Líquidos iónicos como uma vantagem em transferossomas contendo rutina
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2023
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A administração tópica de fármacos para o tratamento de diversas patologias tem-se revelado muito atrativa pois pode representar menos efeitos adversos associados a um bom desempenho dos princípios ativos, mesmo os pouco solúveis em água. Para tal, o estudo de novas formulações promissoras, eficientes e com o melhor desempenho possível associado a uma boa estabilidade é incessante.
Os líquidos iónicos (LI) têm sido amplamente estudados como promotores da solubilidade, estabilidade e desempenho de diversas formulações cutâneas. Em particular, LI com catião de colina ou de imidazol têm-se demonstrado bastante promissores para modular as propriedades de nanossistemas de veiculação.
Assim, este estudo teve como principal objetivo avaliar o impacto da inclusão de LI em transferossomas em termos das suas propriedades físico-químicas e da sua estabilidade coloidal. Para tal, procedeu-se ao estudo da incorporação de três LI, nomeadamente [Cho][Gly], [Emim][Gly] e [Emim][Br] e das suas misturas, em formulações transferossomais contendo rutina, um bioflavonóide promissor pelas suas propriedades pleiotrópicas com potencial para aplicação tópica. O carácter inovador deste trabalho reside ainda na utilização de um método de produção inovador quanto à fase em que os LI foram incorporados no nanossistema vesicular.
Os resultados obtidos revelam que os LI melhoraram consideravelmente a eficiência de associação (AE) e a capacidade de carga (LC) da rutina, assim como o potencial zeta (ZP) das vesículas, diminuindo o tamanho dos transferossomas. Entre os LI estudados, os LI de glicinato revelaram ser os mais promissores para melhorar as características físico-químicas dos transferossomas, como o LC e o ZP. Mais ainda, o método de produção utilizado neste trabalho permitiu melhorar a estabilidade coloidal das formulações transferossomais armazenadas sob refrigeração durante 30 dias.
Assim, este trabalho demonstrou que, de facto, a incorporação de LI em transferossomas contendo rutina pode ser vantajosa. Por outro lado, a escolha do método de produção destes nanossistemas deve ser criteriosa para se obterem transferossomas com as melhores propriedades possíveis. No geral, os nanossistemas vesiculares desenvolvidos são promissores para veicular compostos ativos destinados à administração tópica.
Palavras-chave: Líquidos iónicos, transferossomas, rutina, sistemas vesiculares
The topical administration of drugs for the treatment of various pathologies has proven to be very attractive because it may represent fewer adverse effects associated with a good performance of the active compounds, even those poorly soluble in water. To this end, the study of promising and efficient new formulations with the best possible performance associated with good stability is incessant. Ionic liquids (IL) have been widely studied as promoters of solubility, stability, and performance of various skin formulations. In particular, choline- and imidazole-based IL have shown great promise for modulating the properties of nanodelivery systems. Thus, this study aimed to evaluate the impact of the inclusion of IL in transferosomes in terms of their physicochemical properties and colloidal stability. To this end, we studied the incorporation of three IL, namely [Cho][Gly], [Emim][Gly], [Emim][Br], and their mixtures, in transfersomal formulations containing rutin. It is a promising bioflavonoid due to its pleiotropic properties with the potential for topical application. The innovative character of this work also lies in the use of a novel production method, as to the phase in which the IL was incorporated into the vesicular nanosystem. The results obtained reveal that the IL considerably improved the association efficiency (AE) and the loading capacity (LC) of rutin, as well as the zeta potential (ZP) of the vesicles, decreasing the size of the transfersomes. Among the IL studied, the glycinate-based IL proved to be the most promising for improving the physicochemical characteristics of transfersomes, such as LC and ZP. More so, the production method used in this work allowed to improve the colloidal stability of the transfersomal formulations stored under refrigeration for 30 days. Thus, this work demonstrated that, indeed, the incorporation of IL into rutin-containing transfersomes can be advantageous. On the other hand, the choice of the production method of these nanosystems should be judicious to obtain transfersomes with the best possible properties. Overall, the vesicular nanosystems developed herein are promising to load active compounds intended for topical administration. Keywords: Ionic liquids, transfersomes, rutin, vesicular systems
The topical administration of drugs for the treatment of various pathologies has proven to be very attractive because it may represent fewer adverse effects associated with a good performance of the active compounds, even those poorly soluble in water. To this end, the study of promising and efficient new formulations with the best possible performance associated with good stability is incessant. Ionic liquids (IL) have been widely studied as promoters of solubility, stability, and performance of various skin formulations. In particular, choline- and imidazole-based IL have shown great promise for modulating the properties of nanodelivery systems. Thus, this study aimed to evaluate the impact of the inclusion of IL in transferosomes in terms of their physicochemical properties and colloidal stability. To this end, we studied the incorporation of three IL, namely [Cho][Gly], [Emim][Gly], [Emim][Br], and their mixtures, in transfersomal formulations containing rutin. It is a promising bioflavonoid due to its pleiotropic properties with the potential for topical application. The innovative character of this work also lies in the use of a novel production method, as to the phase in which the IL was incorporated into the vesicular nanosystem. The results obtained reveal that the IL considerably improved the association efficiency (AE) and the loading capacity (LC) of rutin, as well as the zeta potential (ZP) of the vesicles, decreasing the size of the transfersomes. Among the IL studied, the glycinate-based IL proved to be the most promising for improving the physicochemical characteristics of transfersomes, such as LC and ZP. More so, the production method used in this work allowed to improve the colloidal stability of the transfersomal formulations stored under refrigeration for 30 days. Thus, this work demonstrated that, indeed, the incorporation of IL into rutin-containing transfersomes can be advantageous. On the other hand, the choice of the production method of these nanosystems should be judicious to obtain transfersomes with the best possible properties. Overall, the vesicular nanosystems developed herein are promising to load active compounds intended for topical administration. Keywords: Ionic liquids, transfersomes, rutin, vesicular systems
Descrição
Orientação: Catarina Pereira Leite ; coorientação: Tânia Santos de Almeida
Palavras-chave
MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS, CIÊNCIAS FARMACÊUTICAS, PHARMACEUTICAL SCIENCES, LÍQUIDOS IÓNICOS, IONIC LIQUIDS, LIPOSSOMAS, LIPOSOMES, RUTINA, RUTIN