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Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study

INTRODUCTION: Ketorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug, when given orally causes gastrointestinal disturbances. Its transdermal drug delivery may reduce such side effects associated with them. The present investigation was aimed at evaluating the efficiency of various penet...

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Autores principales: Kumar, Pawan, Singh, Shailendra Kumar, Mishra, Dina Nath, Girotra, Priti
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4522863/
https://www.ncbi.nlm.nih.gov/pubmed/26258055
http://dx.doi.org/10.4103/2230-973X.160850
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author Kumar, Pawan
Singh, Shailendra Kumar
Mishra, Dina Nath
Girotra, Priti
author_facet Kumar, Pawan
Singh, Shailendra Kumar
Mishra, Dina Nath
Girotra, Priti
author_sort Kumar, Pawan
collection PubMed
description INTRODUCTION: Ketorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug, when given orally causes gastrointestinal disturbances. Its transdermal drug delivery may reduce such side effects associated with them. The present investigation was aimed at evaluating the efficiency of various penetration enhancers for improved permeation of KT through the skin. MATERIALS AND METHODS: A concentration of 1 mg/mL of the drug solution with enhancers was used to evaluate diffusion through the rat skin using a Franz diffusion cell assembly. 20 different penetration enhancers were selected for this study. RESULTS: Saturated fatty acids like stearic and palmitic acid were found to increase the permeation rate of the drug to a great extent whereas unsaturated fatty acid viz. oleic acid exhibited maximum permeation. Increase in permeability efficiency of various penetration enhancers was observed in the following order: Oleic acid > stearic acid > palmitic acid > isopropyl myristate > tween 80 > span 80 > span 40 > span 20 > l-limonene > l-menthol > fenchone > α-pinene > urea > dimethyl sulfoxide (DMSO) > triton X-100 > tween 20 > dimethyl formamide > acetone > control > citric acid > ascorbic acid. Ascorbic acid and citric acid had no effect on permeation rate. CONCLUSION: The results revealed that the permeation of KT through the skin can maximally be enhanced using oleic acid-an unsaturated fatty acid.
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spelling pubmed-45228632015-08-07 Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study Kumar, Pawan Singh, Shailendra Kumar Mishra, Dina Nath Girotra, Priti Int J Pharm Investig Original Research Article INTRODUCTION: Ketorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug, when given orally causes gastrointestinal disturbances. Its transdermal drug delivery may reduce such side effects associated with them. The present investigation was aimed at evaluating the efficiency of various penetration enhancers for improved permeation of KT through the skin. MATERIALS AND METHODS: A concentration of 1 mg/mL of the drug solution with enhancers was used to evaluate diffusion through the rat skin using a Franz diffusion cell assembly. 20 different penetration enhancers were selected for this study. RESULTS: Saturated fatty acids like stearic and palmitic acid were found to increase the permeation rate of the drug to a great extent whereas unsaturated fatty acid viz. oleic acid exhibited maximum permeation. Increase in permeability efficiency of various penetration enhancers was observed in the following order: Oleic acid > stearic acid > palmitic acid > isopropyl myristate > tween 80 > span 80 > span 40 > span 20 > l-limonene > l-menthol > fenchone > α-pinene > urea > dimethyl sulfoxide (DMSO) > triton X-100 > tween 20 > dimethyl formamide > acetone > control > citric acid > ascorbic acid. Ascorbic acid and citric acid had no effect on permeation rate. CONCLUSION: The results revealed that the permeation of KT through the skin can maximally be enhanced using oleic acid-an unsaturated fatty acid. Medknow Publications & Media Pvt Ltd 2015 /pmc/articles/PMC4522863/ /pubmed/26258055 http://dx.doi.org/10.4103/2230-973X.160850 Text en Copyright: © International Journal of Pharmaceutical Investigation http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Research Article
Kumar, Pawan
Singh, Shailendra Kumar
Mishra, Dina Nath
Girotra, Priti
Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study
title Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study
title_full Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study
title_fullStr Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study
title_full_unstemmed Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study
title_short Enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: An ex-vivo study
title_sort enhancement of ketorolac tromethamine permeability through rat skin using penetration enhancers: an ex-vivo study
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4522863/
https://www.ncbi.nlm.nih.gov/pubmed/26258055
http://dx.doi.org/10.4103/2230-973X.160850
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