DEET-loaded solid lipid particles for skin delivery: in vitro release and skin permeation characteristics in different vehicles.
DEET (N,N-diethyl m-toluamide) is a lipophilic compound which has a common use as an insect repellent and causes not only skin irritation but also systemic side effects at high concentrations in long-term skin application. In this study, DEET is incorporated into solid lipid particles, a colloidal drug delivery system, in order to reduce the percutaneous permeation and avoid toxic effects and also maintain drug effectiveness on the skin surface for a long duration of insect repellence. Solid lipid particles were prepared based on emulsion systems at different concentrations and after the characterization studies, the formulation with 20% lipid phase and 1:1 drug:lipid ratio was carried to in vitro release and skin permeation studies. Solid lipid particles with DEET were compared to free DEET using cream and hydrophilic gel vehicles. Results showed that incorporation of DEET into solid lipid particles reduced the release rate and skin permeation of DEET. Imaging studies using scanning electron microscopy showed that there were still solid lipid particles on skin surface after 2 h indicating that DEET could be present for a longer time on the application site.
Iscan
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Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey. yoncayi@yahoo.com
Hekimoglu
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Sargon
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Hincal
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AA
D003671:DEET / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007302:Insect Repellents / Q000493:pharmacokinetics*; D008055:Lipids / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D010539:Permeability; D014677:Pharmaceutical Vehicles; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects*
D007302:Insect Repellents; D008055:Lipids; D014677:Pharmaceutical Vehicles; D003671:DEET