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Formulation, characterization and stability studies of emulsions containing different vegetable oils and caffeine as active compound
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A permeação eficaz de ingredientes ativos pela barreira cutânea é um dos principais pontos de discussão no que toca a Indústria Cosmética, que tem vindo a crescer de forma considerável nos últimos anos. Muito compostos não apresentam as características físico-químicas necessárias a uma permeação cutânea passiva em quantidades relevantes. De modo a tentar resolver este desafio, o uso de substâncias que facilitam a permeação, os chamados promotores de permeação cutânea, surge como potencial solução, tendo como foco primário a penetração do estrato córneo.
Do conjunto dos excipientes com estas características, os óleos vegetais, ricos em ácidos gordos como o ácido oleico, apresentam-se com possíveis candidatos. Para além de serem produtos naturais, o que acaba por ser a nova tendência no mundo da cosmética, e terem inúmeros benefícios para a pele, os óleos vegetais demonstram a capacidade de acelerar e aumentar a permeação de ativos pela pele. Ao alterarem o estado da bicamada fosfolipídica, destabilizando os ácidos gordos compactados e sendo integrados na própria membrana, permitem que outras substâncias atravessem a pele mais facilmente.
Esta monografia procura explorar a influencia de 3 óleos vegetais diferentes – azeite, óleo de amêndoas doces e óleo de semente de girassol – numa formulação de referência, avaliando os seus efeitos nos atributos físicos e sensoriais da emulsão, assim como na sua estabilidade ao longo do tempo. Foram desenvolvidos estudos de libertação e permeação cutânea usando membranas consideradas o standard para cada um dos testes. Foi utilizada como ativo a cafeína, um composto hidrofílico bem estabelecido e conhecido pelos seus benefícios para a pele, desde as suas propriedades antioxidantes à sua capacidade de aumentar a microcirculação.
Dos óleos vegetais testados, a formulação que continha azeite acabou por apresentar melhores resultados ao longo do tempo. Em comparação com a formulação de referência mostrou dados promissores, com uma permeação mais rápida e extensa da cafeína, apesar de serem necessários mais estudos para determinar se estes resultados são de facto de alguma significância estatística. Este estudo fornece uma base para futura investigação acerca das potenciais aplicações dos óleos vegetais em formulações de aplicação cutânea, nomeadamente enquanto promotores de permeação cutânea.
The efficient permeation of active ingredients through the skin barrier is one of the main talking points when it comes to the Cosmetic Industry, which has experienced a considerable growth over the past few years. Numerous compounds lack the optimal physicochemical characteristics required for passive skin permeation in relevant amounts. To address this challenge, a strategy involving the use of substances that facilitate permeation, the so-called permeation enhancers, has emerged as a possible solution, with a primary focus on crossing the stratum corneum. Amongst potential excipients with these characteristics, vegetable oils, rich in fatty acids like oleic acid, have shown to be plausible contenders. Besides fitting the new trend of natural products being of cosmetic use and having multiple benefits to the skin, they demonstrate the ability to expedite and increase the permeation of active ingredients across the skin by disrupting the phospholipidic bilayer, destabilizing the densely packed fatty acids, and seamlessly integrating into the skin, thus allowing for other substances to be easily delivered transdermally. This dissertation aimed to explore the influence of three different vegetable oils – olive oil, sweet almond oil and sunflower seed oil - on a reference formulation, assessing their effects on the physical and sensory attributes of the emulsion, as well as in its stability over time. Release and permeation studies were conducted using standard membranes for each study and employing caffeine, a well-established hydrophilic compound celebrated for its skin benefits, such as antioxidant properties and the ability of increasing microcirculation. Out of the tested vegetable oils, the findings favored the formulation containing olive oil, which consistently exhibited superior performance over time. In comparison to the reference formulation, the results for this formulation were also promising, with faster and more extensive permeation of the caffeine being achieved, although further studies should be developed to ensure statistical significance. This study lays the groundwork for future research into the diverse potential applications of vegetable oils in skincare formulations, mainly as permeation enhancers.
The efficient permeation of active ingredients through the skin barrier is one of the main talking points when it comes to the Cosmetic Industry, which has experienced a considerable growth over the past few years. Numerous compounds lack the optimal physicochemical characteristics required for passive skin permeation in relevant amounts. To address this challenge, a strategy involving the use of substances that facilitate permeation, the so-called permeation enhancers, has emerged as a possible solution, with a primary focus on crossing the stratum corneum. Amongst potential excipients with these characteristics, vegetable oils, rich in fatty acids like oleic acid, have shown to be plausible contenders. Besides fitting the new trend of natural products being of cosmetic use and having multiple benefits to the skin, they demonstrate the ability to expedite and increase the permeation of active ingredients across the skin by disrupting the phospholipidic bilayer, destabilizing the densely packed fatty acids, and seamlessly integrating into the skin, thus allowing for other substances to be easily delivered transdermally. This dissertation aimed to explore the influence of three different vegetable oils – olive oil, sweet almond oil and sunflower seed oil - on a reference formulation, assessing their effects on the physical and sensory attributes of the emulsion, as well as in its stability over time. Release and permeation studies were conducted using standard membranes for each study and employing caffeine, a well-established hydrophilic compound celebrated for its skin benefits, such as antioxidant properties and the ability of increasing microcirculation. Out of the tested vegetable oils, the findings favored the formulation containing olive oil, which consistently exhibited superior performance over time. In comparison to the reference formulation, the results for this formulation were also promising, with faster and more extensive permeation of the caffeine being achieved, although further studies should be developed to ensure statistical significance. This study lays the groundwork for future research into the diverse potential applications of vegetable oils in skincare formulations, mainly as permeation enhancers.
Descrição
Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, 2023, Universidade de Lisboa, Faculdade de Farmácia.
Palavras-chave
Skin permeation Vegetable oils Fatty acids Enhancer Mestrado Integrado - 2023