Sistemas líquido-cristalinos acrescidos de piperina com potencial aplicação no tratamento da candidíase vulvovaginal
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Data
2021-12-15
Autores
Lima, Amanda Maciel
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Universidade Estadual Paulista (Unesp)
Resumo
A candidíase vulvovaginal (CVV) é a infecção mais usual do trato genital feminino, causada por fungos do gênero Candida spp. Os tratamentos convencionais disponíveis para esse tipo de doença apresentam-se em formulações de uso oral e tópico, as quais exibem desvantagens devido aos efeitos adversos dos agentes antifúngicos utilizados, o aumento da resistência fúngica e o baixo tempo de retenção na mucosa vaginal das formas tópicas. Pesquisas envolvendo compostos de origem natural com potencial promissor de atividade antifúngica como alternativa para o tratamento da CVV vem aumentando, como é o caso da piperina. No entanto, algumas propriedades físico-químicas da piperina dificultam a aplicação terapêutica deste composto, como é o exemplo de sua baixa solubilidade em água, fazendo com que a administração seja incompatível se empregado nas formas farmacêuticas convencionais. Então, a incorporação de piperina em sistemas líquido-cristalinos (SLC) pode ser uma estratégia eficiente para o tratamento dessas infecções, uma vez que torna possível potencializar a ação do composto, liberando-o de maneira controlada, permitindo a exposição mais longa no local da infecção e assim diminuindo a concentração de fármaco utilizada. O estudo em questão propõe o desenvolvimento e caracterização de sistemas líquidos mucoadesivos acrescidos de piperina, com potencial aplicação no tratamento da CVV. Na preparação, o fármaco foi incorporado em dois sistemas líquido-cristalinos de concentrações distintas, sendo o primeiro (F1) constituído por 20% de fase oleosa, formada por ácido oleico e colesterol na razão de 7:1; 60% de Procetyl AWS® como tensoativo; e 20% de dispersão de quitosana a 5% como fase aquosa; o segundo sistema (F2) foi constituído por 20% da fase oleosa, formada por ácido oleico e colesterol na razão de 7:1; 50% de Procetyl AWS® como tensoativo; e 30% de dispersão de quitosana a 5%. Resultados de textura e bioadesão revelaram que os sistemas F2 e F2 com o fármaco (F2+PIP) são os mais bioadesivos. Com relação a estudos de reologia, as mesmas formulações se comportaram como fluidos não-newtonianos, viscoplásticos e tixotrópicos. Além disso, os fluidos apresentam características que os definem como elásticos com grande organização estrutural, observado também pela formação de mesofase hexagonal nos SLCs na microscopia de luz polarizada. Os resultados dos ensaios de caracterização sugerem a potencial aplicação do sistema em terapias antifúngicas tópicas.
Vulvovaginal candidiasis (CVV) is the most common infection of the female genital tract, caused by fungus of the genus Candida spp. The conventional treatments available for this type of disease are in oral and topical formulations, which have disadvantages due to the adverse effects of the antifungal agents used, the increase in fungal resistance and the low retention time in the vaginal mucosa of the topical forms. Research involving compounds of natural origin with promising potential for antifungal activity as an alternative for the treatment of CVV has been increasing, as is the case with piperine. However, some physicochemical properties of piperine make the therapeutic application of this compound difficult, as is the example of its low solubility in water, making its administration incompatible if used in conventional pharmaceutical forms. Therefore, the incorporation of piperine in liquid-crystalline systems (LCS) can be an efficient strategy for the treatment of these infections, as it makes it possible to potentiate the action of the compound, releasing it in a controlled manner, allowing longer exposure at the site infection and thus decreasing the concentration of drug used. The study in question proposes the development and characterization of mucoadhesive liquid systems added with piperine, with potential application in the treatment of VVC. In the preparation, the drug was incorporated into two liquid-crystalline systems of different concentrations, the first (F1) being constituted by 20% of the oil phase, formed by oleic acid and cholesterol in the ratio of 7:1; 60% Procetyl AWS® as a surfactant; and 20% chitosan dispersion at 5% as aqueous phase; the second system (F2) was constituted by 20% of the oil phase, formed by oleic acid and cholesterol in the ratio of 7:1; 50% Procetyl AWS® as a surfactant; and 30% of 5% chitosan dispersion. Texture and bioadhesion results revealed that the F2 and F2 systems with the drug (F2+PIP) are the most bioadhesive. Regarding rheology studies, the same formulations behaved as non-Newtonian, viscoplastic and thixotropic fluids. In addition, fluids have characteristics that define them as elastic with great structural organization, also observed by the formation of hexagonal mesophase in LCSs under polarized light microscopy. The results of the characterization trials suggest the potential application of the system in topical antifungal therapies.
Vulvovaginal candidiasis (CVV) is the most common infection of the female genital tract, caused by fungus of the genus Candida spp. The conventional treatments available for this type of disease are in oral and topical formulations, which have disadvantages due to the adverse effects of the antifungal agents used, the increase in fungal resistance and the low retention time in the vaginal mucosa of the topical forms. Research involving compounds of natural origin with promising potential for antifungal activity as an alternative for the treatment of CVV has been increasing, as is the case with piperine. However, some physicochemical properties of piperine make the therapeutic application of this compound difficult, as is the example of its low solubility in water, making its administration incompatible if used in conventional pharmaceutical forms. Therefore, the incorporation of piperine in liquid-crystalline systems (LCS) can be an efficient strategy for the treatment of these infections, as it makes it possible to potentiate the action of the compound, releasing it in a controlled manner, allowing longer exposure at the site infection and thus decreasing the concentration of drug used. The study in question proposes the development and characterization of mucoadhesive liquid systems added with piperine, with potential application in the treatment of VVC. In the preparation, the drug was incorporated into two liquid-crystalline systems of different concentrations, the first (F1) being constituted by 20% of the oil phase, formed by oleic acid and cholesterol in the ratio of 7:1; 60% Procetyl AWS® as a surfactant; and 20% chitosan dispersion at 5% as aqueous phase; the second system (F2) was constituted by 20% of the oil phase, formed by oleic acid and cholesterol in the ratio of 7:1; 50% Procetyl AWS® as a surfactant; and 30% of 5% chitosan dispersion. Texture and bioadhesion results revealed that the F2 and F2 systems with the drug (F2+PIP) are the most bioadhesive. Regarding rheology studies, the same formulations behaved as non-Newtonian, viscoplastic and thixotropic fluids. In addition, fluids have characteristics that define them as elastic with great structural organization, also observed by the formation of hexagonal mesophase in LCSs under polarized light microscopy. The results of the characterization trials suggest the potential application of the system in topical antifungal therapies.
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Palavras-chave
Sistemas líquido-cristalinos, Piperina, Candidíase Vulvovaginal