Echinacea angustifolia DC. Lipophilic Extract Patch for Skin Application: Preparation, In Vitro and In Vivo Studies
| العنوان: | Echinacea angustifolia DC. Lipophilic Extract Patch for Skin Application: Preparation, In Vitro and In Vivo Studies |
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| المؤلفون: | Dario Voinovich, Dritan Hasa, Antonella Riva, Francesco Cilurzo, Simon Žakelj, Beatrice Perissutti, Stefano Dall'Acqua, Iztok Grabnar |
| المساهمون: | Hasa, Dritan, Žakelj, Simon, Grabnar, Iztok, Cilurzo, Francesco, Dall’Acqua, Stefano, Riva, Antonella, Perissutti, Beatrice, Voinovich, Dario |
| المصدر: | Pharmaceutics, Vol 12, Iss 1096, p 1096 (2020) Pharmaceutics Volume 12 Issue 11 |
| بيانات النشر: | MDPI AG, 2020. |
| سنة النشر: | 2020 |
| مصطلحات موضوعية: | Echinacea angustifolia lipophilic extract, tetraene, drug-in-adhesive patch, in vitro skin permeation, pharmacokinetics, Drug-in-adhesive patch, In vitro skin permeation, Pharmacokinetics, Tetraene, Pharmaceutical Science, lcsh:RS1-441, 02 engineering and technology, Absorption (skin), 030226 pharmacology & pharmacy, Article, lcsh:Pharmacy and materia medica, 03 medical and health sciences, 0302 clinical medicine, Oral administration, In vivo, Transdermal, Chromatography, biology, Chemistry, Echinacea angustifolia, Permeation, 021001 nanoscience & nanotechnology, biology.organism_classification, Bioavailability, 0210 nano-technology |
| الوصف: | Dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamide (tetraene) is the main component of Echinacea angustifolia DC. lipophilic extract, the bioavailability and immunomodulatory effect after oral administration in soft gel capsules in healthy volunteers of which we have already demonstrated. In the present work, we assessed the transdermal administration as an alternative route of administration of such an alkamide. The first step, therefore, encompassed the preparation of a drug-in-adhesive patch with an area of 868 mm2 and containing a dose of 0.64 mg of tetraene. In vitro skin permeation studies in Franz-type diffusion chambers resulted in a tetraene flux of (103 ± 10) ng × cm&minus 2 × h&minus 1 with a very good linearity (r = 0.99). The relatively low lag time of just 13 min indicates low binding and the accumulation of tetraene in the skin. Finally, the patch was administered to six healthy volunteers, and the pharmacokinetic analysis was performed by nonlinear mixed effects modelling with soft gel oral capsules serving as the reference formulation. The in vivo results correlated well with the in vitro permeation and indicated an initial burst tetraene absorption from the patch that was in parallel with the zero-order kinetics of absorption. The rate of the latter process was in good agreement with the one estimated in vitro. The tetraene absorption rate was therefore slow and prolonged with time, resulting in a bioavailability of 39% relative to the soft gel capsules and a very flat plasma concentration profile. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1999-4923 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::052e24cfc67d247d889f6ce5eaaf5df1 https://www.mdpi.com/1999-4923/12/11/1096 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....052e24cfc67d247d889f6ce5eaaf5df1 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 19994923 |
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