Maturação, compostos fenólicos e atividade antioxidante de seriguelas (SPONDIAS PURPUREA L.) cultivadas no cerrado

Monografia (graduação)—Universidade de Brasília, Faculdade de Ceilândia, Curso de Farmácia, 2015.O Cerrado brasileiro, um dos biomas da região Centro-Oeste, é conhecido pela riqueza de sua fauna e flora, e o interesse pelas propriedades de seus frutos vêm aumentando, dada a diversidade de espécies. A seriguela - Spondias purpurea L. - é uma fruta cultivada no Cerrado que possui importantes propriedades nutricionais e constitui fonte de compostos bioativos, que trazem diversos benefícios à saúde. Contudo, poucos estudos descrevem o perfil desses compostos da espécie, principalmente das cultivadas no Cerrado. Diante disso, este trabalho teve como proposta analisar a maturação comercial, composição fenólica e a capacidade antioxidante de seriguelas do Cerrado. A partir dos frutos de Spondias purpurea L., realizou-se as análises de maturação, pela determinação da acidez total titulável, pH e conteúdo de sólidos solúveis totais. Para a preparação dos extratos a partir das cascas das seriguelas, foram utilizados os solventes etanol e metanol. Com os extratos das cascas, analisou-se a composição fenólica, identificando polifenois totais, polifenois polimerizados, polifenois não-polimerizados, ésteres tartáricos, flavonois e orto-difenois; e a capacidade antioxidante pelos métodos ABTS e DPPH. Verificou-se que a fruta demonstrou resultados adequados de maturação, como também apresentou resultados significativos de compostos fenólicos e atividade antioxidante. Conforme a análise de correlação, o conteúdo de polifenois totais, polifenois não-polimerizados e polifenois polimerizados apresentou correlação positiva com DPPH e ABTS. Os métodos ABTS e DPPH demonstraram alta correlação positiva entre si.The Brazilian Cerrado, one of the Midwest biomes, is known by the fauna and flora richness and the interest in their fruits' properties has been increased, due to diversity of species. The ciriguela - Spondias purpurea L. - is a fruit cultivated in Cerrado that has important nutritional properties and it is a source of bioactive compounds, which bring several health benefits. However, studies which describe the profile of these compounds are scarce. Therefore, this work aims to analyze maturation, phenolic composition and antioxidant capacity of Cerrado's red mombin fruits. From a sample of Spondias purpurea L. fruits, the maturation analysis was performed by titratable total acidity, pH and total soluble solids content. The solvents ethanol and methanol were used for ciriguela peels extracts preparation. The peel extracts were used for determination of phenolic composition, identifying total polyphenols, polymerized polyphenols, non-polymerized polyphenols, tartaric esters, flavonols and ortho-difenols; and the antioxidant capacity by ABTS and DPPH methods. It was found that red mombin fruits presented appropriate ripening results, but also presented significant values of phenolic compounds and antioxidant activity. According to the correlation analysis, total polyphenols, non-polymerized polyphenols and polymerized polyphenols content presented positive correlation with DPPH and ABTS. A high positive correlation was obtained between ABTS and DPPH assays

Desenvolvimento, caracterização e avaliação in vitro de nanoemulsões o/a a partir de extratos de Brosimum gaudichaudii (Mama-cadela) como alternativa para o tratamento tópico de vitiligo

