RESUMEN
Torch ginger, Etlingera elatior, is a Zingiberaceae plant with various red, pink, and white inflorescence. The wound healing potential and anti-aging effects of freeze-dried torch ginger inflorescence extracts (FTIEs) from three varieties were compared. The red FTIE had the highest content of phenolic, flavonoid, caffeoylquinic acid, and chlorogenic acid, followed by the white and pink FTIE. Consistent with the chemical constituents, the red FTIE demonstrated the greatest capacities for free radical scavenging, anti-tyrosinase, and anti-collagenase activity, followed by the white and pink FTIE. In cell-based studies, FTIEs displayed cytotoxicity to B16F10 melanoma cells, with the red FTIE showing the greatest activity (LC50 of 115.5 µg/mL). In contrast, the pink and the white FTIEs had less cytotoxicity impact. Nonetheless, at 1000 µg/mL, all three FTIE variants were safe on L929 fibroblasts or RAW 264.7 monocyte cells. White FTIE (500 µg/mL) exhibited the highest activity in stimulating collagen production and the greatest impact on cell migration, whereas the pink and red FTIE had a lesser effect. All FTIEs slightly suppressed the pro-inflammatory cytokines produced by lipopolysaccharide-stimulated monocytes, with no significant variation between FTIE variants. In conclusion, all FTIEs revealed promising potential for anti-aging cosmeceuticals and wound care products at specific concentrations.
Asunto(s)
Extractos Vegetales , Zingiberaceae , Extractos Vegetales/farmacología , Extractos Vegetales/química , Inflorescencia , Zingiberaceae/química , Cicatrización de HeridasRESUMEN
The purpose of this study was to improve in vitro dissolution and in vivo absorption of itraconazole (ITZ), a poorly water-soluble drug, by means of novel pectin-based nanoparticles prepared from nanoemulsion templates. Nanoemulsion templates were prepared by a high-pressure homogenization using pectin (i.e., 0.5-3.0%w/w low-methoxyl pectin (LMP), amidated low-methoxyl pectin (ALMP), or high-methoxyl pectin (HMP)) as an emulsifier and chloroform as an oil phase. HMP provided good oil-in-water emulsions with ITZ loaded in the oil phase. The chloroform in nanoemulsions was then removed to produce the suspensions of nanoparticles dispersed in water phase. After lyophilization, the dried core-shell nanoparticles with good properties in terms of redispersibility, dissolution, and stability were obtained. The alteration of ITZ crystallinity was clearly observed from powder X-ray diffractogram while no interaction between ITZ and pectin was found in the nanoparticles. The ITZ-loaded nanoparticles showed high percent drug dissolved, especially those prepared from HMP, and could maintain their good dissolution properties even after 6-month storage. The in vivo absorption study in fasted rats demonstrated that pectin-based nanoparticles prepared from nanoemulsion templates could improve absorption of ITZ, that is, 1.3-fold higher than the ITZ commercial product (p<0.05). Pectin type highly influenced the dissolution properties and also in vivo plasma profile. These findings suggested that HMP-based nanoparticles seem to be a promising formulation due to their high AUC(0-24h) and C(max).
Asunto(s)
Nanopartículas/química , Pectinas/química , Agua/química , Absorción , Animales , Área Bajo la Curva , Química Farmacéutica , Estabilidad de Medicamentos , Emulsiones/administración & dosificación , Emulsiones/química , Itraconazol/administración & dosificación , Itraconazol/química , Itraconazol/farmacocinética , Masculino , Nanopartículas/administración & dosificación , Aceites/química , Tamaño de la Partícula , Pectinas/administración & dosificación , Pectinas/farmacocinética , Ratas , Ratas Wistar , Solubilidad , Suspensiones/administración & dosificación , Suspensiones/químicaRESUMEN
Understanding the gel ultrastructure is of great importance for process and product development having great effects on the product characteristics. The samples containing high amount of water could not be directly observed using scanning electron microscope (SEM) without removing of water. However, cryo-SEM can be used to study the ultrastructure of hydrated samples. In this study, ultrastructural information of internal structure was obtained by imaging the cryo-fractured beads in a cryo-SEM. This technique was found to be excellent for studying the detailed morphology of structural development and showed better images than normal SEM procedures using freeze-drying for sample preparation. Also, the studies illustrated a morphological change, e.g. from net-like structure to membranous structure caused by syneresis, accompanied by a significant increase in mechanical properties, when the beads are formed by ionotropic gelation. The gelation time of 20 min was found to be the minimum for a complete bead formation, based on the mechanical and SEM data. The results demonstrate the advantageous of cryo-SEM for examining the ultrastructure during bead formation of calcium pectinate.