In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate

Detalhes bibliográficos
Autor(a) principal: Modi, Chetna
Data de Publicação: 2023
Outros Autores: Bharadia, Praful
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Brazilian Journal of Pharmaceutical Sciences
Texto Completo: https://www.revistas.usp.br/bjps/article/view/212207
Resumo: Methotrexate on its oral and intravenous administration results in unwanted adverse effects. This drawback can be overcome by transdermal delivery because of its painless objective for systemic drug administration. Transfersomes are ultra-deformable vesicles with the flexibility to reach deeper tissues of the skin. The objective of this research work was to develop methotrexate transfersomal gel by thin film hydration technique, evaluated for entrapment efficiency, deformability, mean vesicle size, and stability, and incorporated into carbopol gel for ease of handling and skin applicability for a longer period of retention on skin. MTX-TFS gel & conventional gel were characterized for consistency, transparency, viscosity, and pH. Ex-vivo skin permeation studies were performed using abdominal goat skin and drug release kinetic parameters and transdermal flux were calculated using mathematical models. The results indicate that MTX was successfully entrapped (84.77 ± 2.35 %w/w) in transfersomes having 240±1.6 nm vesicle sizes and 27.13±0.7 deformability index. The gel was permeated through the skin at a rate of 28.12±2.58 µg/cm2/hr as compared to the conventional gel (10.35±2.14 µg/cm2/ hr). From the study, it was concluded that the MTX-TFS gel can be used as a possible substitute for the conventional formulation for transdermal drug delivery due to 3 times improvement in transdermal flux.
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spelling In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of MethotrexateMethotrexateTransfesomesTransdermal fluxSkin permeationEx-vivoMethotrexate on its oral and intravenous administration results in unwanted adverse effects. This drawback can be overcome by transdermal delivery because of its painless objective for systemic drug administration. Transfersomes are ultra-deformable vesicles with the flexibility to reach deeper tissues of the skin. The objective of this research work was to develop methotrexate transfersomal gel by thin film hydration technique, evaluated for entrapment efficiency, deformability, mean vesicle size, and stability, and incorporated into carbopol gel for ease of handling and skin applicability for a longer period of retention on skin. MTX-TFS gel & conventional gel were characterized for consistency, transparency, viscosity, and pH. Ex-vivo skin permeation studies were performed using abdominal goat skin and drug release kinetic parameters and transdermal flux were calculated using mathematical models. The results indicate that MTX was successfully entrapped (84.77 ± 2.35 %w/w) in transfersomes having 240±1.6 nm vesicle sizes and 27.13±0.7 deformability index. The gel was permeated through the skin at a rate of 28.12±2.58 µg/cm2/hr as compared to the conventional gel (10.35±2.14 µg/cm2/ hr). From the study, it was concluded that the MTX-TFS gel can be used as a possible substitute for the conventional formulation for transdermal drug delivery due to 3 times improvement in transdermal flux.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2023-05-22info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/21220710.1590/s2175-97902023e22643 Brazilian Journal of Pharmaceutical Sciences; Vol. 59 (2023)Brazilian Journal of Pharmaceutical Sciences; v. 59 (2023)Brazilian Journal of Pharmaceutical Sciences; Vol. 59 (2023)2175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/212207/194321Copyright (c) 2023 Brazilian Journal of Pharmaceutical Scienceshttps://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessModi, ChetnaBharadia, Praful2023-05-22T14:04:54Zoai:revistas.usp.br:article/212207Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2023-05-22T14:04:54Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false
dc.title.none.fl_str_mv In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
title In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
spellingShingle In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
Modi, Chetna
Methotrexate
Transfesomes
Transdermal flux
Skin permeation
Ex-vivo
title_short In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
title_full In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
title_fullStr In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
title_full_unstemmed In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
title_sort In-Vitro and Ex-Vivo Evaluation of Transfersomal Gel of Methotrexate
author Modi, Chetna
author_facet Modi, Chetna
Bharadia, Praful
author_role author
author2 Bharadia, Praful
author2_role author
dc.contributor.author.fl_str_mv Modi, Chetna
Bharadia, Praful
dc.subject.por.fl_str_mv Methotrexate
Transfesomes
Transdermal flux
Skin permeation
Ex-vivo
topic Methotrexate
Transfesomes
Transdermal flux
Skin permeation
Ex-vivo
description Methotrexate on its oral and intravenous administration results in unwanted adverse effects. This drawback can be overcome by transdermal delivery because of its painless objective for systemic drug administration. Transfersomes are ultra-deformable vesicles with the flexibility to reach deeper tissues of the skin. The objective of this research work was to develop methotrexate transfersomal gel by thin film hydration technique, evaluated for entrapment efficiency, deformability, mean vesicle size, and stability, and incorporated into carbopol gel for ease of handling and skin applicability for a longer period of retention on skin. MTX-TFS gel & conventional gel were characterized for consistency, transparency, viscosity, and pH. Ex-vivo skin permeation studies were performed using abdominal goat skin and drug release kinetic parameters and transdermal flux were calculated using mathematical models. The results indicate that MTX was successfully entrapped (84.77 ± 2.35 %w/w) in transfersomes having 240±1.6 nm vesicle sizes and 27.13±0.7 deformability index. The gel was permeated through the skin at a rate of 28.12±2.58 µg/cm2/hr as compared to the conventional gel (10.35±2.14 µg/cm2/ hr). From the study, it was concluded that the MTX-TFS gel can be used as a possible substitute for the conventional formulation for transdermal drug delivery due to 3 times improvement in transdermal flux.
publishDate 2023
dc.date.none.fl_str_mv 2023-05-22
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://www.revistas.usp.br/bjps/article/view/212207
10.1590/s2175-97902023e22643
url https://www.revistas.usp.br/bjps/article/view/212207
identifier_str_mv 10.1590/s2175-97902023e22643
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv https://www.revistas.usp.br/bjps/article/view/212207/194321
dc.rights.driver.fl_str_mv Copyright (c) 2023 Brazilian Journal of Pharmaceutical Sciences
https://creativecommons.org/licenses/by/4.0
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Copyright (c) 2023 Brazilian Journal of Pharmaceutical Sciences
https://creativecommons.org/licenses/by/4.0
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
publisher.none.fl_str_mv Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
dc.source.none.fl_str_mv Brazilian Journal of Pharmaceutical Sciences; Vol. 59 (2023)
Brazilian Journal of Pharmaceutical Sciences; v. 59 (2023)
Brazilian Journal of Pharmaceutical Sciences; Vol. 59 (2023)
2175-9790
1984-8250
reponame:Brazilian Journal of Pharmaceutical Sciences
instname:Universidade de São Paulo (USP)
instacron:USP
instname_str Universidade de São Paulo (USP)
instacron_str USP
institution USP
reponame_str Brazilian Journal of Pharmaceutical Sciences
collection Brazilian Journal of Pharmaceutical Sciences
repository.name.fl_str_mv Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)
repository.mail.fl_str_mv bjps@usp.br||elizabeth.igne@gmail.com
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