Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Outros Autores: | , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/164772 |
Resumo: | The development and clinical application of 2-methoxyestradiol (2-ME) as a new type of antitumor drug are limited due to its poor solubility, rapid metabolism in vivo, and large oral dosage. 2-ME-loaded pHsensitive liposomes (2-ME-PSLs) was prepared containing the lipids, Lipoid E-80 (E-80), cholesteryl hemisuccinate (CHEMS), and cholesterol (CHOL) via thin-film ultrasonic dispersion. First, preparation conditions of 2-ME-PSLs were optimized by orthogonal test. Then 2-ME-PSL was characterized, and the release behavior and stability of 2-ME-PSL in vitro were evaluated. The optimal preparation conditions for 2-ME-PSLs were as follows: 2-ME : E-80+CHEMS 1:15; CHOL : E-80+CHEMS 1:5; ultrasonication time 20 minutes. The mean particle size, PDI, zeta potential, and entrapment efficiency (EE) of 2-MEPSLs were 116 ± 9 nm, 0.161 ± 0.025, −22.4 ± 1.7 mV, and 98.6 ± 0.5%, respectively. As viewed under a transmission electron microscope, 2-ME-PSLs were well dispersed and almost spherical. They exhibited significant pH-sensitive properties and were fairly stable when diluted with a physiological solution. In conclusion, 2-ME-PSLs were successfully prepared and possessed a favorable pH sensitivity and good dissolution stability with a normal solution. |
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Brazilian Journal of Pharmaceutical Sciences |
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Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes2-MethoxyestradiolpH sensitive liposomesIn vitro releaseStabilityThe development and clinical application of 2-methoxyestradiol (2-ME) as a new type of antitumor drug are limited due to its poor solubility, rapid metabolism in vivo, and large oral dosage. 2-ME-loaded pHsensitive liposomes (2-ME-PSLs) was prepared containing the lipids, Lipoid E-80 (E-80), cholesteryl hemisuccinate (CHEMS), and cholesterol (CHOL) via thin-film ultrasonic dispersion. First, preparation conditions of 2-ME-PSLs were optimized by orthogonal test. Then 2-ME-PSL was characterized, and the release behavior and stability of 2-ME-PSL in vitro were evaluated. The optimal preparation conditions for 2-ME-PSLs were as follows: 2-ME : E-80+CHEMS 1:15; CHOL : E-80+CHEMS 1:5; ultrasonication time 20 minutes. The mean particle size, PDI, zeta potential, and entrapment efficiency (EE) of 2-MEPSLs were 116 ± 9 nm, 0.161 ± 0.025, −22.4 ± 1.7 mV, and 98.6 ± 0.5%, respectively. As viewed under a transmission electron microscope, 2-ME-PSLs were well dispersed and almost spherical. They exhibited significant pH-sensitive properties and were fairly stable when diluted with a physiological solution. In conclusion, 2-ME-PSLs were successfully prepared and possessed a favorable pH sensitivity and good dissolution stability with a normal solution.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2019-12-04info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/16477210.1590/s2175-97902019000118204Brazilian Journal of Pharmaceutical Sciences; Vol. 55 (2019); e18204Brazilian Journal of Pharmaceutical Sciences; v. 55 (2019); e18204Brazilian Journal of Pharmaceutical Sciences; Vol. 55 (2019); e182042175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/164772/157958Copyright (c) 2019 Brazilian Journal of Pharmaceutical Scienceshttp://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessHe, SunaWang, BowenZhang, RunfangZhou, HuanhuanYang, Qian2021-01-11T18:31:44Zoai:revistas.usp.br:article/164772Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2021-01-11T18:31:44Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes |
title |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes |
spellingShingle |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes He, Suna 2-Methoxyestradiol pH sensitive liposomes In vitro release Stability |
title_short |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes |
title_full |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes |
title_fullStr |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes |
title_full_unstemmed |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes |
title_sort |
Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes |
author |
He, Suna |
author_facet |
He, Suna Wang, Bowen Zhang, Runfang Zhou, Huanhuan Yang, Qian |
author_role |
author |
author2 |
Wang, Bowen Zhang, Runfang Zhou, Huanhuan Yang, Qian |
author2_role |
author author author author |
dc.contributor.author.fl_str_mv |
He, Suna Wang, Bowen Zhang, Runfang Zhou, Huanhuan Yang, Qian |
dc.subject.por.fl_str_mv |
2-Methoxyestradiol pH sensitive liposomes In vitro release Stability |
topic |
2-Methoxyestradiol pH sensitive liposomes In vitro release Stability |
description |
The development and clinical application of 2-methoxyestradiol (2-ME) as a new type of antitumor drug are limited due to its poor solubility, rapid metabolism in vivo, and large oral dosage. 2-ME-loaded pHsensitive liposomes (2-ME-PSLs) was prepared containing the lipids, Lipoid E-80 (E-80), cholesteryl hemisuccinate (CHEMS), and cholesterol (CHOL) via thin-film ultrasonic dispersion. First, preparation conditions of 2-ME-PSLs were optimized by orthogonal test. Then 2-ME-PSL was characterized, and the release behavior and stability of 2-ME-PSL in vitro were evaluated. The optimal preparation conditions for 2-ME-PSLs were as follows: 2-ME : E-80+CHEMS 1:15; CHOL : E-80+CHEMS 1:5; ultrasonication time 20 minutes. The mean particle size, PDI, zeta potential, and entrapment efficiency (EE) of 2-MEPSLs were 116 ± 9 nm, 0.161 ± 0.025, −22.4 ± 1.7 mV, and 98.6 ± 0.5%, respectively. As viewed under a transmission electron microscope, 2-ME-PSLs were well dispersed and almost spherical. They exhibited significant pH-sensitive properties and were fairly stable when diluted with a physiological solution. In conclusion, 2-ME-PSLs were successfully prepared and possessed a favorable pH sensitivity and good dissolution stability with a normal solution. |
publishDate |
2019 |
dc.date.none.fl_str_mv |
2019-12-04 |
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/164772 10.1590/s2175-97902019000118204 |
url |
https://www.revistas.usp.br/bjps/article/view/164772 |
identifier_str_mv |
10.1590/s2175-97902019000118204 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/164772/157958 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2019 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2019 Brazilian Journal of Pharmaceutical Sciences http://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. 55 (2019); e18204 Brazilian Journal of Pharmaceutical Sciences; v. 55 (2019); e18204 Brazilian Journal of Pharmaceutical Sciences; Vol. 55 (2019); e18204 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 |
_version_ |
1800222914486730752 |