University of Cincinnati, James L. Winkle College of Pharmacy, P.O. Box 670004, Cincinnati, Ohio 45267-0004, USA.
J Control Release. 2012 Jun 28;160(3):502-8. doi: 10.1016/j.jconrel.2012.04.023. Epub 2012 Apr 21.
N,N-diethyl-3-methylbenzamide (DEET) is popular insect repellent which is considered safe and effective, yet is subject to considerable skin absorption. Skin absorption decreases effective repellency since less DEET is available for evaporation. We have investigated the extent to which DEET skin absorption can be reduced and evaporation sustained through encapsulation. DEET permeation through human skin in vitro was measured for an ethanolic solution standard and for two novel topical controlled-release formulations in which the DEET active material was temporarily sequestered within a permeable, charged-film microcapsule. Evaporation measurements were gathered using Tenax TA cartridges and a sampling pump drawing air over the skin. Three formulations were studied: a previously reported microcapsule formulation (Formulation A); a newly-developed microcapsule formulation (Formulation B); and a non-encapsulated ethanol control solution. Formulation B led to a 30% reduction in DEET permeation versus control. The two microcapsule DEET formulations exhibited 36-40% higher cumulative evaporation from the skin than did the control. The vapor trapping measurements in vitro show that Formulation B provided more than 48h of effective evaporation rate for repellency, while Formulation A provided less than 35h and the ethanol control less than 15h. This establishes a technical advantage for the controlled-release approach.
N,N-二乙基-3-甲基苯甲酰胺(DEET)是一种常见的驱虫剂,被认为安全有效,但皮肤吸收较多。皮肤吸收会降低驱虫效果,因为蒸发的 DEET 减少。我们研究了通过封装来减少 DEET 皮肤吸收并维持蒸发的程度。体外研究了乙醇溶液标准品和两种新型局部控释制剂中 DEET 的透皮吸收情况,其中 DEET 活性物质暂时被包封在可渗透的荷电膜微胶囊内。使用 Tenax TA 管和抽气泵从皮肤上方抽取空气来收集蒸发测量值。研究了三种制剂:一种先前报道的微胶囊制剂(制剂 A);一种新开发的微胶囊制剂(制剂 B);和非封装的乙醇对照溶液。制剂 B 使 DEET 渗透减少了 30%。与对照相比,两种微胶囊 DEET 制剂从皮肤中累积蒸发的量高出 36-40%。体外蒸气捕集测量表明,制剂 B 为驱虫提供了超过 48 小时的有效蒸发率,而制剂 A 提供了不到 35 小时,乙醇对照不到 15 小时。这为控释方法建立了技术优势。