Desenvolvimento de nanopartículas de papaína complexada com alginato de sódio como promotor de permeação cutânea
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Data
2023-11-21
Autores
Pimentel, Debora Regina de Oliveira [UNIFESP]
Orientadores
Leite e Silva, Vânia Rodrigues [UNIFESP
Tipo
Dissertação de mestrado
Título da Revista
ISSN da Revista
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Resumo
A via de administração transdérmica é uma das formas de permeação mais antiga da história humana, na qual plantas e outras substâncias naturais eram aplicadas na pele para tratar diversos tipos de afecções. No entanto, as propriedades de barreira da pele fazem dela um obstáculo importante, e um desafio a ser superado. Desta forma, este trabalho propõe a obtenção de nanopartículas poliméricas biodegradáveis de alginato de sódio e papaína (AG-PPN) como possível promotor de permeação cutânea de ativos cosméticos utilizando a cafeína como bioativo modelo. O sistema nanoparticulado AG-PPN foi desenvolvido utilizando o método de coacervação através da neutralização de cargas iônicas das macromoléculas, permitindo a obtenção de PPN ativa e imobilizada. A dispersão obtida foi caracterizada por tamanho e uniformidade através de difração a laser (DL), revelando a formação de 99,93% de nanopartículas abaixo de 500nm e diâmetro médio de 0,19µm. A análise por DLS indicou a formação de um sistema monodisperso, com PdI de 0,332. O valor de potencial zeta foi de -50,4mV demonstrando a prevalência da carga negativa do AG. A dispersão foi caracterizada por diversas técnicas físico-químicas. E a atividade enzimática da PPN na dispersão de AG-PPN em diferentes condições de armazenamento demonstrou que após 10 dias a atividade da amostra armazenada em geladeira se manteve em 96,2%. A adição de crioprotetores à dispersão de AG-PPN demonstrou que a recuperação das nanopartículas com o crioprotetor PVP revelou a formação de 99,80% de partículas com tamanho abaixo ou igual a 500nm, e o crioprotetor PLL 100%, em concentrações de 5 e 4%, respectivamente. No entanto, o crioprotetor lactose, manteve a atividade da PPN em 72,73%. O ensaio de permeação ex vivo demonstrou que nas condições avaliadas, a PPN livre e nanoencapsulada (AG-PPN) não contribuiu para o aumento da permeação da cafeína.
The transdermal route of administration is one of the oldest forms of permeation in human history, in which plants and other natural substances were applied to the skin to treat various ailments. However, the skin's barrier properties make it a major obstacle and a challenge to overcome. In this way, this work proposes obtaining biodegradable polymeric nanoparticles of sodium alginate and papain (AG-PPN) as a possible promoter of skin permeation of cosmetic actives using caffeine as a marker. The AG-PPN nanoparticulate system was developed using the coacervation method by neutralizing the ionic charges of the macromolecules, allowing active and immobilized PPN to be obtained. The dispersion obtained was characterized for size and uniformity using laser diffraction (LD), revealing the formation of 99.93% of nanoparticles below 500nm and an average diameter of 0.19µm. DLS analysis indicated the formation of a monodisperse system, with a PdI of 0.332. The zeta potential value was -50.4mV, demonstrating the prevalence of the negative charge of the GA. The dispersion was characterized by various physicochemical techniques. And the enzymatic activity of PPN in the AG-PPN dispersion under different storage conditions showed that after 10 days the activity of the sample stored in the fridge remained at 96.2%. The addition of cryoprotectants to the AG-PPN dispersion showed that the recovery of nanoparticles with the PVP cryoprotectant revealed the formation of 99.80% of particles with a size less than or equal to 500nm, and the PLL cryoprotectant 100%, at concentrations of 5 and 4%, respectively. However, the cryoprotectant lactose maintained PPN activity at 72.73%. The ex vivo permeation test showed that under the conditions evaluated, free and nanoencapsulated PPN (AG-PPN) did not contribute to increased caffeine permeation.
The transdermal route of administration is one of the oldest forms of permeation in human history, in which plants and other natural substances were applied to the skin to treat various ailments. However, the skin's barrier properties make it a major obstacle and a challenge to overcome. In this way, this work proposes obtaining biodegradable polymeric nanoparticles of sodium alginate and papain (AG-PPN) as a possible promoter of skin permeation of cosmetic actives using caffeine as a marker. The AG-PPN nanoparticulate system was developed using the coacervation method by neutralizing the ionic charges of the macromolecules, allowing active and immobilized PPN to be obtained. The dispersion obtained was characterized for size and uniformity using laser diffraction (LD), revealing the formation of 99.93% of nanoparticles below 500nm and an average diameter of 0.19µm. DLS analysis indicated the formation of a monodisperse system, with a PdI of 0.332. The zeta potential value was -50.4mV, demonstrating the prevalence of the negative charge of the GA. The dispersion was characterized by various physicochemical techniques. And the enzymatic activity of PPN in the AG-PPN dispersion under different storage conditions showed that after 10 days the activity of the sample stored in the fridge remained at 96.2%. The addition of cryoprotectants to the AG-PPN dispersion showed that the recovery of nanoparticles with the PVP cryoprotectant revealed the formation of 99.80% of particles with a size less than or equal to 500nm, and the PLL cryoprotectant 100%, at concentrations of 5 and 4%, respectively. However, the cryoprotectant lactose maintained PPN activity at 72.73%. The ex vivo permeation test showed that under the conditions evaluated, free and nanoencapsulated PPN (AG-PPN) did not contribute to increased caffeine permeation.