In situ microemulsion-gel obtained from bioadhesive hydroxypropyl methylcellulose films for transdermal administration of zidovudine

[Display omitted] •In situ microemulsion-gel (ME-Gel) was obtained for the first time from a polymeric film.•HPMC films were able to promote the formation of a ME-Gel at the application site.•In situ ME-Gel showed significant permeation-enhancing effect.•In situ ME-Gel was shown to be a promising sy...

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Veröffentlicht in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2020-04, Vol.188, p.110739-110739, Article 110739
Hauptverfasser: Souza de Araujo, Guilherme Rodolfo, de Oliveira Porfírio, Leandro, Santos Silva, Luiz André, Gomes Santana, Danielle, Ferreira Barbosa, Paula, Pereira dos Santos, Cochiran, Narain, Narendra, Vitorino Sarmento, Victor Hugo, de Souza Nunes, Rogéria, Ting, Elizabeth, Moreira Lira, Ana Amélia
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container_title Colloids and surfaces, B, Biointerfaces
container_volume 188
creator Souza de Araujo, Guilherme Rodolfo
de Oliveira Porfírio, Leandro
Santos Silva, Luiz André
Gomes Santana, Danielle
Ferreira Barbosa, Paula
Pereira dos Santos, Cochiran
Narain, Narendra
Vitorino Sarmento, Victor Hugo
de Souza Nunes, Rogéria
Ting, Elizabeth
Moreira Lira, Ana Amélia
description [Display omitted] •In situ microemulsion-gel (ME-Gel) was obtained for the first time from a polymeric film.•HPMC films were able to promote the formation of a ME-Gel at the application site.•In situ ME-Gel showed significant permeation-enhancing effect.•In situ ME-Gel was shown to be a promising system for transdermal release of drugs. This study aims to develop in situ microemulsion-gel (ME-Gel) obtained from hydroxypropyl methylcellulose (HPMC) films for transdermal administration of Zidovudine (AZT). Firstly, HPMC films containing propylene glycol (PG) and eucalyptus oil (EO) were obtained and characterized. Later, a pseudo-ternary phase diagram composed of water, EO, tween 80 and PG was obtained and one microemulsion (ME) with a similar proportion of the film components was obtained. ME was transformed in ME-Gel by the incorporation of HPMC. Finally, HPMC films were hydrated with Tween 80 solution to yield in situ ME-Gel and its effect on AZT skin permeation was compared with HPMC film hydrated with water (F5hyd). The results showed that the ME and ME-Gel presented a droplet size of 16.79 and 122.13 μm, respectively, polydispersity index (PDI) < 0.39 and pH between 5.10 and 5.40. The incorporation of HPMC resulted in viscosity about 2 times higher than the use of ME. The presence of AZT did not alter the formulation properties. The in situ ME-Gel promoted a two-fold increase in the permeated amount of AZT compared to F5hyd. The results suggest that it was possible to obtain an ME-Gel in situ from HPMC films and that its effect on transdermal permeation of AZT was significant.
doi_str_mv 10.1016/j.colsurfb.2019.110739
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This study aims to develop in situ microemulsion-gel (ME-Gel) obtained from hydroxypropyl methylcellulose (HPMC) films for transdermal administration of Zidovudine (AZT). Firstly, HPMC films containing propylene glycol (PG) and eucalyptus oil (EO) were obtained and characterized. Later, a pseudo-ternary phase diagram composed of water, EO, tween 80 and PG was obtained and one microemulsion (ME) with a similar proportion of the film components was obtained. ME was transformed in ME-Gel by the incorporation of HPMC. Finally, HPMC films were hydrated with Tween 80 solution to yield in situ ME-Gel and its effect on AZT skin permeation was compared with HPMC film hydrated with water (F5hyd). The results showed that the ME and ME-Gel presented a droplet size of 16.79 and 122.13 μm, respectively, polydispersity index (PDI) &lt; 0.39 and pH between 5.10 and 5.40. The incorporation of HPMC resulted in viscosity about 2 times higher than the use of ME. The presence of AZT did not alter the formulation properties. The in situ ME-Gel promoted a two-fold increase in the permeated amount of AZT compared to F5hyd. The results suggest that it was possible to obtain an ME-Gel in situ from HPMC films and that its effect on transdermal permeation of AZT was significant.