Dissertação (mestrado)—Universidade de Brasília, Faculdade de Ciências da Saúde, Programa de Pós-Graduação em Ciências da Saúde, 2018.Brosimum gaudichaudii é uma planta do Cerrado brasileiro que possui furanocumarinas com potencial terapêutico para tratamento do vitiligo, com destaque ao bergapteno e psoraleno. Nesse sentido, este trabalho teve como objetivo desenvolver nanoemulsões, formulações capazes de incorporar ativos vegetais e modular a permeação através da pele, a partir de extratos de Brosimum gaudichaudii, para tratamento tópico do vitiligo. Os compostos bergapteno e psoraleno foram quantificados por Cromatógrafo Líquido de Alta Eficiência (HPLC). Extratos etanólicos do pó (EXT1) e da casca da raiz (EXT2) de Brosimum gaudichaudii foram preparados e caracterizados por triagem fotoquímica. Apresentaram poucas diferenças na detecção de compostos, mas houve formação de diferentes cristais. Nanoemulsões óleo-em-água (O/A) de cada extrato foram preparadas utilizando Labrasol® e Plurol® para incorporar o EXT1 e o EXT2, obtendo NE1 e NE2. O tamanho de gotícula, o potencial zeta, pH e teor de ativos nas nanoemulsões foram avaliados. Os efeitos dos extratos e padrões sobre a viabilidade, migração e proliferação celular foram analisados em melanócitos e queratinócitos humanos. Além disso, o potencial de irritabilidade das nanoemulsões foi avaliado por ensaio de HET-CAM. No estudo de estabilidade, as nanoemulsões apresentaram pH em torno 4,0. As nanoemulsões apresentaram tamanho de gotícula tamanho ideal, entre 50 e 200 nm. Houve aumento do tamanho de gotícula das nanoemulsões armazenadas em câmara climática, o que pode ser atribuído ao aumento da temperatura. O potencial zeta das nanoemulsões foi negativo, menor que -10 mV. Nos estudos de permeação in vitro, as nanoemulsões reduziram a permeação dos ativos bergapteno e psoraleno. Os extratos demonstraram certa citotoxicidade em melanócitos e queratinócitos, mas estimularam migração celular. As duas nanoemulsões foram classificadas como irritantes leves nos ensaios de HET-CAM e adequadas para uso tópico. As nanoemulsões desenvolvidas nesse trabalho, portanto, apresentaram-se estáveis, com aspectos físicos e características organolépticas adequadas para aplicação tópica, e foram capazes de concentrar os ativos na pele, reduzindo a permeação através da pele, o que poderia causar um impacto negativo na segurança do tratamento do vitiligo.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES).Brosimum gaudichaudii is a Brazilian Cerrado plant which has furanocumarinas with therapeutic potential for vitiligo treatment, like bergapteno and psoralen. Considering its therapeutic potential, this work aimed to develop nanoemulsions, which are formulations capable of incorporating plant compounds and regulate the permeation through the skin, using Brosimum gaudichaudii extracts, for topical treatment of vitiligo. Bergapteno and psoralen compounds were quantified by high efficiency liquid chromatograph (HPLC). Ethanolics extracts of the Powder (EXT1) and the root bark (EXT2) of Brosimum gaudichaudii were prepared and characterized by photochemical screening. They showed few differences in the detection of compounds, but they produced different crystals conformations. Oil-in-water nanoemulsions (O/A) of each extract were prepared using Labrasol ® and Plurol ® to incorporate EXT1 and EXT2, obtaining NE1 and NE2. The droplet size, the zeta potential, pH and contente of bergapten and psoralen in the nanoemulsions were evaluated. The effects of the extracts and standards on the viability, migration and cellular proliferation were analyzed in human melanocytes and keratinocytes. In addition, the irritability potential of the nanoemulsions was evaluated by HET-CAM assay. In the stability study, the nanoemulsions presented PH around 4.0. The nanoemulsions presented an optimal droplet size between 50 and 200 nm. There was an increase in the droplet size of the nanoemulsions stored in the climate chamber, which can be attributed to the increase in temperature. The nanoemulsions’ zeta potential was negative, less than -10 mV. In the in vitro permeation studies, nanoemulsions reduced the permeation of bergapteno and psoralen compounds. The extracts demonstrated a certain cytotoxicity in melanocytes and keratinocytes, but they stimulated cellular migration. The nanoemulsions were classified as mild irritants in the HET-CAM assay and suitable for topical use. The nanoemulsions developed in this work, therefore, were stable, with physical aspects and organoleptic characteristics suitable for topical application, and were able to concentrate the compounds on the skin, reducing the permeation through the skin, the That could cause a negative impact on the safety of vitiligo treatment

