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Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model

BACKGROUND: Ethosomes have been widely used in Transdermal Drug Delivery System (TDDS) as they increase the permeation of drug across the skin. METHODS: Flurbiprofen loaded vesicular ethosomes were formulated, optimized and characterized for particle size, entrapment efficiency, poly dispersive inde...

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Autores principales: Paliwal, Sarvesh, Tilak, Amita, Sharma, Jaiprakash, Dave, Vivek, Sharma, Swapnil, Yadav, Renubala, Patel, Saraswati, Verma, Kanika, Tak, Kajal
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6554971/
https://www.ncbi.nlm.nih.gov/pubmed/31170970
http://dx.doi.org/10.1186/s12944-019-1064-x
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author Paliwal, Sarvesh
Tilak, Amita
Sharma, Jaiprakash
Dave, Vivek
Sharma, Swapnil
Yadav, Renubala
Patel, Saraswati
Verma, Kanika
Tak, Kajal
author_facet Paliwal, Sarvesh
Tilak, Amita
Sharma, Jaiprakash
Dave, Vivek
Sharma, Swapnil
Yadav, Renubala
Patel, Saraswati
Verma, Kanika
Tak, Kajal
author_sort Paliwal, Sarvesh
collection PubMed
description BACKGROUND: Ethosomes have been widely used in Transdermal Drug Delivery System (TDDS) as they increase the permeation of drug across the skin. METHODS: Flurbiprofen loaded vesicular ethosomes were formulated, optimized and characterized for particle size, entrapment efficiency, poly dispersive index (PDI), microscopy using Atomic force microscopy (AFM), Scanning electron microscope (SEM) and Transmission electron microscopy (TEM) and Interaction of drug and excipients were studied using Fourier transform infra-red (FTIR) spectroscopy, Differential scanning colorimetry (DSC), Thermo gravimetric analysis (TGA). Further, ethosomal formulations of flurbiprofen were evaluated for stability study of three months and in vitro drug permeation study was carried out using albino rat skin. In addition, skin irritation test was evaluated by Draize test and in vivo study of prepared formulation was examined through paw edema assay by inducing carrageenan and cold plate method. RESULTS: Amongst all formulations, EF5 formulation exhibited ideal surface morphology, with maximum entrapment efficiency (95%) with optimal excipient concentration i.e. 200 mg phospholipid and 35% ethanol. The ideal vesicle size was achieved as 162.2 ± 2 nm, with zeta potential − 48.14 ± 1.4 mV with the PDI of 0.341. In-vitro permeation study shows a release of 82.56 ± 2.11 g/cm(2) in 24 h and transdermal flux was found as 226.1 μg/cm(2)/h. Cold plate test indicates that the formulation EF5 showed a marked analgesic activity and Carrageenan induced paw edema test indicates that the formulation EF5 inhibits the increase in paw edema. Ethosomal suspension at 4 °C showed maximum stability. CONCLUSIONS: The overall study concluded that this ethosomal approach offers a new delivery system for sustained and targeted delivery for flurbiprofen. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1186/s12944-019-1064-x) contains supplementary material, which is available to authorized users.
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spelling pubmed-65549712019-06-10 Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model Paliwal, Sarvesh Tilak, Amita Sharma, Jaiprakash Dave, Vivek Sharma, Swapnil Yadav, Renubala Patel, Saraswati Verma, Kanika Tak, Kajal Lipids Health Dis Research BACKGROUND: Ethosomes have been widely used in Transdermal Drug Delivery System (TDDS) as they increase the permeation of drug across the skin. METHODS: Flurbiprofen loaded vesicular ethosomes were formulated, optimized and characterized for particle size, entrapment efficiency, poly dispersive index (PDI), microscopy using Atomic force microscopy (AFM), Scanning electron microscope (SEM) and Transmission electron microscopy (TEM) and Interaction of drug and excipients were studied using Fourier transform infra-red (FTIR) spectroscopy, Differential scanning colorimetry (DSC), Thermo gravimetric analysis (TGA). Further, ethosomal formulations of flurbiprofen were evaluated for stability study of three months and in vitro drug permeation study was carried out using albino rat skin. In addition, skin irritation test was evaluated by Draize test and in vivo study of prepared formulation was examined through paw edema assay by inducing carrageenan and cold plate method. RESULTS: Amongst all formulations, EF5 formulation exhibited ideal surface morphology, with maximum entrapment efficiency (95%) with optimal excipient concentration i.e. 200 mg phospholipid and 35% ethanol. The ideal vesicle size was achieved as 162.2 ± 2 nm, with zeta potential − 48.14 ± 1.4 mV with the PDI of 0.341. In-vitro permeation study shows a release of 82.56 ± 2.11 g/cm(2) in 24 h and transdermal flux was found as 226.1 μg/cm(2)/h. Cold plate test indicates that the formulation EF5 showed a marked analgesic activity and Carrageenan induced paw edema test indicates that the formulation EF5 inhibits the increase in paw edema. Ethosomal suspension at 4 °C showed maximum stability. CONCLUSIONS: The overall study concluded that this ethosomal approach offers a new delivery system for sustained and targeted delivery for flurbiprofen. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (10.1186/s12944-019-1064-x) contains supplementary material, which is available to authorized users. BioMed Central 2019-06-07 /pmc/articles/PMC6554971/ /pubmed/31170970 http://dx.doi.org/10.1186/s12944-019-1064-x Text en © The Author(s). 2019 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research
Paliwal, Sarvesh
Tilak, Amita
Sharma, Jaiprakash
Dave, Vivek
Sharma, Swapnil
Yadav, Renubala
Patel, Saraswati
Verma, Kanika
Tak, Kajal
Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model
title Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model
title_full Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model
title_fullStr Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model
title_full_unstemmed Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model
title_short Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model
title_sort flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model
topic Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6554971/
https://www.ncbi.nlm.nih.gov/pubmed/31170970
http://dx.doi.org/10.1186/s12944-019-1064-x
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