Nanopartículas lipídicas sólidas associadas a comprimidos: obtenção, viabilidade de associação, e avaliação sobre o impacto na liberação de substâncias lipofílicas
Data
2022-06-23
Autores
Almeida, Lucas Santos de 
Orientadores
Andréo Filho, Newton
Tipo
Trabalho de conclusão de curso
Título da Revista
ISSN da Revista
Título de Volume
Resumo
A utilização de plataformas nanotecnológicas para a veiculação de fármacos é hoje uma
realidade que interessa e projeta demanda sobre o setor de pesquisa acadêmica e de indústrias
farmacêuticas. Tal interesse se dá pela ampla gama de possibilidades que está estratégia de
administração possibilita: controle da liberação, aumento da biodisponibilidade,
direcionamento do fármaco ao seu sítio de ação, entre outras. O presente trabalho, buscou
desenvolver uma plataforma de veiculação baseada em um sistema composto por
nanopartículas lipídicas sólidas (NLS) associadas a excipientes (diluentes para compressão
direta – DCD) usualmente utilizados na fabricação de comprimidos, com a proposta de
promover uma maior biodisponibilidade de fármacos lipossolúveis quando administrado
oralmente. Para a produção das NLS utilizou-se dos processos de emulsificação por inversão
de fases e homogeneização a alta pressão. Junto a formulação utilizada para a produção das
nanopartículas, a fim de avaliar a capacidade de incorporação de substâncias lipofílicas no
sistema, o corante oil red foi adicionado a formulação, e utilizado como substância modelo,
sendo quantificado por UV-vis à 511 nm. Uma vez obtidas as nanoestruturas, estas foram
associadas a celulose microcristalina 200 através do processo de liofilização. Após este
processo as misturas foram avaliadas quanto ao aspecto, teor de oil red e liberação das NLS das
misturas. Por fim, partindo do material liofilizado obtido, foi realizado o processo de aquisição
de comprimidos a partir do processo de compressão direta. Os comprimidos obtidos foram
caracterizados frente a aspectos de dureza, peso, dimensões e perfil de liberação. Dentro dos
principais resultados obtidos com o projeto, destacam-se os associados a liberação das
nanopartículas, onde foi possível comparar o quanto de oil red se mostrou disponível no meio
na ausência e na presença das NLS: 84,5±2,0% do corante disponível foi encontrado no meio
aquoso quando associado as nanopartículas, enquanto somente 9,9±1,6% do corante disponível
foi encontrado no meio quando não associado as nanoestruturas. Essa liberação uma vez
vinculada a biodisponibilidade da substância lipofílica carreada, pode ser de interessante para
a administração de formas farmacêuticas sólidas por via oral. A quantidade disponível para
substância modelo permanece na faixa de 84,0% após o processo de obtenção de comprimidos
por compressão direta, sendo este um indicador da compatibilidade do sistema nanoestruturado
para com esta forma farmacêutica.
The use of nanotechnology platforms for drug delivery is today a reality who interest and project demand on the sector of academic research and pharmaceutical industries. That interest comes by the vast range of possibilities attached to this strategic way of administration: release control, increased bioavailability, targeting drugs to its action site, among others. The present project sought develop a platform of drug delivery based on a system compound by solid lipids nanoparticles (SLN) associated to excipients (diluents for direct compression – DDC) usually used for the manufacture of tablets. With the propose of promote an increased bioavailability on lipophilic drugs when administered orally. For the production of this SLN was used the process of emulsification by reverse phases and high press homogenization. United to the formulation used for the production of the nanoparticles, with the purpose of measure the capacity of lipophilic substances incorporation on the system, the colorant oil red was add to the formulation as model substance able to be quantified by UV-vis at 511nm. Once obtained the nanostructures, they were associated with microcrystalline cellulose 200 through the lyophilization process. After this process, the mixtures were evaluated for appearance, residual humidity, oil red content and SLN release from the mixtures. Finally, starting from the lyophilized material obtained, the process of acquiring tablets from the direct compression process was performed. The tablets obtained were characterized in terms of hardness, weight, dimensions and release profile. Within the main results obtained with the project, stand out those associated with the release of nanoparticles, where it was possible to compare how much oil red was available in the medium in the absence and presence of SLN: 84,5 ± 2.0% of the colorant was found available in the aqueous medium when associated with nanoparticles, while only 9.9 ± 1.6% of the colorant was found available in the medium when not associated with nanostructures. The release once attached to the bioavailability of the lipophilic substance carried could be interesting for the administration of solids dosage forms orally. The amount available for the model substance remains in the range of 84,0% after the process of obtaining tablets by direct compression, which is an indicator of the compatibility of the nanostructured system with this pharmaceutical form.
The use of nanotechnology platforms for drug delivery is today a reality who interest and project demand on the sector of academic research and pharmaceutical industries. That interest comes by the vast range of possibilities attached to this strategic way of administration: release control, increased bioavailability, targeting drugs to its action site, among others. The present project sought develop a platform of drug delivery based on a system compound by solid lipids nanoparticles (SLN) associated to excipients (diluents for direct compression – DDC) usually used for the manufacture of tablets. With the propose of promote an increased bioavailability on lipophilic drugs when administered orally. For the production of this SLN was used the process of emulsification by reverse phases and high press homogenization. United to the formulation used for the production of the nanoparticles, with the purpose of measure the capacity of lipophilic substances incorporation on the system, the colorant oil red was add to the formulation as model substance able to be quantified by UV-vis at 511nm. Once obtained the nanostructures, they were associated with microcrystalline cellulose 200 through the lyophilization process. After this process, the mixtures were evaluated for appearance, residual humidity, oil red content and SLN release from the mixtures. Finally, starting from the lyophilized material obtained, the process of acquiring tablets from the direct compression process was performed. The tablets obtained were characterized in terms of hardness, weight, dimensions and release profile. Within the main results obtained with the project, stand out those associated with the release of nanoparticles, where it was possible to compare how much oil red was available in the medium in the absence and presence of SLN: 84,5 ± 2.0% of the colorant was found available in the aqueous medium when associated with nanoparticles, while only 9.9 ± 1.6% of the colorant was found available in the medium when not associated with nanostructures. The release once attached to the bioavailability of the lipophilic substance carried could be interesting for the administration of solids dosage forms orally. The amount available for the model substance remains in the range of 84,0% after the process of obtaining tablets by direct compression, which is an indicator of the compatibility of the nanostructured system with this pharmaceutical form.