Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes

Detalhes bibliográficos
Autor(a) principal: He, Suna
Data de Publicação: 2019
Outros Autores: Wang, Bowen, Zhang, Runfang, Zhou, Huanhuan, Yang, Qian
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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spelling 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
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