</description><identifier>ISSN: 0927-7765</identifier><identifier>EISSN: 1873-4367</identifier><identifier>DOI: 10.1016/j.colsurfb.2019.110739</identifier><identifier>PMID: 31901623</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Eucalyptus oil ; Microemulsion ; Microemulsion-gel ; Polymer ; Transdermal film ; Zidovudine</subject><ispartof>Colloids and surfaces, B, Biointerfaces, 2020-04, Vol.188, p.110739-110739, Article 110739</ispartof><rights>2019 Elsevier B.V.</rights><rights>Copyright © 2019 Elsevier B.V. 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This study aims to develop in situ microemulsion-gel (ME-Gel) obtained from hydroxypropyl methylcellulose (HPMC) films for transdermal administration of Zidovudine (AZT). Firstly, HPMC films containing propylene glycol (PG) and eucalyptus oil (EO) were obtained and characterized. Later, a pseudo-ternary phase diagram composed of water, EO, tween 80 and PG was obtained and one microemulsion (ME) with a similar proportion of the film components was obtained. ME was transformed in ME-Gel by the incorporation of HPMC. Finally, HPMC films were hydrated with Tween 80 solution to yield in situ ME-Gel and its effect on AZT skin permeation was compared with HPMC film hydrated with water (F5hyd). The results showed that the ME and ME-Gel presented a droplet size of 16.79 and 122.13 μm, respectively, polydispersity index (PDI) &lt; 0.39 and pH between 5.10 and 5.40. The incorporation of HPMC resulted in viscosity about 2 times higher than the use of ME. The presence of AZT did not alter the formulation properties. The in situ ME-Gel promoted a two-fold increase in the permeated amount of AZT compared to F5hyd. The results suggest that it was possible to obtain an ME-Gel in situ from HPMC films and that its effect on transdermal permeation of AZT was significant.</description><subject>Eucalyptus oil</subject><subject>Microemulsion</subject><subject>Microemulsion-gel</subject><subject>Polymer</subject><subject>Transdermal film</subject><subject>Zidovudine</subject><issn>0927-7765</issn><issn>1873-4367</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><recordid>eNqFUUtv1DAQthCILqV_ofKRSxY_Eju5gSpoK1XiAmfLscddr-x4sZMV6Zkfjlfbcu1ppNE3870QuqZkSwkVn_dbk0JZshu3jNBhSymRfHiDNrSXvGm5kG_RhgxMNlKK7gJ9KGVPCGEtle_RBadDfcL4Bv29n3Dx84KjNzlBXELxaWoeIeA0ztpPYLHLKeLRJ213UPwR8G61Of1ZDzkd1oAjzLs1GAhhCakAdj7Egl3KeM56KhZy1AFrG_3kS13NlQAnh5-8TcfFVoqP6J3TocDV87xEv75_-3lz1zz8uL2_-frQGC76ueGSDBxEzyyTVAjLq4PWjG7sQHSSd86Zric9p1JLZoTjtCOOUuGE6FvaDfwSfTr_rcp_L1BmFX05CdcTpKUoxjkfOGkJq1BxhtZUSsng1CH7qPOqKFGnBtRevTSgTg2ocwP18PqZYxkj2P9nL5FXwJczAKrTo4esivEwGbA-g5mVTf41jn_K8J4A</recordid><startdate>202004</startdate><enddate>202004</enddate><creator>Souza de Araujo, Guilherme Rodolfo</creator><creator>de Oliveira Porfírio, Leandro</creator><creator>Santos Silva, Luiz André</creator><creator>Gomes Santana, Danielle</creator><creator>Ferreira Barbosa, Paula</creator><creator>Pereira dos Santos, Cochiran</creator><creator>Narain, Narendra</creator><creator>Vitorino Sarmento, Victor Hugo</creator><creator>de Souza Nunes, Rogéria</creator><creator>Ting, Elizabeth</creator><creator>Moreira Lira, Ana Amélia</creator><general>Elsevier B.V</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0001-6882-002X</orcidid><orcidid>https://orcid.org/0000-0003-3451-9049</orcidid></search><sort><creationdate>202004</creationdate><title>In situ microemulsion-gel obtained from bioadhesive hydroxypropyl methylcellulose films for transdermal administration of zidovudine</title><author>Souza de Araujo, Guilherme Rodolfo ; de Oliveira Porfírio, Leandro ; Santos Silva, Luiz André ; Gomes Santana, Danielle ; Ferreira Barbosa, Paula ; Pereira dos Santos, Cochiran ; Narain, Narendra ; Vitorino Sarmento, Victor Hugo ; de Souza Nunes, Rogéria ; Ting, Elizabeth ; Moreira Lira, Ana