The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds

Detalhes bibliográficos
Autor(a) principal: Caparica, Rita
Data de Publicação: 2017
Tipo de documento: Dissertação
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10437/8377
Resumo: The pharmaceutical industry has developed alternative forms of drug delivery over the years and the delivery through the skin, topical or transdermal delivery, has been increasingly used. However, incorporating poorly soluble or partially insoluble drugs into the developed delivery systems has been difficult to solve. Ionic liquids have specific properties, arising from their structure, which allows them to be used in aqueous, oily or hydroalcoholic solutions. Hence, ionic liquids can be used as excipients with the aim of increasing/improving the topical and transdermal delivery of drugs. Herein, the efficacy of ionic liquids derived from amino acids, [Cho][Phe] and [Cho][Glu], as solubility and/or permeation promoters of poorly soluble actives were evaluated. The studied actives were ferulic acid and rutin, both natural antioxidant compounds, with low solubility, which restricts their use in topical and dermocosmetic products, since they require the use of high proportions of organic solvents. The solubility studies carried out showed that the solubility of both active compounds is always increased in the presence of the prepared ionic liquids in all the studied conditions. Regarding the permeation studies, the ionic liquids did not shown a significant effect on the permeation of the studied actives. The obtained results indicate that the ionic liquids studied can be efficient functional ingredients, since they allow an increase in the solubility of the studied actives, even at low concentrations of the studied ionic liquids.
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spelling The influence of ionic liquids on the solubility/permeation of poorly soluble active compoundsMESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICASCIÊNCIAS FARMACÊUTICASFARMACOLOGIALÍQUIDOS IÓNICOSSOLUBILIDADESISTEMAS DE LIBERTAÇÃO DE MEDICAMENTOSPHARMACEUTICAL SCIENCESPHARMACOLOGYIONIC LIQUIDSSOLUBILITYDRUG DELIVERY SYSTEMSThe pharmaceutical industry has developed alternative forms of drug delivery over the years and the delivery through the skin, topical or transdermal delivery, has been increasingly used. However, incorporating poorly soluble or partially insoluble drugs into the developed delivery systems has been difficult to solve. Ionic liquids have specific properties, arising from their structure, which allows them to be used in aqueous, oily or hydroalcoholic solutions. Hence, ionic liquids can be used as excipients with the aim of increasing/improving the topical and transdermal delivery of drugs. Herein, the efficacy of ionic liquids derived from amino acids, [Cho][Phe] and [Cho][Glu], as solubility and/or permeation promoters of poorly soluble actives were evaluated. The studied actives were ferulic acid and rutin, both natural antioxidant compounds, with low solubility, which restricts their use in topical and dermocosmetic products, since they require the use of high proportions of organic solvents. The solubility studies carried out showed that the solubility of both active compounds is always increased in the presence of the prepared ionic liquids in all the studied conditions. Regarding the permeation studies, the ionic liquids did not shown a significant effect on the permeation of the studied actives. The obtained results indicate that the ionic liquids studied can be efficient functional ingredients, since they allow an increase in the solubility of the studied actives, even at low concentrations of the studied ionic liquids.A indústria farmacêutica ao longo dos anos tem vindo a desenvolver formas alternativas de veicular fármacos. A veiculação através da pele, veiculação tópica ou trandérmica, tem vindo a ser cada vez mais utilizada. No entanto, a dificuldade de incorporar fármacos pouco solúveis ou parcialmente insolúveis, nos sistemas de veiculação desenvolvidos, tem sido difícil de solucionar. Os líquidos iónicos têm características específicas, provenientes da sua estrutura, que permite que estes possam ser utilizados em soluções aquosas, oleosas ou hidroalcoólicas. Desta forma, os líquidos iónicos podem ser utilizados como excipientes em formulações tópicas com o objetivo de aumentar/melhorar a veiculação tópica e transdérmica de fármacos. No âmbito deste trabalho, foi avaliada a eficácia de líquidos iónicos derivados de aminoácidos, [Cho][Phe] e [Cho][Glu], como