Plataforma de carreadores lipídicos para veiculação de bioativos em formas farmacêuticas sólidas: desenvolvimento de nanopartículas lipídicas para veiculação em pós e cápsulas
Data
2021-11-30
Autores
Vasconcelos, Ana Paula Macedo de [UNIFESP]
Orientadores
Andréo Filho, Newton [UNIFESP]
Tipo
Dissertação de mestrado
Título da Revista
ISSN da Revista
Título de Volume
Resumo
A nanotecnologia é definida pela National Science Foundation – NSF, agência americana dedicada ao progresso da ciência, como sendo o desenvolvimento de pesquisa e tecnologia nos níveis atômico, molecular ou macromolecular. Em termos gerais, as nanopartículas são estruturas coloidais, que apresentam dimensões compreendidas entre 0,1 e 1000 nm. O objetivo desse trabalho foi desenvolver uma plataforma de nanocarreadores lipídicos para veiculação de bioativos. Inicialmente realizou-se uma revisão bibliográfica para conhecer as possibilidades de nanoestruturas lipídicas, formulação e processo, suas vantagens e dificuldades. Para escolha da formulação e processo foram realizados DoE (Design of experiments) por planejamento estatístico fatorial do tipo 2³ adicionados três pontos centrais considerando dois níveis e três fatores. Foram avaliados a porcentagem total de tensoativos (%TA - 4% e 8%), proporção de lauril sulfato de sódio (LSS) na mistura de tensoativos (%LSS TA - 0% e 10%) e porcentagem de fase oleosa (%FO - 10% e 20%) assim como tempo (5 e 15 minutos), pressão (5000 psi e 15000 psi) e temperatura (30°C e 70ºC), resultando na escolha de 8% de tensoativos (%TA), sem adição de lauril sulfato de sódio (0% para %LSS) e 10 % de fase oleosa (%FO) e cerca de 12.500 psi, temperatura de 70ºC, durante 15 minutos de processamento. Por fim as nanopartículas foram incorporadas aos diluentes amido pré-gelatinizado, celulose microcristalina 102 e celulose microcristalina 200 e caracterizadas através umidade, do tamanho de partículas, Potencial Zeta, Difração a Laser (SLS) e Recuperação. A umidade de todas as amostras foi abaixo de 5,0%. Considerando os valores encontrados no teste de recuperação do Oil Red todas amostras demonstraram resultados adequados, com foco nas amostras de proporção 5:5. O teste de recuperação demonstrou melhores resultados para o diluente MCC200. A partir dos resultados de caracterização, foi escolhida a proporção de DLT:NL de 5:5 de Celulose microcristalina PH200 como possível insumo carreador de nanopartículas lipídicas para veiculação em formas sólidas de uso oral como pós e cápsula.
Nanotechnology is defined by the National Science Foundation – NSF, an American agency dedicated to the progress of science, as the development of research and technology at the atomic, molecular or macromolecular levels. In general terms, nanoparticles are colloidal structures, which have dimensions between 0.1 and 1000 nm. The objective of this work was to develop a lipid nanocarrier platform for the delivery of bioactives. Initially, a bibliographical review was carried out to know the possibilities of lipid nanostructures, formulation and process, their advantages and difficulties. To choose the formulation and process, DoE (Design of Experiments) was carried out by factorial statistical planning of type 2³, adding three central points considering two levels and three factors. The total percentage of surfactants (%TA - 4% and 8%), proportion of sodium lauryl sulfate (LSS) in the surfactant mixture (%LSS TA - 0% and 10%) and percentage of oil phase (%) were evaluated FO - 10% and 20%) as well as time (5 and 15 minutes), pressure (5000 psi and 15000 psi) and temperature (30°C and 70°C), resulting in the choice of 8% surfactants (%TA), without addition of sodium lauryl sulfate (0% to %LSS) and 10% oil phase (%FO) and about 12,500 psi, temperature 70°C, during 15 minutes of processing. Finally, the nanoparticles were incorporated into the diluents pregelatinized starch, microcrystalline cellulose 102 and microcrystalline cellulose 200 and characterized by moisture, particle size, Zeta Potential, Laser Diffraction (SLS) and Recovery. The moisture of all samples was below 5.0%. Considering the values found in the Oil Red recovery test, all samples showed adequate results, with a focus on samples with a 5:5 ratio. Recovery testing showed better results for the MCC200 diluent. From the characterization results, the DLT:NL ratio of 5:5 of Microcrystalline Cellulose PH200 was chosen as a possible carrier input for lipid nanoparticles for delivery in solid forms for oral use such as powders and capsules.
Nanotechnology is defined by the National Science Foundation – NSF, an American agency dedicated to the progress of science, as the development of research and technology at the atomic, molecular or macromolecular levels. In general terms, nanoparticles are colloidal structures, which have dimensions between 0.1 and 1000 nm. The objective of this work was to develop a lipid nanocarrier platform for the delivery of bioactives. Initially, a bibliographical review was carried out to know the possibilities of lipid nanostructures, formulation and process, their advantages and difficulties. To choose the formulation and process, DoE (Design of Experiments) was carried out by factorial statistical planning of type 2³, adding three central points considering two levels and three factors. The total percentage of surfactants (%TA - 4% and 8%), proportion of sodium lauryl sulfate (LSS) in the surfactant mixture (%LSS TA - 0% and 10%) and percentage of oil phase (%) were evaluated FO - 10% and 20%) as well as time (5 and 15 minutes), pressure (5000 psi and 15000 psi) and temperature (30°C and 70°C), resulting in the choice of 8% surfactants (%TA), without addition of sodium lauryl sulfate (0% to %LSS) and 10% oil phase (%FO) and about 12,500 psi, temperature 70°C, during 15 minutes of processing. Finally, the nanoparticles were incorporated into the diluents pregelatinized starch, microcrystalline cellulose 102 and microcrystalline cellulose 200 and characterized by moisture, particle size, Zeta Potential, Laser Diffraction (SLS) and Recovery. The moisture of all samples was below 5.0%. Considering the values found in the Oil Red recovery test, all samples showed adequate results, with a focus on samples with a 5:5 ratio. Recovery testing showed better results for the MCC200 diluent. From the characterization results, the DLT:NL ratio of 5:5 of Microcrystalline Cellulose PH200 was chosen as a possible carrier input for lipid nanoparticles for delivery in solid forms for oral use such as powders and capsules.