Administração oral de insulina: realidade ou ficção?
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2017
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A Diabetes é considerada por muitos como um dos maiores problemas de Saúde em todo o Mundo, onde cerca de 387 milhões de pessoas têm a doença diagnosticada, sendo que este valor tende a aumentar. É, por isso, considerada por muitos autores a epidemia do século XXI. Esta é uma doença que não tem cura, daí a procura constante de novos tratamentos inovadores, e mais cómodos para o doente. Na Diabetes Mellitus tipo 1 há a necessidade constante, durante toda a vida, da administração exógena da hormona. Uma vez que esta é administrada por via subcutânea, torna-se desconfortável para o doente, podendo até levar a reações alérgicas no local de administração tais como lipodistrofias, e daí a preocupação de encontrar uma outra forma de administração, sendo a preferencial a via oral. Contudo, alguns problemas relacionados com natureza proteica fazem desta tarefa um grande desafio uma vez que a fraca estabilidade da insulina à degradação proteolítica e hidrolítica, baixa permeabilidade intestinal e tempo de semi-vida curto na circulação sistémica, levam consequentemente a uma fraca absorção intestinal. Para ultrapassar todos os problemas associados à natureza proteica, recorreu-se a nanotecnologia para veiculação do fármaco. Para tal utilizaram-se nanopartículas poliméricas constituídas por poli(ácido lático-co-ácido glicólico) (PLGA). Esta abordagem apresentou resultados promissores, não só devido ao tamanho reduzido que confere uma elevada área de contato entre a superfície da partícula e a célula intestinal, mas também pela proteção enzimática e aumento do tempo de semi-vida da insulina.
Diabetes is considered by many people as one of the biggest health problems in the world where about 387 million people have been diagnosed, and this value tends to increase. Therefore, it is considered by many authors the epidemic of the XXI century. This is a disease that has no cure, hence the constant search for new innovative treatments and more comfortable for the patient. In type 1 there is a constant need for the entire life from exogenous administration of the hormone. Since this is administered subcutaneously, it becomes uncomfortable for the patient and may even lead to allergic reactions at the injection site such as lipodystrophy, hence the concern to find another route of administration, and the preferential is the oral administration. However, some problems related with protein nature makes this task a big challenge since the poor stability of insulin mainly due to hydrolytic and proteolytic degradation, poor intestinal permeability and a short half-life time in the systemic circulation, leading to poor intestinal absorption. For overcoming all the problems associated with protein nature, nanoparticles may be considered a great strategy. For this purpose we prepared polymeric nanoparticles composed by poly (lactic-co-glycolic acid) (PLGA). This approach has been giving promising results, not only due to the particle small size that leads to a high contact area between the particle surface and intestinal cell, but also by enzymatic protection which confers and increase of half-life time of insulin.
Diabetes is considered by many people as one of the biggest health problems in the world where about 387 million people have been diagnosed, and this value tends to increase. Therefore, it is considered by many authors the epidemic of the XXI century. This is a disease that has no cure, hence the constant search for new innovative treatments and more comfortable for the patient. In type 1 there is a constant need for the entire life from exogenous administration of the hormone. Since this is administered subcutaneously, it becomes uncomfortable for the patient and may even lead to allergic reactions at the injection site such as lipodystrophy, hence the concern to find another route of administration, and the preferential is the oral administration. However, some problems related with protein nature makes this task a big challenge since the poor stability of insulin mainly due to hydrolytic and proteolytic degradation, poor intestinal permeability and a short half-life time in the systemic circulation, leading to poor intestinal absorption. For overcoming all the problems associated with protein nature, nanoparticles may be considered a great strategy. For this purpose we prepared polymeric nanoparticles composed by poly (lactic-co-glycolic acid) (PLGA). This approach has been giving promising results, not only due to the particle small size that leads to a high contact area between the particle surface and intestinal cell, but also by enzymatic protection which confers and increase of half-life time of insulin.
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Orientação: Ana Catarina Pinto Reis
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MESTRADO INTEGRADO EM CIÊNCIAS FARMACÊUTICAS, FARMACOLOGIA, CIÊNCIAS FARMACÊUTICAS, NANOTECNOLOGIA, INSULINA, DIABETES, NANOPARTÍCULAS PLGA, PROTEÍNAS, PHARMACEUTICAL SCIENCES, PHARMACOLOGY, NANOTECHNOLOGY, INSULIN, DIABETES, PLGA NANOPARTICLES, PROTEINS