promotores da solubilidade e/ou da permeação de ativos pouco solúveis. Os ativos estudados foram o ácido ferúlico e a rutina, ambos compostos antioxidantes naturais, com baixa solubilidade, o que restringe a sua utilização em produtos tópicos e dermocosméticos, por exigirem a utilização de altas proporções de solventes orgânicos. Os estudos de solubilidade realizados permitiram demonstrar que a solubilidade de ambos os ativos é sempre aumentada na presença dos líquidos iónicos preparados, em todas as condições analisadas. Relativamente aos estudos de permeação, os líquidos iónicos não demonstraram ter um efeito significativo na permeação dos ativos estudados. Os resultados obtidos indicam que os líquidos iónicos estudados podem ser eficientes ingredientes funcionais, uma vez que permitem um aumento da solubilidade dos ativos estudados, mesmo a baixas concentrações de líquido iónico.2017-12-28T12:03:42Z2017-01-01T00:00:00Z2017info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfhttp://hdl.handle.net/10437/8377TID:201766469engCaparica, Ritainfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-03-09T14:06:37Zoai:recil.ensinolusofona.pt:10437/8377Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T17:14:07.762589Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
title The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
spellingShingle The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
Caparica, Rita
MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS
CIÊNCIAS FARMACÊUTICAS
FARMACOLOGIA
LÍQUIDOS IÓNICOS
SOLUBILIDADE
SISTEMAS DE LIBERTAÇÃO DE MEDICAMENTOS
PHARMACEUTICAL SCIENCES
PHARMACOLOGY
IONIC LIQUIDS
SOLUBILITY
DRUG DELIVERY SYSTEMS
title_short The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
title_full The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
title_fullStr The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
title_full_unstemmed The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
title_sort The influence of ionic liquids on the solubility/permeation of poorly soluble active compounds
author Caparica, Rita
author_facet Caparica, Rita
author_role author
dc.contributor.author.fl_str_mv Caparica, Rita
dc.subject.por.fl_str_mv MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS
CIÊNCIAS FARMACÊUTICAS
FARMACOLOGIA
LÍQUIDOS IÓNICOS
SOLUBILIDADE
SISTEMAS DE LIBERTAÇÃO DE MEDICAMENTOS
PHARMACEUTICAL SCIENCES
PHARMACOLOGY
IONIC LIQUIDS
SOLUBILITY
DRUG DELIVERY SYSTEMS
topic MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS
CIÊNCIAS FARMACÊUTICAS
FARMACOLOGIA
LÍQUIDOS IÓNICOS
SOLUBILIDADE
SISTEMAS DE LIBERTAÇÃO DE MEDICAMENTOS
PHARMACEUTICAL SCIENCES
PHARMACOLOGY
IONIC LIQUIDS
SOLUBILITY
DRUG DELIVERY SYSTEMS
description The pharmaceutical industry has developed alternative forms of drug delivery over the years and the delivery through the skin, topical or transdermal delivery, has been increasingly used. However, incorporating poorly soluble or partially insoluble drugs into the developed delivery systems has been difficult to solve. Ionic liquids have specific properties, arising from their structure, which allows them to be used in aqueous, oily or hydroalcoholic solutions. Hence, ionic liquids can be used as excipients with the aim of increasing/improving the topical and transdermal delivery of drugs. Herein, the efficacy of ionic liquids derived from amino acids, [Cho][Phe] and [Cho][Glu], as solubility and/or permeation promoters of poorly soluble actives were evaluated. The studied actives were ferulic acid and rutin, both natural antioxidant compounds, with low solubility, which restricts their use in topical and dermocosmetic products, since they require the use of high proportions of organic solvents. The solubility studies carried out showed that the solubility of both active compounds is always increased in the presence of the prepared ionic liquids in all the studied conditions. Regarding the permeation studies, the ionic liquids did not shown a significant effect on the permeation of the studied actives. The obtained results indicate that the ionic liquids studied can be efficient functional ingredients, since they allow an increase in the solubility of the studied actives, even at low concentrations of the studied ionic liquids.
publishDate 2017
dc.date.none.fl_str_mv 2017-12-28T12:03:42Z
2017-01-01T00:00:00Z
2017
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
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dc.identifier.uri.fl_str_mv http://hdl.handle.net/10437/8377
TID:201766469
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