Influence of monoolein on progesterone transdermal delivery

This work aimed to investigate in vitro the influence of monoolein (MO) on progesterone (PG) transdermal delivery and skin retention. Information about the role of MO as an absorption enhancer for lipophilic molecules can help on innovative product development capable of delivering the hormone through the skin in a consistent manner, improving transdermal therapy of hormonal replacement. MO was dispersed in propylene glycol under heat at concentrations of 0% (control), 5% w/w, 10% w/w and 20% w/w. Then, 0.6% of PG (w/w) was added to each formulation. Permeation profile of the hormone was determined in vitro for 48 h using porcine skin in Franz diffusion cells. PG permeation doubled when 5% (w/w) of MO was present in formulation in comparison to both the control and higher MO concentrations (10% and 20% w/w). An equal trend was observed for PG retention in stratum corneum (SC) and reminiscent skin (E+D). PG release rates from the MO formulations, investigated using cellulose membranes, revealed that concentrations of MO higher than 5% (w/w) hindered PG release, which indeed negatively reflected on the hormone permeation through the skin. In conclusion, this work demonstrated the feasibility of MO addition (at 5% w/w) in formulations as a simple method to increase transdermal PG delivery for therapies of hormonal replacement. In contrast, higher MO concentrations (from 10% to 20% w/w) can control active release, and this approach could be extrapolated to other lipophilic, low-molecular-weight molecules.Este trabalho teve como objetivo investigar in vitro a influência de monooleína (MO) na permeação transdérmica de progesterona (PG), bem como sobre a retenção cutânea desse hormônio a fim de (i) liberar de maneira mais consistente hormônio através da pele para melhorar a terapia transdérmica de reposição hormonal e (ii) trazer mais informações sobre o papel da MO como promotor da absorção cutânea de moléculas lipofílicas, tema ainda pouco explorado na literatura. MO foi dispersa em propilenoglicol, a concentrações de 0% (controle), 5%, 10% e 20% (p/p). Adicionou-se, em seguida, 0,6% (p/p) de PG a cada uma das formulações. O perfil de permeação do hormônio foi então determinado in vitro durante 48 h, utilizando pele de porco em células de difusão do tipo Franz. MO a 5% (p/p) foi capaz de duplicar a permeação de PG em comparação ao controle e às concentrações mais elevadas de MO, assim como a retenção de PG no estrato córneo (SC) e epiderme e derme remanescentes (E+D). A velocidade de liberação de PG a partir das formulações foi investigada usando membranas de celulose e este estudo revelou que concentrações de MO superiores a 5% (p/p) impediram a liberacão de PG, o que de fato refletiu de forma negativa na permeação cutânea do hormônio. Concluindo, este trabalho demonstrou a viabilidade da adição de MO a uma formulação como um método simples para aumentar a permeação transdérmica de PG para uso em terapias de reposição hormonal. Por outro lado, altas concentrações de MO (de 10% a 20% p/p) controlam a liberação de PG e este efeito pode ser extrapolado para outras moléculas lipofílicas de baixa massa molecular

Influence of monoolein on progesterone transdermal delivery

abstract This work aimed to investigate in vitro the influence of monoolein (MO) on progesterone (PG) transdermal delivery and skin retention. Information about the role of MO as an absorption enhancer for lipophilic molecules can help on innovative product development capable of delivering the hormone through the skin in a consistent manner, improving transdermal therapy of hormonal replacement. MO was dispersed in propylene glycol under heat at concentrations of 0% (control), 5% w/w, 10% w/w and 20% w/w. Then, 0.6% of PG (w/w) was added to each formulation. Permeation profile of the hormone was determined in vitro for 48 h using porcine skin in Franz diffusion cells. PG permeation doubled when 5% (w/w) of MO was present in formulation in comparison to both the control and higher MO concentrations (10% and 20% w/w). An equal trend was observed for PG retention in stratum corneum (SC) and reminiscent skin (E+D). PG release rates from the MO formulations, investigated using cellulose membranes, revealed that concentrations of MO higher than 5% (w/w) hindered PG release, which indeed negatively reflected on the hormone permeation through the skin. In conclusion, this work demonstrated the feasibility of MO addition (at 5% w/w) in formulations as a simple method to increase transdermal PG delivery for therapies of hormonal replacement. In contrast, higher MO concentrations (from 10% to 20% w/w) can control active release, and this approach could be extrapolated to other lipophilic, low-molecular-weight molecules

Influence of monoolein on progesterone transdermal delivery

abstract This work aimed to investigate in vitro the influence of monoolein (MO) on progesterone (PG) transdermal delivery and skin retention. Information about the role of MO as an absorption enhancer for lipophilic molecules can help on innovative product development capable of delivering the hormone through the skin in a consistent manner, improving transdermal therapy of hormonal replacement. MO was dispersed in propylene glycol under heat at concentrations of 0% (control), 5% w/w, 10% w/w and 20% w/w. Then, 0.6% of PG (w/w) was added to each formulation. Permeation profile of the hormone was determined in vitro for 48 h using porcine skin in Franz diffusion cells. PG permeation doubled when 5% (w/w) of MO was present in formulation in comparison to both the control and higher MO concentrations (10% and 20% w/w). An equal trend was observed for PG retention in stratum corneum (SC) and reminiscent skin (E+D). PG release rates from the MO formulations, investigated using cellulose membranes, revealed that concentrations of MO higher than 5% (w/w) hindered PG release, which indeed negatively reflected on the hormone permeation through the skin. In conclusion, this work demonstrated the feasibility of MO addition (at 5% w/w) in formulations as a simple method to increase transdermal PG delivery for therapies of hormonal replacement. In contrast, higher MO concentrations (from 10% to 20% w/w) can control active release, and this approach could be extrapolated to other lipophilic, low-molecular-weight molecules