RESUMEN
Metformin is a drug commonly used for the treatment of type 2 diabetes. However, it has been associated with damaging side effects when used over a long period of time. A potential solution to this problem is the implementation of a prolonged-release system for metformin, which would enhance the efficiency of the doses administered to patients. To achieve this, it is necessary to use materials compatible with humans. Electrospinning is an efficient technique that can be employed for this purpose, utilizing solvents that are safe for human use. Therefore, the objective of this study was to prepare and characterize a system for the prolonged release of metformin from zein and gelatin through coaxial electrospinning as well as to investigate its in vitro release. Metformin-loaded zein/gelatin coaxial nanofibers were prepared using the coaxial electrospinning technique and then characterized by morphological, structural, and thermal analysis. Morphologically, metformin-loaded zein/gelatin coaxial nanofibers were obtained with an average diameter of 322.6 ± 44.5 nm and a smooth surface. Fourier transform infrared spectroscopy (FTIR) analysis showed band shifts at a higher wavenumber due to drug-protein interactions by hydrogen bonding between N-H and C=O groups. Thermal gravimetric analysis (TGA) results suggested a possible interaction between materials due to an increase in the degradation temperatures of zein and gelatin when metformin was included. The transition of the crystallinity of metformin to the amorphous form was also confirmed by differential scanning calorimetry (DSC). Coaxial nanofibers exhibited an encapsulation efficiency of 66% and a profile release that showed an initial release of metformin (40%) in the first hour, followed by a gradual release until it reached equilibrium at 60 h and a cumulative release of 97% of metformin. It was concluded that using the coaxial electrospinning technique, it is possible to obtain nanofibers from polymeric solutions of zein and gelatin to encapsulate metformin, with a potential application as a prolonged-release system.
RESUMEN
Quercetin is a hydrophobic flavonoid with high antioxidant activity. However, for biological applications, the bioavailability of quercetin is low due to physiological barriers. For this reason, an alternative is the protection of quercetin in matrices of biopolymers as zein. The objective of this work was to prepare and characterize quercetin-loaded zein nanoparticles by electrospraying and its study of in vitro bioavailability. The physicochemical parameters such as viscosity, density, and electrical conductivity of zein solutions showed a dependence of the ethanol concentration. In addition, rheological parameters demonstrated that solutions of zein in aqueous ethanol present Newtonian behavior, rebounding in the formation of nanoparticles by electrospraying, providing spherical, homogeneous, and compact morphologies, mainly at a concentration of 80% (v/v) of ethanol and of 5% (w/v) of zein. The size and shape of quercetin-loaded zein nanoparticles were studied by transmission electron microscopy (TEM), observing that it was entrapped, distributed throughout the nanoparticle of zein. Analysis by Fourier transform-infrared (FT-IR) of zein nanoparticles loaded with quercetin revealed interactions via hydrogen bonds. The efficacy of zein nanoparticles to entrap quercetin was particularly high for all quercetin concentration evaluated in this work (87.9 ± 1.5% to 93.0 ± 2.6%). The in vitro gastrointestinal release of trapped quercetin after 240 min was 79.1%, while that for free quercetin was 99.2%. The in vitro bioavailability was higher for trapped quercetin (5.9%) compared to free quercetin (1.9%), than of gastrointestinal digestion. It is concluded, that the electrospraying technique made possible the obtention of quercitin-loaded zein nanoparticles increasing their bioavailability. PRACTICAL APPLICATION: This type of nanosystems can be used in the food and pharmaceutical industry. Quercetin-loaded zein nanoparticles for its improvement compared to free quercetin can be used to decrease the prevalence of chronic degenerative diseases by increasing of the bioavailability of quercetin in the bloodstream. Other application can be as an antioxidant system in functional foods or oils to increase shelf life.
Asunto(s)
Composición de Medicamentos/métodos , Quercetina/química , Zeína/química , Antioxidantes/química , Antioxidantes/metabolismo , Disponibilidad Biológica , Biopolímeros/química , Línea Celular , Portadores de Fármacos/química , Composición de Medicamentos/instrumentación , Humanos , Enlace de Hidrógeno , Interacciones Hidrofóbicas e Hidrofílicas , Nanopartículas/química , Nanopartículas/metabolismo , Tamaño de la Partícula , Quercetina/metabolismo , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
Currently, electrospraying is a novel process for obtaining the nanoparticles from biopolymers. Zein nanoparticles have been obtained by this method and used to protect both hydrophilic and hydrophobic antioxidant molecules from environmental factors. The objective of this work was to prepare and characterize gallic acid-loaded zein nanoparticles obtained by the electrospraying process to provide protection to gallic acid from environmental factors. Thus, it was related to the concentration of gallic acid in physicochemical and rheological properties of the electrosprayed solution, and also to equipment parameters, such as voltage, flow rate, and distance of the collector in morphology, and particle size. The physicochemical properties showed a relationship in the formation of a Taylor cone, in which at a low concentration of gallic acid (1% w/v), low viscosity (0.00464 ± 0.00001 Pa·s), and density (0.886 ± 0.00002 g/cm3 ), as well as high electrical conductivity (369 ± 4.3 µs/cm), forms a stable cone-jet mode. The rheological properties and the Power Law model of the gallic acid-zein electrosprayed solution demonstrated Newtonian behavior (n = 1). The morphology and size of the particle were dependent on the concentration of gallic acid. Electrosprayed parameters with high voltage (15 kV), low flow rate (0.1 mL/hr), and short distance (10 cm) exhibited a smaller diameter and spherical morphology. FT-IR showed interaction in the gallic acid-loaded zein nanoparticle by hydrogen bonds. Therefore, the electrospraying process is a feasible technique for obtaining gallic acid-loaded zein nanoparticles and providing potential protection to gallic acid from environmental factors.