Complexation and enhancement of temozolomide solubility with cyclodextrins

Detalhes bibliográficos
Autor(a) principal: Gürten, Berna
Data de Publicação: 2018
Outros Autores: Yenigül, Elçin, Sezer, Ali Demir, Malta, Seyda
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Brazilian Journal of Pharmaceutical Sciences
Texto Completo: https://www.revistas.usp.br/bjps/article/view/153802
Resumo: Temozolomide is a poorly soluble anti-cancer drug used in the treatment of some brain cancers. Following literature reports about the enhancement of solubility and stability for these kinds of drugs upon complexation with cyclodextrins, we aimed to form an inclusion complex between temozolomide and the different types of cyclodextrins (CDs) to enhance its solubility. In this study, three different cyclodextrins (β-CD, hydroxyl-β-CD and γ-CD) were used, and changes in solubility was measured by UV-Vis Spectroscopy and HPLC. Morphological changes upon complexation were shown by the Scanning Electron Microscope (SEM), and weight loss profiles with respect to temperatures which were unique to the compounds were shown by Thermogravimetric Analysis. Changes in heat release profiles were shown by Differential Scanning Calorimeter (DSC). Drug solubility was measured to be increased to around 25% for 1:1 molar ratio for all used CD complexations. Changes of morphology, heat release and weight loss profiles are consistent with the formation of an inclusion complex between CDs and temozolomide. In this study, success was shown in the enhancement of temozolomide solubility upon complexation with different types of CDs. It has been demonstrated that cyclodextrins can be used as complexing agents for poorly soluble anti-cancer drugs, increasing their solubility and hence drug availability
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spelling Complexation and enhancement of temozolomide solubility with cyclodextrinsTemozolomide/solubility/complexationCyclodextrinsChromatographyCalorimetryTemozolomide is a poorly soluble anti-cancer drug used in the treatment of some brain cancers. Following literature reports about the enhancement of solubility and stability for these kinds of drugs upon complexation with cyclodextrins, we aimed to form an inclusion complex between temozolomide and the different types of cyclodextrins (CDs) to enhance its solubility. In this study, three different cyclodextrins (β-CD, hydroxyl-β-CD and γ-CD) were used, and changes in solubility was measured by UV-Vis Spectroscopy and HPLC. Morphological changes upon complexation were shown by the Scanning Electron Microscope (SEM), and weight loss profiles with respect to temperatures which were unique to the compounds were shown by Thermogravimetric Analysis. Changes in heat release profiles were shown by Differential Scanning Calorimeter (DSC). Drug solubility was measured to be increased to around 25% for 1:1 molar ratio for all used CD complexations. Changes of morphology, heat release and weight loss profiles are consistent with the formation of an inclusion complex between CDs and temozolomide. In this study, success was shown in the enhancement of temozolomide solubility upon complexation with different types of CDs. It has been demonstrated that cyclodextrins can be used as complexing agents for poorly soluble anti-cancer drugs, increasing their solubility and hence drug availabilityUniversidade de São Paulo. Faculdade de Ciências Farmacêuticas2018-07-26info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/15380210.1590/s2175-97902018000217513Brazilian Journal of Pharmaceutical Sciences; Vol. 54 Núm. 2 (2018); e17513Brazilian Journal of Pharmaceutical Sciences; v. 54 n. 2 (2018); e17513Brazilian Journal of Pharmaceutical Sciences; Vol. 54 No. 2 (2018); e175132175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/153802/150185Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)info:eu-repo/semantics/openAccessGürten, BernaYenigül, ElçinSezer, Ali DemirMalta, Seyda2019-03-17T13:56:54Zoai:revistas.usp.br:article/153802Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2019-03-17T13:56:54Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false
dc.title.none.fl_str_mv Complexation and enhancement of temozolomide solubility with cyclodextrins
title Complexation and enhancement of temozolomide solubility with cyclodextrins
spellingShingle Complexation and enhancement of temozolomide solubility with cyclodextrins
Gürten, Berna
Temozolomide/solubility/complexation
Cyclodextrins
Chromatography
Calorimetry
title_short Complexation and enhancement of temozolomide solubility with cyclodextrins
title_full Complexation and enhancement of temozolomide solubility with cyclodextrins
title_fullStr Complexation and enhancement of temozolomide solubility with cyclodextrins
title_full_unstemmed Complexation and enhancement of temozolomide solubility with cyclodextrins
title_sort Complexation and enhancement of temozolomide solubility with cyclodextrins
author Gürten, Berna
author_facet Gürten, Berna
Yenigül, Elçin
Sezer, Ali Demir
Malta, Seyda
author_role author
author2 Yenigül, Elçin
Sezer, Ali Demir
Malta, Seyda
author2_role author
author
author
dc.contributor.author.fl_str_mv Gürten, Berna
Yenigül, Elçin
Sezer, Ali Demir
Malta, Seyda
dc.subject.por.fl_str_mv Temozolomide/solubility/complexation
Cyclodextrins
Chromatography
Calorimetry
topic Temozolomide/solubility/complexation
Cyclodextrins
Chromatography
Calorimetry
description Temozolomide is a poorly soluble anti-cancer drug used in the treatment of some brain cancers. Following literature reports about the enhancement of solubility and stability for these kinds of drugs upon complexation with cyclodextrins, we aimed to form an inclusion complex between temozolomide and the different types of cyclodextrins (CDs) to enhance its solubility. In this study, three different cyclodextrins (β-CD, hydroxyl-β-CD and γ-CD) were used, and changes in solubility was measured by UV-Vis Spectroscopy and HPLC. Morphological changes upon complexation were shown by the Scanning Electron Microscope (SEM), and weight loss profiles with respect to temperatures which were unique to the compounds were shown by Thermogravimetric Analysis. Changes in heat release profiles were shown by Differential Scanning Calorimeter (DSC). Drug solubility was measured to be increased to around 25% for 1:1 molar ratio for all used CD complexations. Changes of morphology, heat release and weight loss profiles are consistent with the formation of an inclusion complex between CDs and temozolomide. In this study, success was shown in the enhancement of temozolomide solubility upon complexation with different types of CDs. It has been demonstrated that cyclodextrins can be used as complexing agents for poorly soluble anti-cancer drugs, increasing their solubility and hence drug availability
publishDate 2018
dc.date.none.fl_str_mv 2018-07-26
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/153802
10.1590/s2175-97902018000217513
url https://www.revistas.usp.br/bjps/article/view/153802
identifier_str_mv 10.1590/s2175-97902018000217513
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv https://www.revistas.usp.br/bjps/article/view/153802/150185
dc.rights.driver.fl_str_mv Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)
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. 54 Núm. 2 (2018); e17513
Brazilian Journal of Pharmaceutical Sciences; v. 54 n. 2 (2018); e17513
Brazilian Journal of Pharmaceutical Sciences; Vol. 54 No. 2 (2018); e17513
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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