Amélia</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c368t-37093e682d27166d36234cbfb5e65735ffc5808317a72c6f3150f116f66841593</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Eucalyptus oil</topic><topic>Microemulsion</topic><topic>Microemulsion-gel</topic><topic>Polymer</topic><topic>Transdermal film</topic><topic>Zidovudine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Souza de Araujo, Guilherme Rodolfo</creatorcontrib><creatorcontrib>de Oliveira Porfírio, Leandro</creatorcontrib><creatorcontrib>Santos Silva, Luiz André</creatorcontrib><creatorcontrib>Gomes Santana, Danielle</creatorcontrib><creatorcontrib>Ferreira Barbosa, Paula</creatorcontrib><creatorcontrib>Pereira dos Santos, Cochiran</creatorcontrib><creatorcontrib>Narain, Narendra</creatorcontrib><creatorcontrib>Vitorino Sarmento, Victor Hugo</creatorcontrib><creatorcontrib>de Souza Nunes, Rogéria</creatorcontrib><creatorcontrib>Ting, Elizabeth</creatorcontrib><creatorcontrib>Moreira Lira, Ana Amélia</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Souza de Araujo, Guilherme Rodolfo</au><au>de Oliveira Porfírio, Leandro</au><au>Santos Silva, Luiz André</au><au>Gomes Santana, Danielle</au><au>Ferreira Barbosa, Paula</au><au>Pereira dos Santos, Cochiran</au><au>Narain, Narendra</au><au>Vitorino Sarmento, Victor Hugo</au><au>de Souza Nunes, Rogéria</au><au>Ting, Elizabeth</au><au>Moreira Lira, Ana Amélia</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In situ microemulsion-gel obtained from bioadhesive hydroxypropyl methylcellulose films for transdermal administration of zidovudine</atitle><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle><addtitle>Colloids Surf B Biointerfaces</addtitle><date>2020-04</date><risdate>2020</risdate><volume>188</volume><spage>110739</spage><epage>110739</epage><pages>110739-110739</pages><artnum>110739</artnum><issn>0927-7765</issn><eissn>1873-4367</eissn><abstract>[Display omitted] •In situ microemulsion-gel (ME-Gel) was obtained for the first time from a polymeric film.•HPMC films were able to promote the formation of a ME-Gel at the application site.•In situ ME-Gel showed significant permeation-enhancing effect.•In situ ME-Gel was shown to be a promising system for transdermal release of drugs. This study aims to develop in situ microemulsion-gel (ME-Gel) obtained from hydroxypropyl methylcellulose (HPMC) films for transdermal administration of Zidovudine (AZT). Firstly, HPMC films containing propylene glycol (PG) and eucalyptus oil (EO) were obtained and characterized. Later, a pseudo-ternary phase diagram composed of water, EO, tween 80 and PG was obtained and one microemulsion (ME) with a similar proportion of the film components was obtained. ME was transformed in ME-Gel by the incorporation of HPMC. Finally, HPMC films were hydrated with Tween 80 solution to yield in situ ME-Gel and its effect on AZT skin permeation was compared with HPMC film hydrated with water (F5hyd). The results showed that the ME and ME-Gel presented a droplet size of 16.79 and 122.13 μm, respectively, polydispersity index (PDI) &lt; 0.39 and pH between 5.10 and 5.40. The incorporation of HPMC resulted in viscosity about 2 times higher than the use of ME. The presence of AZT did not alter the formulation properties. The in situ ME-Gel promoted a two-fold increase in the permeated amount of AZT compared to F5hyd. The results suggest that it was possible to obtain an ME-Gel in situ from HPMC films and that its effect on transdermal permeation of AZT was significant.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>31901623</pmid><doi>10.1016/j.colsurfb.2019.110739</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0001-6882-002X</orcidid><orcidid>https://orcid.org/0000-0003-3451-9049</orcidid></addata></record>
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subjects Eucalyptus oil
Microemulsion
Microemulsion-gel
Polymer
Transdermal film
Zidovudine
title In situ microemulsion-gel obtained from bioadhesive hydroxypropyl methylcellulose films for transdermal administration of zidovudine
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