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A sustainable approach to develop new advanced topical delivery system for skincare
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O hidroxitirosol (HT) é um promissor composto natural, utilizado para tratar problemas de pele, devido às suas elevadas propriedades antioxidantes. No entanto, o HT é extremamente instável, o que justifica a necessidade de técnicas de administração tópica inovadoras e sustentáveis para aumentar a sua estabilidade e biodisponibilidade em produtos de cuidados para a pele.
As tentativas iniciais de encapsular o HT utilizando nanopartículas poliméricas de quitosano (CSNPs) mostraram instabilidade na formulação, que foi solucionada com a adição de um complexo de albumina sérica bovina (BSA) pra otimizar o sistema. A caracterização revelou que ambas as formulações de nanopartículas diminuíram de tamanho, enquanto que a adição de um complexo de BSA ajudou a manter o tamanho das nanopartículas estável (289 – 363 nm) e homogéneo (PdI < 0.6). O potencial zeta (ζP), em ambas as formulações, indicou para uma superfície com carga positiva (forte estabilidade electroestática). A eficiência de encapsulação (EE) e a quantidade de fármaco (DL) nas CSNPs iniciais não apresentaram linearidade nem reprodutibilidade entre resultados. Por outro lado, a presença do complexo de BSA aumentou a EE e DL do sistema. Os ensaios de citotoxicidade com HT BSA-CSNPs em fibroblastos (HFFF2) demonstraram uma elevada viabilidade celular (> 93%) e um possível efeito citotóxico em queratinócitos (HaCaT) (viabilidade celular > 85%). Além disso, estas nanopartículas foram capazes de reduzir a formação de espécies reativas de oxigénio (ROS) (> 70%), realçando o seu forte poder antioxidante. As HT BSA-CSNPs foram incorporadas com sucesso numa matriz de gel polimérica, para manter integridade estrutural e melhorando o comportamento elástico do gel. O gel com HT BSA-CSNPs demonstrou maior adesividade, com um aumento da força normal de pico (0.401 ± 0.013 N), tempo de adesão prolongado (3.474 ± 1.242 s) e maior área sob a curva força-tempo (2.059 ± 0.385 N.s).
Em suma, este trabalho ofereceu provas de que o HT pode ser um composto antioxidante viável para utilização em cosméticos, através do desenvolvimento de uma formulação sustentável baseada num gel de nanopartículas poliméricas para encapsular a molécula de HT e preservar a sua estabilidade estrutural e garantir o seu efeito antioxidante.
Hydroxytyrosol (HT), is a promising natural compound used to address skin conditions, due to its high antioxidant properties. However, HT is extremely unstable, and therefore the need to use innovative and sustainable topical delivery techniques, to increase its stability and bioavailability on skincare applications. Initial attempts to encapsulate HT using polymeric chitosan nanoparticles (CSNPs) showed formulation instability, which was addressed adding bovine serum albumin (BSA)-complex to optimize the system. Characterization revealed that both nanoparticle formulations lowered in size, while the addition of a BSA-complex helped to maintain their size stable (289 - 363 nm) and homogeneous (PdI < 0.6). Zeta potential (ζP), on both formulations, indicate a positively charged surface (strong electro- static stability). Encapsulation efficiency (EE) and drug loading (DL) in the initial CSNPs showed no linearity nor reproducibility between results. On the contrary, the presence of the BSA-complex increased the EE and DL of the system. HT BSA-CSNPs cytotoxicity assays in fibroblasts (HFFF2) demonstrated high cell viability (> 93%) and a possible cytotoxic effect on keratinocytes (HaCaT) (cell viability > 85%). Also, these nanoparticles were able to reduce reactive oxygen species (ROS) formation (> 70%), highlighting strong antioxidant potential. The HT BSA-CSNPs were successfully incorporated into a polymeric gel matrix, maintaining its structural integrity and enhancing its elastic behavior. The gel with HT BSA-CSNPs demonstrated improved adhesive- ness, with increased peak normal force (0.401 ± 0.013 N), prolonged adhesion time (3.474 ± 1.242 s), and a larger area under the force-time curve (2.059 ± 0.385 N.s). To sum up, this work offered proof that HT can be a viable antioxidant compound to be used in cosmetics, by developing a sustainable formulation based on a gel with polymeric nanoparticles to encapsulate the HT molecule and to preserve its structure stability and guarantee its antioxidant effect.
Hydroxytyrosol (HT), is a promising natural compound used to address skin conditions, due to its high antioxidant properties. However, HT is extremely unstable, and therefore the need to use innovative and sustainable topical delivery techniques, to increase its stability and bioavailability on skincare applications. Initial attempts to encapsulate HT using polymeric chitosan nanoparticles (CSNPs) showed formulation instability, which was addressed adding bovine serum albumin (BSA)-complex to optimize the system. Characterization revealed that both nanoparticle formulations lowered in size, while the addition of a BSA-complex helped to maintain their size stable (289 - 363 nm) and homogeneous (PdI < 0.6). Zeta potential (ζP), on both formulations, indicate a positively charged surface (strong electro- static stability). Encapsulation efficiency (EE) and drug loading (DL) in the initial CSNPs showed no linearity nor reproducibility between results. On the contrary, the presence of the BSA-complex increased the EE and DL of the system. HT BSA-CSNPs cytotoxicity assays in fibroblasts (HFFF2) demonstrated high cell viability (> 93%) and a possible cytotoxic effect on keratinocytes (HaCaT) (cell viability > 85%). Also, these nanoparticles were able to reduce reactive oxygen species (ROS) formation (> 70%), highlighting strong antioxidant potential. The HT BSA-CSNPs were successfully incorporated into a polymeric gel matrix, maintaining its structural integrity and enhancing its elastic behavior. The gel with HT BSA-CSNPs demonstrated improved adhesive- ness, with increased peak normal force (0.401 ± 0.013 N), prolonged adhesion time (3.474 ± 1.242 s), and a larger area under the force-time curve (2.059 ± 0.385 N.s). To sum up, this work offered proof that HT can be a viable antioxidant compound to be used in cosmetics, by developing a sustainable formulation based on a gel with polymeric nanoparticles to encapsulate the HT molecule and to preserve its structure stability and guarantee its antioxidant effect.
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Palavras-chave
Sustainable formulation hydroxytyrosol nanoparticles stability