Comparison of percutaneous penetration <i>in vitro</i> using clofibric acid esters and amides as novel enhancers in two species: mouse and guinea pig

Michniak, B. B.; Chapman, James

doi:10.1111/j.1467-2494.1992.tb00050.x

Cited by 4 publications

(2 citation statements)

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“…Methods used in the percutaneous absorption studies were the same as described previously [7,8]. and was evaporated quickly using a stream of warm air from a hair dryer.…”

Section: Diffusion Cell Receptor and Skin Extract Samplesmentioning

confidence: 99%

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A simple and specific high performance liquid chromatography method for the assay of a series of novel dermal penetration enhancers

Michniak

Seyda

1993

Intern J of Cosmetic Sci

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Synopsis A series of clofibric acid amides has been synthesized and previously reported by the authors as possessing enhancer activity in vitro in athymic nude mouse skin against model drugs, hydrocortisone-21-acetate and beta-methasone-17-valerate. An assay was required for each of these enhancers however, which would be specific for each compound and would also separate model drugs and their metabolite peaks. This study reports reverse phase high performance liquid chromatography assays for clofibric acid amide and seven derivatives (Ia-Ig). All enhancers showed maximum absorption at 232 nm, betamethasone (BM) and its valerate (BMV) at 238 nm, and hydrocortisone (HC) and its acetate (HCA) at 242 nm. Practical units of detection for the amides were 0.46-2.8 mug ml(-1) and peaks were sharp and well-separated from steroid peaks in three vehicles - methanol alone. Franz diffusion cell receptor phase samples (isotonic phosphate buffer), and full-thickness athymic nude mouse skin extracts in methanol. Mobile phases consisted of various proportions of acetonitrile and water, some with 2-propanol. The octyl amide for example, with mobile phase CH(3)CN: H(2)O (85:15) at 1 ml min(-1) had a retention time (t(R)) of 7.9 mins. Under the same conditions, retention times for the steroids were HC, t(R)= 3.3 mins; HCA, t(R)= 4.3 mins; BM, t(R)= 3.4 mins; BMV, t(R)= 4.6 mins. Résumé Les auteurs avaient démontré dans un article précédent le pouvoir accélérateur de pénétration dermique in vitro d'une gamme d'amides d'acide clofibrique sur la peau de souris sans poils, et sans thymus avec des médicaments types tels que l'acetate 21 d'hydrocortisone et le valerate 17 de beta-metasone. Il a cependant été requis, pour chacun de ces accélérateurs, un test spécifique pour chaque composition, permettant de séparer chaque médicament et les pics des métabolites. Cette étude décrit des tests par chromatographie liquide à haute performance en phase inverse pour l'acide chlofibrique et 7 dérivés (Ia-Ig). Tous les accélérateurs ont montré une absorption maximale à 232 nm, la beta-metasone (BM) et son valerate (BMV) à 238 nm, l'hydrocortisone (HC) et son acetate (HCA) à 242 nm. Les unités de détection s'élevaient à 0.46-2.8 mug ml(-1) pour les amides et les pics étaient aigus et distincts des pics stéroïdes et se composaient de 3 véhicules - le méthanol seul, des échantillons du récepteur de cellule de diffusion Franz (tampon du phosphate isotonique) et des extraits de peau de souris sans thymus dans du méthanol. Les phases mobiles étaient constituées de différentes proportions d'acetonitrile et d'eau, certaines avec du propanol-2. L'amide octyl par exemple, avec une phase mobile CH(3)CN: H(2)O (85:15) à 1 ml min(-1) avait un temps de rétention (t(R)) de 7.9 min. Dans des conditions identiques, les temps de rétention pour les stéroïdes étaient les suivants: pour HC, t(R)= 3.3 mins; pour HCA, t(R)= 4.3 mins; pour BM: t(R)= 3.4 mins; pour BMV: t(R)= 4.6 mins.

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“…Methods used in the percutaneous absorption studies were the same as described previously [7,8]. and was evaporated quickly using a stream of warm air from a hair dryer.…”

Section: Diffusion Cell Receptor and Skin Extract Samplesmentioning

confidence: 99%

“…Methods used in the percutaneous absorption studies were the same as described previously [7,8]. Full thickness skins obtained from male athymic nude mice 6-8 weeks old BALB/c ByJ-nu stock (Jackson Laboratory, Bar Harbor, MA, USA) were placed in modified Franz diffusion cells.…”

Section: Diffusion Cell Receptor and Skin Extract Samplesmentioning

confidence: 99%