Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium

The objective of this study was to develop a novel elastic bilayer vesicle entrapped with the non-steroidal anti-inflammatory drug (NSAID), diclofenac diethylammonium (DCFD) for topical use. Eighteen bilayer vesicular formulations composing of DPPC or Tween 61 or Span 60 mixed with cholesterol (at 1...

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Main Authors: A. Manosroi, P. Jantrawut, J. Manosroi
Format: Journal
Published: 2018
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http://cmuir.cmu.ac.th/jspui/handle/6653943832/60713
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spelling th-cmuir.6653943832-607132018-09-10T03:47:51Z Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium A. Manosroi P. Jantrawut J. Manosroi Pharmacology, Toxicology and Pharmaceutics The objective of this study was to develop a novel elastic bilayer vesicle entrapped with the non-steroidal anti-inflammatory drug (NSAID), diclofenac diethylammonium (DCFD) for topical use. Eighteen bilayer vesicular formulations composing of DPPC or Tween 61 or Span 60 mixed with cholesterol (at 1:1, 3:7 and 1:1 molar ratios, respectively) and ethanol at 0-25% (v/v), by chloroform film method with sonication were developed. The elastic Tween 61 niosomes which gave no sedimentation, no layer separation, unchanged particle sizes (about 200 nm) were selected to entrap DCFD. The entrapment efficiency of the drug in the conventional and elastic Tween 61 niosomes was 65 and 93%, respectively. At least 87% of DCFD determined by HPLC remained in elastic Tween 61 niosomes when kept at 4, 27 and 45 °C for 3 months. The deformability index values of the elastic niosomes were 13.76 and 3.44 times higher than the conventional niosomes entrapped and not entrapped with the drug, respectively, indicating the higher flexibility of the elastic vesicle especially, when entrapped with the drug. Transdermal absorption through excised rat skin was performed by vertical Franz diffusion cell at 32 ± 2 °C for 6 h. Gel containing elastic niosomes exhibited fluxes of DCFD in the stratum corneum (SC), deeper skin layer (viable epidermis and dermis, VED) and receiver chamber at 191.27 ± 9.52, 16.97 ± 2.77 and 3.76 ± 0.54 μg/(cm2h), whereas the commercial emulgel, containing an equivalent DCFD, gave 60.84 ± 13.63, 7.33 ± 1.70 and 0.14 ± 0.01 μg/(cm2h), respectively. The in vivo anti-inflammatory activity was evaluated by ethyl phenylpropiolate (EPP)-induced rat ear edema (n = 3). DCFD entrapped in the developed elastic niosomes and incorporated in gel gave the same ear edema inhibition percentages of 23.81% at 30 min, but 2 and 9 times more inhibition percentages at 45 and 60 min than the commercial emulgel, respectively. This result has not only demonstrated the enhancement of transdermal absorption through rat skin, but also the in vivo anti-inflammatory effect of DCFD when entrapped in the developed novel elastic Tween 61 niosomes, as well. © 2008 Elsevier B.V. All rights reserved. 2018-09-10T03:47:51Z 2018-09-10T03:47:51Z 2008-08-06 Journal 03785173 2-s2.0-47249114766 10.1016/j.ijpharm.2008.04.033 https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=47249114766&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/60713
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
topic Pharmacology, Toxicology and Pharmaceutics
spellingShingle Pharmacology, Toxicology and Pharmaceutics
A. Manosroi
P. Jantrawut
J. Manosroi
Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium
description The objective of this study was to develop a novel elastic bilayer vesicle entrapped with the non-steroidal anti-inflammatory drug (NSAID), diclofenac diethylammonium (DCFD) for topical use. Eighteen bilayer vesicular formulations composing of DPPC or Tween 61 or Span 60 mixed with cholesterol (at 1:1, 3:7 and 1:1 molar ratios, respectively) and ethanol at 0-25% (v/v), by chloroform film method with sonication were developed. The elastic Tween 61 niosomes which gave no sedimentation, no layer separation, unchanged particle sizes (about 200 nm) were selected to entrap DCFD. The entrapment efficiency of the drug in the conventional and elastic Tween 61 niosomes was 65 and 93%, respectively. At least 87% of DCFD determined by HPLC remained in elastic Tween 61 niosomes when kept at 4, 27 and 45 °C for 3 months. The deformability index values of the elastic niosomes were 13.76 and 3.44 times higher than the conventional niosomes entrapped and not entrapped with the drug, respectively, indicating the higher flexibility of the elastic vesicle especially, when entrapped with the drug. Transdermal absorption through excised rat skin was performed by vertical Franz diffusion cell at 32 ± 2 °C for 6 h. Gel containing elastic niosomes exhibited fluxes of DCFD in the stratum corneum (SC), deeper skin layer (viable epidermis and dermis, VED) and receiver chamber at 191.27 ± 9.52, 16.97 ± 2.77 and 3.76 ± 0.54 μg/(cm2h), whereas the commercial emulgel, containing an equivalent DCFD, gave 60.84 ± 13.63, 7.33 ± 1.70 and 0.14 ± 0.01 μg/(cm2h), respectively. The in vivo anti-inflammatory activity was evaluated by ethyl phenylpropiolate (EPP)-induced rat ear edema (n = 3). DCFD entrapped in the developed elastic niosomes and incorporated in gel gave the same ear edema inhibition percentages of 23.81% at 30 min, but 2 and 9 times more inhibition percentages at 45 and 60 min than the commercial emulgel, respectively. This result has not only demonstrated the enhancement of transdermal absorption through rat skin, but also the in vivo anti-inflammatory effect of DCFD when entrapped in the developed novel elastic Tween 61 niosomes, as well. © 2008 Elsevier B.V. All rights reserved.
format Journal
author A. Manosroi
P. Jantrawut
J. Manosroi
author_facet A. Manosroi
P. Jantrawut
J. Manosroi
author_sort A. Manosroi
title Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium
title_short Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium
title_full Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium
title_fullStr Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium
title_full_unstemmed Anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium
title_sort anti-inflammatory activity of gel containing novel elastic niosomes entrapped with diclofenac diethylammonium
publishDate 2018
url https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=47249114766&origin=inward
http://cmuir.cmu.ac.th/jspui/handle/6653943832/60713
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