RESUMEN
Poor aqueous solubility and low bioavailability are limiting factors in the oral delivery of lipophilic drugs. In a formulation approach to overcome these limitations, rice bran (RB) oil was evaluated as drug carrier in the development of self-nanoemulsifying drug delivery systems (SNEDDS). The performance of RB in formulations incorporating Kolliphor RH40 or Kolliphor EL as surfactants and Transcutol HP as cosolvent was compared to a common oil vehicle, corn oil (CO). Serial dilutions of the preconcentrates were performed in various media [distilled water and simulated intestinal fluids mimicking fasted state (FaSSIF) and fed state (FeSSIF)] and at different dilution ratios to simulate the in vivo droplets' behavior. The developed SNEDDS were assessed by means of phase separation, droplet size, polydispersity index, and ζ-potential. Complex ternary diagrams were constructed to identify compositions exhibiting monophasic behavior, droplet size < 100 nm, and polydispersity index (PDI) < 0.25. Multifactor analysis and response surface areas intended to determine the factors significantly affecting droplet size. The oil capacity to accommodate lipophilic drugs was assessed via fluorescence spectroscopy based on the solvatochromic behavior of Nile Red. Solubility studies were performed to prepare fenofibrate- and itraconazole-loaded SNEDDS and assess their droplet size, whereas dissolution experiments were conducted in simulated intestinal fluids. Caco-2 cell viability studies confirmed the safety of the SNEDDS formulations at 1:100 and 1:1000 dilutions after cell exposure in culture for 4 h. The obtained results showed similar performance between RB and CO supporting the potential of RB as oil vehicle for the effective oral delivery of lipophilic compounds.
Asunto(s)
Sistemas de Liberación de Medicamentos/métodos , Emulsionantes/química , Nanopartículas/química , Aceite de Salvado de Arroz/química , Disponibilidad Biológica , Células CACO-2 , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Portadores de Fármacos/administración & dosificación , Portadores de Fármacos/química , Emulsionantes/administración & dosificación , Excipientes/administración & dosificación , Excipientes/química , Humanos , Nanopartículas/administración & dosificación , Tamaño de la Partícula , Aceite de Salvado de Arroz/administración & dosificación , Solubilidad , Tensoactivos/química , Agua/químicaRESUMEN
The effect of hop sourdough fermentation combined with rice bran (RB) addition was investigated for improving technological, bioactive and sensory properties of wheat bread by optimizing the quantities of RB, yeast, sourdough and hop extract contents based on response surface methodology. The bread produced according to the optimized formula was compared with control bread, sourdough or RB-enhanced bread with regard to quality attributes, bioaccessible phenolics and antioxidant activity. Sourdough fermentation combined with RB flour increased volume of loaves and consumer acceptance with no significant variations in crumb moisture content and crumb firmness during storage. RB darkened crumb while no effects on colour were observed for sourdough bread. Sourdough technology allowed increasing phenolic content of RB bread with no significant differences in its antioxidant activity. The bioaccessible ferulic and sinapic acids, the main phenolics released in vitro digestion of optimized bread were lower compared to those of control bread.