Development of drug-in-adhesive patch formulations for transdermal delivery of fluoxetine: In vitro and in vivo evaluations
| Autor: | Eunjae Jung, In-Soo Yoon, Seung-Hyuk Choi, Sang-Jun Ban, Eun Young Lee, Dae-Duk Kim, Hoo-Kyun Choi, Jungsun Kim |
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| Rok vydání: | 2015 |
| Předmět: |
Male
Drug Chemistry Pharmaceutical Skin Absorption media_common.quotation_subject Cmax Transdermal Patch Pharmaceutical Science In Vitro Techniques Pharmacology Rats Sprague-Dawley Mice Pharmacokinetics In vivo Fluoxetine Cadaver Animals Humans Medicine media_common Transdermal Drug in adhesive Mice Hairless business.industry Plasma levels In vitro Rats Antidepressive Agents Second-Generation business |
| Zdroj: | International Journal of Pharmaceutics. 487:49-55 |
| ISSN: | 0378-5173 |
| Popis: | The aim of this study was to develop drug-in adhesive (DIA) patch formulations for the transdermal delivery of fluoxetine (FX). The DIA patch formulations containing FX were prepared and optimized with various pressure sensitive adhesives, drug contents and enhancers. Among the various formulations, DuroTak 87-502B-based patch formulation containing 20% (w/w) FX with no enhancer was selected for in vivo pharmacokinetic study based on in vitro permeation studies using hairless mouse, rat and human cadaver skins. The Cmax of FX after the transdermal administration of the optimized patch formulation in rats was 52.38 ng/ml, and plasma concentration of FX was maintained for 36 h. Moreover, the predicted human Css (55.79 ng/ml) and Cmax (27.35 ng/ml) were in good agreement with the reported plasma levels (15-55 ng/ml) of oral FX in clinical applications. These results suggest that the optimized patch formulation could be further developed for clinical applications, providing the therapeutic plasma level of FX over an extended period. To the best of our knowledge, our results are the first reported in vitro and in vivo data on the preparation and optimization of FX-loaded DIA patch, showing its feasibility as an effective transdermal delivery system for FX. |
| Databáze: | OpenAIRE |
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