Desenvolvimento de lipossomas deformáveis (etossomas, transferossomas e transetossomas) para veiculação conjunta de cafeína e resveratrol como ativos cosméticos
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Data
2023-09-29
Autores
Montanheri, Lilian Rosário da Silva [UNIFESP]
Orientadores
Filho, Newton Andréo [UNIFESP]
Tipo
Dissertação de mestrado
Título da Revista
ISSN da Revista
Título de Volume
Resumo
Os lipossomas são sistemas vesiculares que permitem a encapsulação de ativos com diferentes características, sendo eles hidrofílicos ou lipofílicos. Por conta da sua composição, são bastante biocompatíveis com diferentes tecidos. Diferente dos lipossomas convencionais, os lipossomas deformáveis, possuem na sua composição, substâncias que conferem à bicamada lipídica, alta flexibilidade. O uso dos lipossomas deformáveis, pode ser uma alternativa interessante para facilitar ou promover maior permeação cutânea dos bioativos. Inicialmente (Capítulo I) realizou-se uma revisão bibliográfica visando estabelecer uma visão geral dos parâmetros, equipamentos e modelos matemáticos utilizados para avaliar a deformabilidade de sistemas vesiculares e identificar o grupo mais usual e robusto de parâmetros a serem adotados como método analítico para determinação da deformabilidade. Além disso, estabelecer uma faixa de variação no diâmetro médio das vesículas frequentemente aceito como efeito do teste de deformação em vez de fragmentação e reorganização das vesículas. Na segunda parte do trabalho (Capítulo II) desenvolveu-se lipossomas deformáveis, contemplando os Etossomas (ET), Transferossomas (TR) e os Transetossomas (TE), utilizando o método de Injeção de Solvente (método de baixa energia), para a veiculação conjunta da cafeína e do resveratrol, como ativos cosméticos. A partir dos resultados de caracterização, foi possível determinar a concentração de etanol para os ET. Para a escolha do ativador de superfície nos TR, foram avaliados dois tensoativos (Tween 80 e Álcool oleico Etoxilado 20 OE), em seis diferentes concentrações (0,06, 0,12, 0,18, 0,24, 0,3 e 0,36%) onde foram incorporados no meio etanólico ou no meio aquoso. E com base nesses resultados, obter as formulações de TE. Nos três sistemas, os bioativos foram incorporados, nas concentrações de 2 e 0,146% (p/v), para cafeína e resveratrol, respectivamente. As análises de DL indicaram sistemas na faixa de 0,20 a 0,21 µm, e por DLS na faixa de 106,8 a 234,8 nm, com PDI de 0,14 a 0,63. Outras técnicas foram realizadas para a avaliação físico-química de todos os sistemas, bem como o ensaio de liberação dos ativos (in vitro) e a avaliação da citotoxicidade dos sistemas (in vitro). A avaliação da estabilidade, física e química, do lote de bancada e escalonado (nível de escalonamento de 5 vezes), em temperatura ambiente (25°C) e geladeira (8°C), foi acompanhada por 90 dias, onde o TR-CR foi o sistema que não apresentou variações de tamanho ao longo do estudo.
Liposomes are vesicular systems that allow the encapsulation of actives with different characteristics, whether hydrophilic or lipophilic. Due to their composition, they are quite biocompatible with different tissues. Unlike conventional liposomes, deformable liposomes have in their composition substances that give the lipid bilayer high flexibility. The use of deformable liposomes can be an interesting alternative to facilitate or promote greater skin permeation of bioactives. Initially (Chapter I) a literature review was carried out in order to establish an overview of the parameters, equipment and mathematical models used to assess the deformability of vesicular systems and to identify the most usual and robust group of parameters to be adopted as an analytical method for determining the deformability. Furthermore, establishing a range of variation in the mean vesicle diameter is often accepted as an effect of the deformation test rather than fragmentation and reorganization of the vesicles. In the second part of the work (Chapter II) deformable liposomes were developed, including Etosomes (ET), Transferosomes (TR) and Transetosomes (TE), using the Solvent Injection method (low energy method), for the delivery combination of caffeine and resveratrol, as cosmetic actives. From the characterization results, it was possible to determine the ethanol concentration for TE. For the choice of the surface activator in the RT, two surfactants (Tween 80 and Ethoxylated Oleyl Alcohol 20 EO) were evaluated, in six different concentrations (0.06, 0.12, 0.18, 0.24, 0.3 and 0.36%) where they were incorporated into an ethanolic medium or an aqueous medium. And based on these results, obtain the TE formulations. In the three systems, the bioactives were incorporated, in concentrations of 2 and 0.146% (w/v), for caffeine and resveratrol, respectively. DL analyzes indicated systems in the range of 0.20 to 0.21 μm, and by DLS in the range of 106.8 to 234.8 nm, with PDI from 0.14 to 0.63. Other techniques were performed for the physicalchemical evaluation of all systems, as well as the active release test (in vitro) and the evaluation of the cytotoxicity of the systems (in vitro). The evaluation of the stability, physical and chemical, of the bench and staggered batch (staggering level of 5 times), at room temperature (25°C) and refrigerator (8°C), was followed up for 90 days, where the TRCR was the system that did not show size variations throughout the study.
Liposomes are vesicular systems that allow the encapsulation of actives with different characteristics, whether hydrophilic or lipophilic. Due to their composition, they are quite biocompatible with different tissues. Unlike conventional liposomes, deformable liposomes have in their composition substances that give the lipid bilayer high flexibility. The use of deformable liposomes can be an interesting alternative to facilitate or promote greater skin permeation of bioactives. Initially (Chapter I) a literature review was carried out in order to establish an overview of the parameters, equipment and mathematical models used to assess the deformability of vesicular systems and to identify the most usual and robust group of parameters to be adopted as an analytical method for determining the deformability. Furthermore, establishing a range of variation in the mean vesicle diameter is often accepted as an effect of the deformation test rather than fragmentation and reorganization of the vesicles. In the second part of the work (Chapter II) deformable liposomes were developed, including Etosomes (ET), Transferosomes (TR) and Transetosomes (TE), using the Solvent Injection method (low energy method), for the delivery combination of caffeine and resveratrol, as cosmetic actives. From the characterization results, it was possible to determine the ethanol concentration for TE. For the choice of the surface activator in the RT, two surfactants (Tween 80 and Ethoxylated Oleyl Alcohol 20 EO) were evaluated, in six different concentrations (0.06, 0.12, 0.18, 0.24, 0.3 and 0.36%) where they were incorporated into an ethanolic medium or an aqueous medium. And based on these results, obtain the TE formulations. In the three systems, the bioactives were incorporated, in concentrations of 2 and 0.146% (w/v), for caffeine and resveratrol, respectively. DL analyzes indicated systems in the range of 0.20 to 0.21 μm, and by DLS in the range of 106.8 to 234.8 nm, with PDI from 0.14 to 0.63. Other techniques were performed for the physicalchemical evaluation of all systems, as well as the active release test (in vitro) and the evaluation of the cytotoxicity of the systems (in vitro). The evaluation of the stability, physical and chemical, of the bench and staggered batch (staggering level of 5 times), at room temperature (25°C) and refrigerator (8°C), was followed up for 90 days, where the TRCR was the system that did not show size variations throughout the study.
Descrição
Citação
MONTANHERI, Lilian Rosário da Silva. Desenvolvimento de lipossomas deformáveis (etossomas, transferossomas e transetossomas) para veiculação conjunta de cafeína e resveratrol como ativos cosméticos. 2023. 159 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Diadema, 2023