A influência do propilenoglicol em gel de poloxamer na permeação e retenção cutânea da metformina
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2025-01-16
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O objetivo desse estudo foi avaliar a influência do propilenoglicol em gel de poloxamer na permeabilidade e na retenção cutânea in vitro da metformina. Para a quantificação da metformina, validou-se parcialmente o método analítico por cromatografia líquida de alta eficiência (CLAE). Géis a base de poloxamer (16%) contendo metformina (0,1%) e propilenoglicol (5 e 10%) foram obtidos e estudos de permeação e retenção in vitro foram realizados em pele de orelha de porco. Solução aquosa e gel de poloxamer (16%) sem propilenoglicol, ambos contendo metformina à concentração de 0,1%, foram empregados como controle. O método por CLAE para a quantificação da metformina mostrou-se seletivo, linear (0,2-10,0ug/mL), exato e preciso (˂15%). A recuperação da metformina da pele, empregando água como solvente extrator, mostrou-se consistente e reprodutível (79,58 a 90,03%). Os estudos de permeação e retenção mostraram que as preparações a base de poloxamer contendo propilenoglicol (5% e 10%) foram mais efetivas em promover a permeação cutânea da metformina (liberação transdérmica), em relação aos controles. O gel de poloxamer por si só não apresenta efeito promotor de absorção, quando comparado com a solução aquosa. O gel de poloxamer com maior teor de propilenoglicol (10%) foi mais efetivo em promover a permeação da metformina em relação ao gel de poloxamer com menor teor de propilenoglicol (5%). A quantidade de metformina retida na pele não se altera em função da formulação.
Em suma, os resultados sugerem que o propilenoglicol promove a permeação cutânea da metformina e o efeito é concentração dependente.
The aim of this study was to evaluate the influence of propylene glycol in poloxamer gel on the in vitro cutaneous permeability and retention of metformin. For the quantification of metformin, the analytical method by high-performance liquid chromatography (HPLC) was partially validated. Poloxamer-based gels (16%) containing metformin (0,1%) and propylene glycol (5% and 10%) were obtained and in vitro permeation and retention studies were performed on pig ear skin. Aqueous solution and poloxamer gel (16%) without propylene glycol, both containing metformin at a concentration of 0,1%, were used as controls. The HPLC method for the quantification of metformin proved to be selective, linear (0,2-10,0ug/mL), accurate and precise (˂15%). The recovery of metformin from the skin, using water as the extracting solvent, was consistent and reproducible (79,58 to 90,03%). The permeation and retention studies showed that the poloxamer-based preparations containing propylene glycol (5% and 10%) were more effective in promoting the cutaneous permeation of metformin (transdermal delivery), compared to the controls. The poloxamer gel by itself did not present an absorption-promoting effect, when compared to the aqueous solution. The poloxamer gel with a higher propylene glycol content (10%) was more effective in promoting the permeation of metformin compared to the poloxamer gel with a lower propylene glycol content (5%). The amount of metformin retained in the skin did not change as a function of the formulation. In summary, the results suggest that propylene glycol promotes the cutaneous permeation of metformin and the effect is concentration-dependent.
The aim of this study was to evaluate the influence of propylene glycol in poloxamer gel on the in vitro cutaneous permeability and retention of metformin. For the quantification of metformin, the analytical method by high-performance liquid chromatography (HPLC) was partially validated. Poloxamer-based gels (16%) containing metformin (0,1%) and propylene glycol (5% and 10%) were obtained and in vitro permeation and retention studies were performed on pig ear skin. Aqueous solution and poloxamer gel (16%) without propylene glycol, both containing metformin at a concentration of 0,1%, were used as controls. The HPLC method for the quantification of metformin proved to be selective, linear (0,2-10,0ug/mL), accurate and precise (˂15%). The recovery of metformin from the skin, using water as the extracting solvent, was consistent and reproducible (79,58 to 90,03%). The permeation and retention studies showed that the poloxamer-based preparations containing propylene glycol (5% and 10%) were more effective in promoting the cutaneous permeation of metformin (transdermal delivery), compared to the controls. The poloxamer gel by itself did not present an absorption-promoting effect, when compared to the aqueous solution. The poloxamer gel with a higher propylene glycol content (10%) was more effective in promoting the permeation of metformin compared to the poloxamer gel with a lower propylene glycol content (5%). The amount of metformin retained in the skin did not change as a function of the formulation. In summary, the results suggest that propylene glycol promotes the cutaneous permeation of metformin and the effect is concentration-dependent.
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