3(2) Designing and optimization of aceclofenac transdermal films using response surface methodology: investigating the effect of hydrophilic and hydrophobic matrix on ex vivo and in vivo permeation characteristics

3(2) factorial design and response surface methodology in the fabrication of matrix transdermal films of aceclofenac (ACL) was utilized in this study to investigate the effects of polymers (hydrophilic and hydrophobic) and penetration enhancer (PE) on ex vivo and in vivo drug performance. FTIR and D...

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Veröffentlicht in:Journal of pharmaceutical investigation 2017, 47(6), , pp.541-558
Hauptverfasser: Yadav, Pragya, Rastogi, Vaibhav, Porwal, Mayur, Upadhyay, Prashant, Verma, Anurag
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Sprache:eng
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Zusammenfassung:3(2) factorial design and response surface methodology in the fabrication of matrix transdermal films of aceclofenac (ACL) was utilized in this study to investigate the effects of polymers (hydrophilic and hydrophobic) and penetration enhancer (PE) on ex vivo and in vivo drug performance. FTIR and DSC showed no interaction of drug with polymers. The physicochemical characterization showed uniformity among the formulations. Results from the permeation study suggested the effect of polyvinyl pyrrolidone (PVP K-30) and PE, on increasing concentration of PVP K-30 with respect to ethyl cellulose as well as increased concentration of PE resulted in enhanced permeation through the matrix. Significant effect of PE on the lipid and protein framework of the skin was also observed which is responsible for increased permeation. From response surface curve and contour plots, an optimized formulation was selected and evaluated for their ex vivo permeation, skin irritation, in vivo efficacy and stability studies. The optimized formulation showed Higuchi controlled diffusion and was found to be non-irritant and efficacious in reducing carrageenan induced paw edema in rats over a prolonged duration of time as compared to oral delivery. Thus, results indicated that the prepared transdermal system can be a promising non-oral approach to deliver effective amount of ACL to treat various inflammatory conditions.
ISSN:2093-5552
2093-6214
DOI:10.1007/s40005-016-0285-5