Avaliação da atividade antiproliferativa in vitro, liberação, permeação e retenção cutânea in vitro e estabilidade de emulsões contendo (-)- Terpinen-4-OL
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Data
2011-04-08
Autores
Maccari, Flavia Lima Ribeiro [UNESP]
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Editor
Universidade Estadual Paulista (Unesp)
Resumo
O terpinen-4-ol é o principal componente da M. alternifólia, apresenta atividade antiinflamatória, antibacteriana e antifúngica; em estudos recentes in vitro a atividade antineoplásica para linhagens celulares de melanoma (M14) foi demonstrada. O objetivo específico deste trabalho foi verificar a atividade farmacológica in vitro dos isômeros óticos (-) terpinen-4-ol e (+) terpinen-4-ol e do óleo de Melaleuca alternifolia em nove linhagens diferentes de células tumorais, incluindo a célula UACC-62 do melanoma que ainda não havia sido estudada, e a concentração eficaz para o desenvolvimento de formulação que possa ter ação contra o melanoma. Após realização dos ensaios farmacológicos in vitro verificou-se que o (-)terpinen-4-ol apresentou melhor atividade nas linhagens celulares de melanoma, sendo o princípio ativo de escolha para as duas formulações que foram desenvolvidas, testadas e comprovadas a qualidade e estabilidade. Para caracterização das formulações foram efetuados os ensaios reológicos, sendo comprovado que as emulsões desenvolvidas são adequadas para o uso tópico no que diz respeito às suas características reológicas, sendo que as duas apresentaram comportamento de fluxo semelhante, diferindo apenas na área de histerese. Posteriormente foram feitos testes de permeação e retenção cutânea in vitro, para verificar qual formulação permite que o princípio ativo atinja em maior concentração a camada de interesse para atividade contra o melanoma. O método proposto para quantificação do (-)-terpinen-4-ol foi validado e utilizado nos ensaios de estabilidade acelerada, liberação, permeação e retenção cutânea in vitro. Os ensaios de liberação demonstraram que as duas formulações apresentam cinética de zero ordem, com fluxo de 14,62 µg/cm2 /h para formulação 1 e de 6,70 µg/cm2 /h para formulação F2. Na retenção cutânea...
The terpinen-4-ol is the major component of M. alternifolia, has anti-inflammatory, antibacterial and antifungal, in recent studies in vitro anticancer activity for melanoma cell lines (M14) was demonstrated. The specific objective of this study was to assess the in vitro pharmacological activity of optical isomers (-) terpinen-4-ol and (+) terpinen-4-ol and oil of Melaleuca alternifolia in nine different tumor cell lines, including cell UACC -62 melanoma that had not yet been studied, and effective concentration for the formulation development that may have action against melanoma. After performing the in vitro pharmacological tests showed that the (-) terpinen-4-ol showed better activity in melanoma cell lines, with the active ingredient of choice for the two formulations were developed, tested and proven quality and stability. For characterization of the formulations were made the rheological tests and confirmed that the developed emulsions are suitable for topical use in relation to their rheological characteristics, and the two had similar flow behavior, differing only in the area of hysteresis. Subsequent tests were performed permeation and skin retention in vitro, to determine which formulation allows the active ingredient reaches higher concentration in the layer of interest for activity against melanoma. The proposed method for quantification of (-)-terpinen-4-ol was validated and used in accelerated stability testing, release, skin permeation and retention in vitro. The release assays demonstrated that both formulations have zero order kinetics at a rate of 14.62 g/cm2/h for formulation 1 and 6.70 g/cm2/h for formulation F2. In vitro skin retention was found that the F1 showed retention of terpinen-4-ol smaller in the stratum corneum, compared to F2. Conversely, the retention in the epidermis over the dermis of terpinen-4-ol was higher in F1. It was found that formulation F1 ... (Complete abstract click electronic access below)
The terpinen-4-ol is the major component of M. alternifolia, has anti-inflammatory, antibacterial and antifungal, in recent studies in vitro anticancer activity for melanoma cell lines (M14) was demonstrated. The specific objective of this study was to assess the in vitro pharmacological activity of optical isomers (-) terpinen-4-ol and (+) terpinen-4-ol and oil of Melaleuca alternifolia in nine different tumor cell lines, including cell UACC -62 melanoma that had not yet been studied, and effective concentration for the formulation development that may have action against melanoma. After performing the in vitro pharmacological tests showed that the (-) terpinen-4-ol showed better activity in melanoma cell lines, with the active ingredient of choice for the two formulations were developed, tested and proven quality and stability. For characterization of the formulations were made the rheological tests and confirmed that the developed emulsions are suitable for topical use in relation to their rheological characteristics, and the two had similar flow behavior, differing only in the area of hysteresis. Subsequent tests were performed permeation and skin retention in vitro, to determine which formulation allows the active ingredient reaches higher concentration in the layer of interest for activity against melanoma. The proposed method for quantification of (-)-terpinen-4-ol was validated and used in accelerated stability testing, release, skin permeation and retention in vitro. The release assays demonstrated that both formulations have zero order kinetics at a rate of 14.62 g/cm2/h for formulation 1 and 6.70 g/cm2/h for formulation F2. In vitro skin retention was found that the F1 showed retention of terpinen-4-ol smaller in the stratum corneum, compared to F2. Conversely, the retention in the epidermis over the dermis of terpinen-4-ol was higher in F1. It was found that formulation F1 ... (Complete abstract click electronic access below)
Descrição
Palavras-chave
Fármacos, Farmacologia, Permeação cutânea in vitro, Terpinen-4-ol, Release, Skin retention in vitro, Permeation in vitro, Antiproliferative in vitro, Methods validation, Drug stability, Quality control
Como citar
MACCARI, Flavia Lima Ribeiro. Avaliação da atividade antiproliferativa in vitro, liberação, permeação e retenção cutânea in vitro e estabilidade de emulsões contendo (-)- Terpinen-4-OL. 2011. 132 f. Dissertação (mestrado) - Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, 2011.