Desenvolvimento de formulações antienvelhecimento constituídas por fitoquímicos para administração cutânea
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2022
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Atualmente, a crescente preocupação com os cuidados da pele, por forma a prevenir e retardar os efeitos do envelhecimento da pele, fez com que as indústrias farmacêutica e cosmética se dedicassem à investigação de compostos e produtos antienvelhecimento. A procura, por parte dos utilizadores, de produtos inovadores, naturais, eficazes e seguros tem fomentado o estudo de inúmeros fitoquímicos quanto às suas propriedades antienvelhecimento.
O ácido gálico (AG) e o ácido desidroabiético (ADA) são exemplos de fitoquímicos com estas propriedades. No entanto, as suas características físico-químicas condicionam a sua aplicação na pele. Nesse sentido, este trabalho teve como objetivo o desenvolvimento de formulações semissólidas convencionais e nanoformulações para veicular o AG e o ADA para administração cutânea, tendo em vista a otimização da sua eficácia e estabilidade. Para tal, as formulações semissólidas produzidas consistiram num creme do tipo óleo em água (O/A) para incorporar o ADA e num hidrogel para incorporar o AG, de acordo com as suas propriedades lipofílicas e hidrofílicas, respetivamente. Em relação às nanoformulações, foram desenvolvidas nanopartículas lipídicas sólidas (SLN) para a veiculação de ambos. A caracterização das formulações desenvolvidas consistiu no estudo das características organoléticas, do pH, da viscosidade aparente e, no caso das SLN, também do diâmetro hidrodinâmico (Dh) e do índice de polidispersão (PDI). As formulações semissólidas foram armazenadas a 5, 25 e 40 (± 2) °C, enquanto as SLN foram mantidas à temperatura de 25 (± 2) °C, durante 30 dias.
As formulações semissólidas apresentaram valores de pH e de viscosidade estáveis e compatíveis com a aplicação na pele, ao longo dos 30 dias. Contudo, no hidrogel com AG verificou-se uma alteração de coloração, de amarelo para castanho, que sugere a oxidação do composto. Com a utilização das SLN esta instabilidade não se verificou. Após a produção, as SLN apresentaram valores de Dh (300-400 nm) e de PDI (<0,2) favoráveis para a aplicação na pele. Uma vez que os valores destes parâmetros aumentaram durante o armazenamento e o pH e a viscosidade das nanoformulações foram reduzidos, seria favorável otimizar as formulações contendo SLN em trabalhos futuros.
No geral, este trabalho preliminar demonstrou a potencialidade da nanotecnologia para proteção de fitoquímicos da degradação e a possibilidade de veiculação de fitoquímicos em formulações convencionais e formulações contendo SLN.
Nowadays, the growing concern with skin care, in order to prevent and delay the effects of skin aging, has led the pharmaceutical and cosmetic industries to focus on the investigation of antiaging compounds and products. The users' demand for innovative, natural, efficacious, and safe products has triggered the study of various phytochemicals concerning their antiaging properties. Gallic acid (GA) and dehydroabietic acid (DAA) are examples of phytochemicals with these properties. However, their physicochemical characteristics affect their application on the skin. In this sense, this work aimed to develop conventional semisolid formulations, as well as nanotechnology-based formulations to load GA and DAA, in order to optimizing their efficacy and stability. For this purpose, regarding conventional formulations, a O/W cream was produced to load DAA, while a hydrogel was produced to load GA, according to their lipophilic and hydrophilic properties, respectively. Moreover, solid lipid nanoparticles (SLN) were developed to load both phytochemicals. All formulations were characterized in terms of organoleptic properties, pH, viscosity, and, in the case of SLN-containing formulations, hydrodynamic diameter (Dh) and polydispersity index (PDI). The semi-solid formulations were stored at 5, 25 and 40 (± 2) °C, while the SLN were kept at 25 (± 2) °C, for 30 days. The semisolid formulations displayed pH and viscosity values that were stable and compatible with skin applications over the 30 days. However, in the hydrogel with GA there was a color change, from yellow to brown, which suggests the oxidation of the compound. With the use of SLNs, this instability was not observed. After production, SLN showed favorable Dh (300-400 nm) and PDI (<0.2) values for skin applications. Since the values of these parameters increased during storage and the pH and viscosity of the nanoformulations were reduced, it would be favorable to optimize the SLN-containing formulations in future work. Overall, this preliminary work demonstrated the potential of nanotechnology for protecting phytochemicals from degradation and the possibility of loading phytochemicals in conventional formulations and SLN-containing formulations.
Nowadays, the growing concern with skin care, in order to prevent and delay the effects of skin aging, has led the pharmaceutical and cosmetic industries to focus on the investigation of antiaging compounds and products. The users' demand for innovative, natural, efficacious, and safe products has triggered the study of various phytochemicals concerning their antiaging properties. Gallic acid (GA) and dehydroabietic acid (DAA) are examples of phytochemicals with these properties. However, their physicochemical characteristics affect their application on the skin. In this sense, this work aimed to develop conventional semisolid formulations, as well as nanotechnology-based formulations to load GA and DAA, in order to optimizing their efficacy and stability. For this purpose, regarding conventional formulations, a O/W cream was produced to load DAA, while a hydrogel was produced to load GA, according to their lipophilic and hydrophilic properties, respectively. Moreover, solid lipid nanoparticles (SLN) were developed to load both phytochemicals. All formulations were characterized in terms of organoleptic properties, pH, viscosity, and, in the case of SLN-containing formulations, hydrodynamic diameter (Dh) and polydispersity index (PDI). The semi-solid formulations were stored at 5, 25 and 40 (± 2) °C, while the SLN were kept at 25 (± 2) °C, for 30 days. The semisolid formulations displayed pH and viscosity values that were stable and compatible with skin applications over the 30 days. However, in the hydrogel with GA there was a color change, from yellow to brown, which suggests the oxidation of the compound. With the use of SLNs, this instability was not observed. After production, SLN showed favorable Dh (300-400 nm) and PDI (<0.2) values for skin applications. Since the values of these parameters increased during storage and the pH and viscosity of the nanoformulations were reduced, it would be favorable to optimize the SLN-containing formulations in future work. Overall, this preliminary work demonstrated the potential of nanotechnology for protecting phytochemicals from degradation and the possibility of loading phytochemicals in conventional formulations and SLN-containing formulations.
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Orientação: Catarina Pereira Leite
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MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS, CIÊNCIAS FARMACÊUTICAS, COMPOSTOS FITOQUÍMICOS, FORMAS FARMACÊUTICAS, PHARMACEUTICAL SCIENCES, PHYTOCHEMICALS, PHARMACEUTICAL FORMS, NANOPARTÍCULAS LIPÍDICAS SÓLIDAS, ANTIENVELHECIMENTO, SOLID LIPID NANOPARTICLES, ANTIAGING, DEHYDROABIETIC ACID, ÁCIDO DESIDROABIÉTICO, ÁCIDO GÁLICO, GALLIC ACID