Complexation and enhancement of temozolomide solubility with cyclodextrins
Autor(a) principal: | |
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Data de Publicação: | 2018 |
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/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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Brazilian Journal of Pharmaceutical Sciences |
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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 |
_version_ |
1800222913733853184 |