title: Development of drug-in-adhesive patch formulations for transdermal delivery of fluoxetine: In vitro and in vivo evaluations.
abstract: 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.
authors: College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Republic of Korea.
authors: Eunjae
authors: E
authors: Jung
authors: College of Pharmacy, Chosun University, Gwangju 501-759, Republic of Korea.
authors: Eun Young
authors: EY
authors: Lee
authors: College of Pharmacy, Chosun University, Gwangju 501-759, Republic of Korea.
authors: Hoo-Kyun
authors: HK
authors: Choi
authors: College of Pharmacy, Chosun University, Gwangju 501-759, Republic of Korea.
authors: Sang-Jun
authors: SJ
authors: Ban
authors: College of Pharmacy, Chosun University, Gwangju 501-759, Republic of Korea.
authors: Seung-Hyuk
authors: SH
authors: Choi
authors: Division of Health Sciences, Dongseo University, Busan 617-716, Republic of Korea.
authors: Jung Sun
authors: JS
authors: Kim
authors: College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam 534-729, Republic of Korea. Electronic address: isyoon@mokpo.ac.kr.
authors: In-Soo
authors: IS
authors: Yoon
authors: College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Republic of Korea. Electronic address: ddkim@snu.ac.kr.
authors: Dae-DuK
authors: DD
authors: Kim
mesh_terms: D000818:Animals; D018687:Antidepressive Agents, Second-Generation / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002102:Cadaver; D002626:Chemistry, Pharmaceutical; D005473:Fluoxetine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D057968:Transdermal Patch
chemical_list: D018687:Antidepressive Agents, Second-Generation; D005473:Fluoxetine
keywords: Drug-in-adhesive; Fluoxetine; Patch; Pharmacokinetics; Transdermal delivery