Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel

Detalhes bibliográficos
Autor(a) principal: Chaud, Marco Vinicius
Data de Publicação: 2010
Outros Autores: Tamascia, Pollyanna, de Lima, Andreäa Cristina [UNESP], Paganelli, Maria Ondina, Gremiäo, Maria Palmira Daflon [UNESP], de Freitas, Osvaldo
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.1590/s1984-82502010000300010
http://hdl.handle.net/11449/231973
Resumo: The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction.
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spelling Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantelPraziquantel/dissolution ratesPraziquantel/intestinal absorptionPraziquantel/solubilitySolid dispersionThe solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction.Department of Pharmaceutical Sciences University of Sorocaba - UNISODepartment of Pharmacy Faculty of Health Sciences Methodist University of PiracicabaDepartment of Drugs and Pharmaceutical Faculty of Pharmaceutical Sciences of Araraquara São Paulo State University Júlio de Mesquita FilhoDepartment of Pharmaceutical Sciences of Ribeirão Preto University of São PauloDepartment of Drugs and Pharmaceutical Faculty of Pharmaceutical Sciences of Araraquara São Paulo State University Júlio de Mesquita FilhoUniversity of Sorocaba - UNISOMethodist University of PiracicabaUniversidade Estadual Paulista (UNESP)Universidade de São Paulo (USP)Chaud, Marco ViniciusTamascia, Pollyannade Lima, Andreäa Cristina [UNESP]Paganelli, Maria OndinaGremiäo, Maria Palmira Daflon [UNESP]de Freitas, Osvaldo2022-04-29T08:48:23Z2022-04-29T08:48:23Z2010-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article473-481http://dx.doi.org/10.1590/s1984-82502010000300010Brazilian Journal of Pharmaceutical Sciences, v. 46, n. 3, p. 473-481, 2010.2175-97901984-8250http://hdl.handle.net/11449/23197310.1590/s1984-825020100003000102-s2.0-78651068892Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengBrazilian Journal of Pharmaceutical Sciencesinfo:eu-repo/semantics/openAccess2024-06-24T13:46:33Zoai:repositorio.unesp.br:11449/231973Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T23:40:46.080222Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
title Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
spellingShingle Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
Chaud, Marco Vinicius
Praziquantel/dissolution rates
Praziquantel/intestinal absorption
Praziquantel/solubility
Solid dispersion
title_short Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
title_full Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
title_fullStr Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
title_full_unstemmed Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
title_sort Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel
author Chaud, Marco Vinicius
author_facet Chaud, Marco Vinicius
Tamascia, Pollyanna
de Lima, Andreäa Cristina [UNESP]
Paganelli, Maria Ondina
Gremiäo, Maria Palmira Daflon [UNESP]
de Freitas, Osvaldo
author_role author
author2 Tamascia, Pollyanna
de Lima, Andreäa Cristina [UNESP]
Paganelli, Maria Ondina
Gremiäo, Maria Palmira Daflon [UNESP]
de Freitas, Osvaldo
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv University of Sorocaba - UNISO
Methodist University of Piracicaba
Universidade Estadual Paulista (UNESP)
Universidade de São Paulo (USP)
dc.contributor.author.fl_str_mv Chaud, Marco Vinicius
Tamascia, Pollyanna
de Lima, Andreäa Cristina [UNESP]
Paganelli, Maria Ondina
Gremiäo, Maria Palmira Daflon [UNESP]
de Freitas, Osvaldo
dc.subject.por.fl_str_mv Praziquantel/dissolution rates
Praziquantel/intestinal absorption
Praziquantel/solubility
Solid dispersion
topic Praziquantel/dissolution rates
Praziquantel/intestinal absorption
Praziquantel/solubility
Solid dispersion
description The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction.
publishDate 2010
dc.date.none.fl_str_mv 2010-01-01
2022-04-29T08:48:23Z
2022-04-29T08:48:23Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://dx.doi.org/10.1590/s1984-82502010000300010
Brazilian Journal of Pharmaceutical Sciences, v. 46, n. 3, p. 473-481, 2010.
2175-9790
1984-8250
http://hdl.handle.net/11449/231973
10.1590/s1984-82502010000300010
2-s2.0-78651068892
url http://dx.doi.org/10.1590/s1984-82502010000300010
http://hdl.handle.net/11449/231973
identifier_str_mv Brazilian Journal of Pharmaceutical Sciences, v. 46, n. 3, p. 473-481, 2010.
2175-9790
1984-8250
10.1590/s1984-82502010000300010
2-s2.0-78651068892
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Brazilian Journal of Pharmaceutical Sciences
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 473-481
dc.source.none.fl_str_mv Scopus
reponame:Repositório Institucional da UNESP
instname:Universidade Estadual Paulista (UNESP)
instacron:UNESP
instname_str Universidade Estadual Paulista (UNESP)
instacron_str UNESP
institution UNESP
reponame_str Repositório Institucional da UNESP
collection Repositório Institucional da UNESP
repository.name.fl_str_mv Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)
repository.mail.fl_str_mv
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