Desarrollo de un sistema transportador de fármacos de baja solubilidad, cargue y cuantificación de principios activos en el sistema de transporte desarrollado
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Fecha
2024
Autores
De La Hoz Álvarez, Andrés
Cabrera González, Angely
Mercado Reyes, Jesús
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Ediciones Universidad Simón Bolívar
Facultad de Ciencias Básicas y Biomédicas
Facultad de Ciencias Básicas y Biomédicas
Resumen
La baja solubilidad de algunos principios activos supone un reto para la formulación de nuevos y mejores medicamentos por ello en los últimos años se han intensificado estudios para el desarrollo de nuevas plataformas para el transporte de fármacos de baja solubilidad con las que se obtenga una buena liberación, biodisponibilidad y Absorción, una de ellas es la microencapsulación mediante la cual se pueden cargar principios activos hidrofóbicos de manera eficaz. La presente investigación se centra en la producción de micropartículas lipídicas solidas como sistema transportador de fármacos de baja solubilidad, el cargue y cuantificación de principios activos en el sistema de transporte desarrollado. Las micropartículas fueron creadas a partir de alcohol cetílico, ácido esteárico, ácido palmítico y quitosano por el método de microemulsión, usando Tween 20 y 80 como emulsionante y Fexofenadina como principio activo debido a su escasa solubilidad en agua. Con estas materias primas fue posible desarrollar tres formulaciones, las cuales se estudiaron a través de difracción láser con ayuda de un analizador de partículas Mastersizer 3000+ Ultra mediante el cual se obtuvo la distribución de los tamaños de partículas. Adicionalmente, para la cuantificación de Fexofenadina en capsulada en los sistemas de transporte preparados se construyó una curva de calibración con un estándar externo, preparando soluciones cuyas concentraciones fueron, 0.09 mg/mL, 0.06 mg/mL, 0.03 mg/mL y 0.009 mg/mL, Seguidamente se leyeron las absorbancias a una longitud de onda de 220 nm en un espectrofotómetro UV-Visible Agilent Technologies 8453. Finalmente, usando la ecuación de ajuste lineal se calculó la concentración de Fexofenadina en cada sistema de transporte. Entre los resultados relevantes del trabajo se destaca la obtención de al menos un 50% de micropartículas con tamaños inferiores a 6.17 μm; lo que favorece la velocidad de disolución, la biodisponibilidad y con ello una mejor absorción, por otra parte, los porcentajes de encapsulación del fármaco van desde 54.05 ± 0.03 % hasta el 78.58 ± 0.09 %. Los resultados de esta investigación muestran que esta tecnología es una herramienta prometedora para el desarrollo de sistemas de transporte de fármacos de baja solubilidad con alta capacidad de carga de principios activos.
The low solubility of some active ingredients is a challenge for the formulation of new and better drugs, therefore in recent years studies have intensified for the development of new platforms for the transport of low solubility drugs with which a good release, bioavailability and absorption are obtained, one of them is the microencapsulation by which hydrophobic active ingredients can be loaded effectively. The present research focuses on the production of solid lipid microparticles as a carrier system for low solubility drugs, the loading and quantification of active ingredients in the developed transport system. The microparticles were created from cetyl alcohol, stearic acid, palmitic acid and chitosan by the microemulsion method, using Tween 20 and 80 as emulsifier and Fexofenadine as active principle due to its low solubility in water. With these raw materials it was possible to develop three formulations, which were studied through laser diffraction with the help of a Mastersizer 3000+ Ultra particle analyzer by means of which the distribution of particle sizes was obtained. Additionally, for the quantification of Fexofenadine in capsulated in the prepared transport systems, a calibration curve was constructed with an external standard, preparing solutions whose concentrations were 0.09 mg/mL, 0.06 mg/mL, 0.03 mg/mL and 0.009 mg/mL. The absorbances were then read at a wavelength of 220 nm in an Agilent Technologies 8453 UV-Visible spectrophotometer. Finally, using the linear fitting equation, the concentration of Fexofenadine in each transport system was calculated. Among the relevant results of the work, it is highlighted the obtaining of at least 50% of microparticles with sizes smaller than 6.17 μm; which favors the dissolution rate, the bioavailability and with it a better absorption, on the other hand, the encapsulation percentages of the drug range from 54.05 ± 0.03 % to 78.58 ± 0.09 %. The results of this research show that this technology is a promising tool for the development of low solubility drug transport systems with high loading capacity of active ingredients.
The low solubility of some active ingredients is a challenge for the formulation of new and better drugs, therefore in recent years studies have intensified for the development of new platforms for the transport of low solubility drugs with which a good release, bioavailability and absorption are obtained, one of them is the microencapsulation by which hydrophobic active ingredients can be loaded effectively. The present research focuses on the production of solid lipid microparticles as a carrier system for low solubility drugs, the loading and quantification of active ingredients in the developed transport system. The microparticles were created from cetyl alcohol, stearic acid, palmitic acid and chitosan by the microemulsion method, using Tween 20 and 80 as emulsifier and Fexofenadine as active principle due to its low solubility in water. With these raw materials it was possible to develop three formulations, which were studied through laser diffraction with the help of a Mastersizer 3000+ Ultra particle analyzer by means of which the distribution of particle sizes was obtained. Additionally, for the quantification of Fexofenadine in capsulated in the prepared transport systems, a calibration curve was constructed with an external standard, preparing solutions whose concentrations were 0.09 mg/mL, 0.06 mg/mL, 0.03 mg/mL and 0.009 mg/mL. The absorbances were then read at a wavelength of 220 nm in an Agilent Technologies 8453 UV-Visible spectrophotometer. Finally, using the linear fitting equation, the concentration of Fexofenadine in each transport system was calculated. Among the relevant results of the work, it is highlighted the obtaining of at least 50% of microparticles with sizes smaller than 6.17 μm; which favors the dissolution rate, the bioavailability and with it a better absorption, on the other hand, the encapsulation percentages of the drug range from 54.05 ± 0.03 % to 78.58 ± 0.09 %. The results of this research show that this technology is a promising tool for the development of low solubility drug transport systems with high loading capacity of active ingredients.
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Palabras clave
Micropartículas, Difracción Laser, Fexofenadina, Transportador de fármacos, Tamaño de partícula, Principio activo
