Síntese e caracterização de sólidos de coordenação biocompatíveis para incorporação de fármacos
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Data
2017-02-20
Autores
Alves, Renata Carolina [UNESP]
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Universidade Estadual Paulista (Unesp)
Resumo
Dentre os sólidos de coordenação, destacam-se os Metal-Organic Frameworks (MOFs), que são polímeros de coordenação com estrutura aberta contendo poros potencialmente vazios. Por serem cristalinos, porosos, leves e possuírem valores elevados de área superficial e considerável estabilidade térmica, essa nova classe de compostos vem sendo aplicada em diversas áreas como armazenamento e separação de gases, catálise heterogênea, drug delivery, sensores químicos, entre outras. A possibilidade de construção desses materiais porosos usando bioelementos e ligantes orgânicos biocompatíveis ou com atividade biológica deu origem aos BioMOFs (Metal-Organic Frameworks Biocompatíveis). Esses compostos, além das características já descritas anteriormente, possuem baixa ou nenhuma citotoxicidade frente a células humanas, sendo adequados então para serem investigados como sistemas de liberação de fármaco. Dentro dessa perspectiva, o objetivo principal deste trabalho consistiu na síntese, caracterização e avaliação do potencial de liberação do fármaco modelo diclofenaco de sódio de sólidos de coordenação baseados no ligante biológico adenina e íons cobre (II). Foram sintetizados dois compostos, CUBA e BioMOF-Cu, sendo o primeiro um cluster heptanuclear inédito e o segundo, um BioMOF já reportado na literatura. Experimentos de fisissorção de N2 revelaram a natureza não porosa do cluster CUBA e baixa área superficial de 55,13 m2 g-1. No entanto, há poros de superfície com diâmetro médio de 35,87 nm. No que se refere ao BioMOF-Cu, este apresenta natureza microporosa com área superficial de 505 m2 g-1. Ensaios de drug delivery mostraram que ambos os compostos têm alta capacidade de adsorção de diclofenaco de sódio (60,7% e 84,7% para CUBA e BioMOF-Cu, respectivamente), porém apresentam uma baixa taxa de liberação (~ 20%), provavelmente associada à coordenação do fármaco ao centro metálico nos dois materiais. Foi também determinada neste trabalho a citotoxicidade de ambos os compostos e da adenina e os resultados não mostraram toxicidade frente a linhagem celular MRC-5.Tendo em vista os resultados obtidos neste trabalho, podemos dizer que o objetivo principal foi alcançado, uma vez que foram obtidos sólidos de coordenação porosos, de baixa citotoxicidade e que apresentaram uma liberação sustentada frente ao fármaco diclofenaco de sódio.
Among the coordination solids, we highlight the Metal-Organic Frameworks (MOFs), which are coordination polymers that have open structure containing potentially void pores. Because they are crystalline, porous, light and have high surface area values and considerable thermal stability, this new class of compounds has been applied in several areas such as gas separation, heterogeneous catalysis, drug delivery, chemical sensors, among others. The possibility of building porous materials using biocompatible or biologically active organic elements and binders gave rise to BioMOFs (Biocompatible Metal-Organic Frameworks). These compounds, in addition to the features already described above, do not require any cytotoxicity to human cells, being suitable for the drug delivery systems. In this perspective, the main objective of this work was to synthesize, characterize and evaluate the release potential of the diclofenac sodium model of coordination solids based on the biological binder adenine and copper (II) ions. Two compounds, CUBA and BioMOF-Cu, were synthesized, the first being an unpublished heptanuclear cluster and the second, a BioMOF already reported in the literature. Nitrogen adsorption experiments revealed a non-porous nature of the CUBA cluster and surface area of 55.13 m2 g-1. However, there are surface pores with an average diameter of 35.87 nm. With regard to BioMOF-Cu, it has a microporous nature with a surface area of 505 m2 g-1. (60.7% and 84.7% for CUBA and BioMOF-Cu, respectively). However, a low release rate (~ 20%) was associated with the coordination of the drug in the metallic center of the two materials. The cytotoxicity of both compounds and adenine was also determined in the present study and the results showed no toxicity against the MRC-5 cell line. In view of the results obtained in this work, we can say that the main objective was achieved, since they were obtained a porous, low-cytotoxic, porous coordination solids and sustained release against the diclofenac sodium drug.
Among the coordination solids, we highlight the Metal-Organic Frameworks (MOFs), which are coordination polymers that have open structure containing potentially void pores. Because they are crystalline, porous, light and have high surface area values and considerable thermal stability, this new class of compounds has been applied in several areas such as gas separation, heterogeneous catalysis, drug delivery, chemical sensors, among others. The possibility of building porous materials using biocompatible or biologically active organic elements and binders gave rise to BioMOFs (Biocompatible Metal-Organic Frameworks). These compounds, in addition to the features already described above, do not require any cytotoxicity to human cells, being suitable for the drug delivery systems. In this perspective, the main objective of this work was to synthesize, characterize and evaluate the release potential of the diclofenac sodium model of coordination solids based on the biological binder adenine and copper (II) ions. Two compounds, CUBA and BioMOF-Cu, were synthesized, the first being an unpublished heptanuclear cluster and the second, a BioMOF already reported in the literature. Nitrogen adsorption experiments revealed a non-porous nature of the CUBA cluster and surface area of 55.13 m2 g-1. However, there are surface pores with an average diameter of 35.87 nm. With regard to BioMOF-Cu, it has a microporous nature with a surface area of 505 m2 g-1. (60.7% and 84.7% for CUBA and BioMOF-Cu, respectively). However, a low release rate (~ 20%) was associated with the coordination of the drug in the metallic center of the two materials. The cytotoxicity of both compounds and adenine was also determined in the present study and the results showed no toxicity against the MRC-5 cell line. In view of the results obtained in this work, we can say that the main objective was achieved, since they were obtained a porous, low-cytotoxic, porous coordination solids and sustained release against the diclofenac sodium drug.
Descrição
Palavras-chave
BioMOFs, Blocos de construção biocompatíveis, Cluster metálico, Adenina, Sistemas de liberação de fármacos