Dermal absorption of permethrin following topical administration

Tomalik-Scharte, Dorota; Lazar, Andreas; Meins, Jean-François Le; Bastian, B.; Ihrig, Melanie; Wachall, B.; Jetter, Alexander; Tantcheva-Poór, Illiana; Mahrle, G.; Fuhr, Uwe

doi:10.1007/s00228-005-0932-7

Cited by 75 publications

(55 citation statements)

References 10 publications

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“…This disease is caused by the mite Sarcoptes scabiei, which burrows into the skin and consumes epidermis and sera of the host, resulting in inflammation, allergy-like reactions, and pruritic lesions (4)(5)(6)(7). The currently available treatment options for scabies range from topical scabicides like permethrin, pyrethroids, crotamiton, and lindane to oral medications like antihistamines (8). Benzyl benzoate (BB) is one of the oldest drugs used for the treatment of scabies and is considered as the preferred treatment option for the same (9).…”

Section: Introductionmentioning

confidence: 99%

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

et al. 2015

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Abstract. Benzyl benzoate (BB) is one of the oldest drugs used for the treatment of scabies and is recommended as the "first-line intervention" for the cost-effective treatment of the disease. Though a promising candidate, its application is reported to be associated with irritation of the skin and eye, resulting in poor patient compliance. Hence, the present study aims to develop BB-loaded topical microemulsion for the safer and effective delivery of BB. Pseudo-ternary phase diagrams with BB as the oily phase itself, along with Tween 80 as surfactant, and mixture of phospholipid and ethanol as the cosurfactant along with aqueous solution as the external phase were constructed and various compositions were formulated. The optimized formulation was characterized for particle-size, zeta-potential, drugcontent, globule-morphology pH, and refractive-index, whereas evaluated for skin permeation, retention, compliance, and dermatokinetics. The nanosized formulation offered threefold higher drug permeation vis-a-vis plain drug solution across LACA mice abdominal skin. The drug retention of the selected formulation was nearly twice of that from the marketed product, assuring depot formulation and sustained release. The skin histopathology revealed the non-irritant nature of the formulation, as no changes in the normal skin histology were observed. The dermatokinetic studies confirmed better permeation and enhanced skin bioavailability of BB to epidermis as well as dermis vis-à-vis the conventional product. The results indicate that the developed lipid-based microemulsion hydrogel can alleviate the concerns associated with BB and can provide a better and safer delivery option in substantial amounts to various skin layers.

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Section: Introductionmentioning

confidence: 99%

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

et al. 2015

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“…The SHEDS-Multimedia modeling of permethrin , applied a fractional absorption of permethrin based on the dermal dose-excretion study of Tomalik-Scharte et al (2005). Here we modified our method according to Kissel (2011), who observed that in fluxlimited systems (i.e., dermal studies conducted with high surface loadings) an inverse proportionality between surface loading and fractional absorption may be observed.…”

Section: Dermal Exposurementioning

confidence: 96%

EPA's SHEDS-multimedia model: Children's cumulative pyrethroid exposure estimates and evaluation against NHANES biomarker data

Xue

Zartarian

Tornero‐Velez

et al. 2014

Environment International

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The U.S. EPA's SHEDS-Multimedia model was applied to enhance the understanding of children's exposures and doses to multiple pyrethroid pesticides, including major contributing chemicals and pathways. This paper presents combined dietary and residential exposure estimates and cumulative doses for seven commonly used pyrethroids, and comparisons of model evaluation results with NHANES biomarker data for 3-PBA and DCCA metabolites. Model input distributions were fit to publicly available pesticide usage survey data, NHANES, and other studies, then SHEDS-Multimedia was applied to estimate total pyrethroid exposures and doses for 3-5 year olds for one year variability simulations. For dose estimations we used a pharmacokinetic model and two approaches for simulating dermal absorption. SHEDS-Multimedia predictions compared well to NHANES biomarker data: ratios of 3-PBA observed data to SHEDS-Multimedia modeled results were 0.88, 0.51, 0.54 and 1.02 for mean, median, 95th, and 99th percentiles, respectively; for DCCA, the ratios were 0.82, 0.53, 0.56, and 0.94. Modeled time-averaged cumulative absorbed dose of the seven pyrethroids was 3.1 nmol/day (versus 8.4 nmol/day for adults) in the general population (residential pyrethroid use and non-use homes) and 6.7 nmol/day (versus 10.5 nmol/day for adults) in the simulated residential pyrethroid use population. For the general population, contributions to modeled cumulative dose by chemical were permethrin (60%), cypermethrin (22%), and cyfluthrin (16%); for residential use homes, contributions were cypermethrin (49%), permethrin (29%), and cyfluthrin (17%). The primary exposure route for 3-5 year olds in the simulated residential use population was non-dietary ingestion exposure; whereas for the simulated general population, dietary exposure was the primary exposure route. Below the 95th percentile, the major exposure pathway was dietary for the general population; non-dietary ingestion was the major pathway starting below the 70th percentile for the residential use population. The new dermal absorption methodology considering surface loading had some impact, but did not change the order of key pathways.

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“…Obwohl Pyrethrine und Pyrethroide in dieser Altersgruppe verstärkt transdermal penetrieren, verursachen sie dennoch keine systemischen Wirkspiegel bei großflä-chigem Auftragen [4], weil ihre Abbaurate in der Haut (und ggf. auch in der Leber) hoch genug ist (nachgewiesen am Kaninchen [5]).…”

Section: Allgemeine Pharmakokinetische Eigenschaftenunclassified

“…Oxidation, Hydrolyse, Konjugation) sorgt für eine schnelle Elimination, sodass die HWZ von Permethrin kurz ist.Nach Anwendung vom 0,5% Permethrin am Menschen konnten nach 7 Tagen keine Hauptmetabolite des Wirkstoffs im Urin mehr nachgewiesen werden, unabhängig davon, ob eine Lösung (Präparat gegen Läuse) oder Creme (Präparat gegen Skabies) verwandt wurde[4]. (Fall)berichte zu toxischen Wirkungen.Der Absatz von permethrinhaltigen Prä-paraten liegt nach Extrapolation der bekannten Daten seit Zulassung Mitte der 1980er-Jahre weltweit bei 200-250 Mio.…”

unclassified

Geringe Toxizität der Läusemittel Pyrethrin, Pyrethroide und Permethrin

Sunderkötter

Kirchhefer

2010

Hautarzt

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Dermal absorption of permethrin following topical administration

Cited by 75 publications

References 10 publications

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

EPA's SHEDS-multimedia model: Children's cumulative pyrethroid exposure estimates and evaluation against NHANES biomarker data

Geringe Toxizität der Läusemittel Pyrethrin, Pyrethroide und Permethrin

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