions. The Jss, P, and K values of DEET from the 30-45% ethanolic solutions were significantly higher than those from the 75-90% ethanolic solutions, while the tL and D values were similar for each solution. Therefore, there is potential for significant absorption of DEET after the dermal application of commercial mosquito repellents, and ethanol, used as a solvent, may enhance the permeation of DEET.
N,N - 二乙基 - 间甲苯酰胺(避蚊胺,DEET)是许多商用驱蚊剂中的活性成分,人们认为其使用后会引发多种局部和全身不良反应。许多研究人员对纯避蚊胺的皮肤吸收情况进行了研究;然而,文献中仅有一篇报道涉及商用驱蚊剂中避蚊胺的吸收以及避蚊胺浓度对其经皮吸收的影响。本研究的首要目标是评估四种商用产品(大沼泽地(95%)、驱鹿者(52.25%)、Off Skintastic(6.65%)和Skedaddle(6.2%))中避蚊胺的渗透特性,并与纯避蚊胺(约100%)进行比较。第二个目标是研究避蚊胺的溶剂乙醇对避蚊胺渗透的影响,并探究其增强避蚊胺经皮吸收的潜力。采用Franz扩散池的无限剂量技术,对商用驱蚊剂以及含有不同乙醇百分比的溶液中的避蚊胺进行了经人体皮肤的渗透研究。从每种情况的渗透曲线中获得了稳态通量(Jss)、滞后时间(tL)、扩散系数(D)、渗透率(P)和皮肤/载体分配系数(K)等渗透参数。避蚊胺的累积渗透量可按以下顺序排列:纯避蚊胺(100%) = 大沼泽地(95%) > 驱鹿者(52.25%) > Skedaddle(6.2%) = Off Skintastic(6.65%)。纯避蚊胺的通量值最高,为63.20 ± 24.52微克/平方厘米·小时,而Off Skintastic的通量值最低,为21.12 ± 14.75微克/平方厘米·小时。每种产品的tL和D值与纯避蚊胺相似。在36小时结束时,30 - 45%乙醇溶液中避蚊胺的总渗透量显著高于纯避蚊胺和60 - 90%乙醇溶液中的渗透量。30 - 45%乙醇溶液中避蚊胺的Jss、P和K值显著高于75 - 90%乙醇溶液中的相应值,而每种溶液的tL和D值相似。因此,商用驱蚊剂经皮应用后避蚊胺有显著吸收的可能性,且作为溶剂的乙醇可能会增强避蚊胺的渗透。