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O leite de vaca tem sido reconhecido como um produto valioso a ser incorporado na formulação de medicamentos. A sua composição é rica em proteínas com elevado valor biológico; lípidos, maioritariamente organizados em micelas; carbohidratos, do qual se destaca a lactose; vitaminas e sais minerais que existem em menores quantidades. Naturalmente, todos estes compostos desempenham funções biológicas que podem ser aproveitadas para o transporte de fármacos. Tirando partido de todas estas propriedades, o leite tem sido descrito como sendo capaz de aumentar a solubilidade das substâncias ativas e de redirecioná-las para alvos biológicos específicos, aumentando a sua biodisponibilidade e diminuindo a sua toxicidade. Além disso, tem vindo a ser verificada a sua capacidade de proteção gástrica representando uma vantagem principalmente em relação a anti-inflamatórios não esteroides. Por último, o leite parece ser capaz de mascarar o mau sabor de algumas substâncias. Esta capacidade mostra-se especialmente importante em crianças e idosos impactando positivamente a adesão à terapêutica.
Apesar do leite parecer um excipiente promissor, ainda não é oficialmente reconhecido como tal. O facto de ser um produto de origem natural e a sua estabilidade limitada podem representar fatores condicionantes. De forma a aumentar a sua estabilidade pode ser aplicadas tecnologias como o "freeze-drying", "spray-drying" ou "fluidized-bed" de modo a reduzir a quantidade de água presente na sua composição.
Cow’s milk has been increasingly recognized as a valuable food product to be integrated in a drug formulation. Milk’s composition is very rich in proteins, presenting a high biological value; lipids, mostly organized in micelles; carbohydrates of which lactose stands out being a widely used drug excipient; vitamins and mineral salts that are present in relative minimal amounts. Naturally, each of these compounds shows biological functions in the organism that can be availed for a drug delivery purpose. The whole milk combining all the proprieties together is described to enhance the solubility of the active ingredients which is one of the biggest issues that affect their bioavailability and also to direct the active molecules to specific targets decreasing their toxicity. Gastroprotection has additionally been reported as a milk ability being beneficial in drugs reportedly aggressive to the gastrointestinal system such as non-steroid anti-inflammatory drugs. Furthermore, milk shows to be an opportunity to mask the unpleasant taste of the drugs. This has come up as a necessity over geriatric and pediatric populations that present swallowing constraints and therefore the taste is crucial for therapy compliance. Although milk is considered a promising excipient, it has never run into a commercialized product. As a natural product, there are regulatory issue that are more difficult to be controlled such as contaminants, microbiologic growth, exact composition, among others. Its limited stability results in a short shelf-life and is mostly due to its high-water content. It has been applied technological techniques that reduce the free water with insignificant damage to the structure of milk components. Among these techniques are spray drying, freeze drying, fluidized bed processes and hybrid version techniques. This way its functionality is preserved and as well as its stability is raised. Milk allergenicity and intolerance is also an increasingly concern that must be taken in consideration.
Cow’s milk has been increasingly recognized as a valuable food product to be integrated in a drug formulation. Milk’s composition is very rich in proteins, presenting a high biological value; lipids, mostly organized in micelles; carbohydrates of which lactose stands out being a widely used drug excipient; vitamins and mineral salts that are present in relative minimal amounts. Naturally, each of these compounds shows biological functions in the organism that can be availed for a drug delivery purpose. The whole milk combining all the proprieties together is described to enhance the solubility of the active ingredients which is one of the biggest issues that affect their bioavailability and also to direct the active molecules to specific targets decreasing their toxicity. Gastroprotection has additionally been reported as a milk ability being beneficial in drugs reportedly aggressive to the gastrointestinal system such as non-steroid anti-inflammatory drugs. Furthermore, milk shows to be an opportunity to mask the unpleasant taste of the drugs. This has come up as a necessity over geriatric and pediatric populations that present swallowing constraints and therefore the taste is crucial for therapy compliance. Although milk is considered a promising excipient, it has never run into a commercialized product. As a natural product, there are regulatory issue that are more difficult to be controlled such as contaminants, microbiologic growth, exact composition, among others. Its limited stability results in a short shelf-life and is mostly due to its high-water content. It has been applied technological techniques that reduce the free water with insignificant damage to the structure of milk components. Among these techniques are spray drying, freeze drying, fluidized bed processes and hybrid version techniques. This way its functionality is preserved and as well as its stability is raised. Milk allergenicity and intolerance is also an increasingly concern that must be taken in consideration.
Descrição
Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, 2020, Universidade de Lisboa, Faculdade de Farmácia.
Palavras-chave
Gastroprotection Milk Targeted drug delivery Taste masking Mestrado integrado - 2020
