Microencapsulation decreases the skin absorption of N,N-diethyl-m-toluamide (DEFT)

被引:27
作者
Kasting, Gerald B. [1 ]
Bhatt, Varsha D. [1 ]
Speaker, Tycho J. [2 ]
机构
[1] Univ Cincinnati, James L Winkle Coll Pharm, Acad Hlth Ctr, Cincinnati, OH 45267 USA
[2] Capsulent, Santa Cruz, CA 95060 USA
关键词
DEFT; repellent; encapsulation; microencapsulation; percutaneous absorption; skin permeation;
D O I
10.1016/j.tiv.2007.11.003
中图分类号
R99 [毒物学(毒理学)];
学科分类号
100405 ;
摘要
The insect repellent N,N-diethyl-3-methylbenzamide (DEFT) is widely used and is generally regarded as safe when used according to label instructions. Yet many studies have shown it to be absorbed through the skin. The objective of this study was to determine whether the skin absorption rate of DEET could be decreased while maintaining an evaporation rate consistent with effective repellency. To this end, an aqueous suspension containing C-14-DEET (15% w/w) entrapped in walled polysaccharide microcapsules was prepared and tested for skin absorption in vitro using modified Franz cells maintained in a fume hood. The control formulation was 15% w/w DEFT in ethanol. Two doses (3 mu L and 5 mu L per 0.79 cm(2) cell) of each formulation were applied to split-thickness human cadaver skin (n = 8/dose), and permeation was monitored for 24 h. The microencapsulated DEFT formulation lead to a 25-35% reduction of radiolabel permeation compared to the ethanolic DEET formulation. Skin levels of radioactivity at 24 h were comparable, indicating that DEET evaporation from the microencapsulated formulation was comparable to or greater than that from ethanol. Hence microencapsulation increased the ratio of DEET evaporation rate to skin penetration rate relative to unencapsulated control in this in vitro study. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:548 / 552
页数:5
相关论文
共 14 条
[1]  
CHAUDHURI RS, 2007, THESIS U CINCINNATI
[2]  
CUSSLER EL, 1997, DIFFUSION MASS TRANS, P166
[3]   N, N-diethyl-m-toluamide-containing microcapsules for bio-cloth finishing [J].
Fei, Bin ;
Xin, John H. .
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 2007, 77 (01) :52-57
[4]  
FRANZ TJ, 1990, J INVEST DERMATOL, V94, P525
[5]   Influence of encapsulation on the in vitro percutaneous absorption of octyl methoxycinnamate [J].
Jiménez, MM ;
Pelletier, J ;
Bobin, MF ;
Martini, MC .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2004, 272 (1-2) :45-55
[6]   Kinetics of finite dose absorption through skin 2: Volatile compounds [J].
Kasting, GB ;
Miller, MA .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2006, 95 (02) :268-280
[7]   IMPROVING THE SENSITIVITY OF IN-VITRO SKIN PENETRATION EXPERIMENTS [J].
KASTING, GB ;
FILLOON, TG ;
FRANCIS, WR ;
MEREDITH, MP .
PHARMACEUTICAL RESEARCH, 1994, 11 (12) :1747-1754
[8]  
Lehman P.A., 2007, OCCUPATIONAL ENV EXP
[9]   Dose and airflow dependence of benzyl alcohol disposition on skin [J].
Miller, MA ;
Bhatt, V ;
Kasting, GB .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2006, 95 (02) :281-291
[10]   Preparation of polymeric nanocapsules containing octyl methoxycinnamate by the emulsification-diffusion technique:: Penetration across the stratum corneum [J].
Olvera-Martínez, BI ;
Cázares-Delgadillo, J ;
Calderilla-Faardo, SB ;
Villalobos-García, R ;
Ganem-Quintanar, A ;
Quintanar-Guerrero, D .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2005, 94 (07) :1552-1559