ABSTRACT
Copaifera spp. essential oil (EOC) was extracted by hydrodistillation of Copaifera oleoresin (COR). The EOC was characterized by GC/MS and a novel EOC-loaded nanoemulsion was developed to enhance the EOC solubility and to evaluate its utility as antinflammatory. EOC contain 14 volatile compounds (including ß-caryophyllene: 51.52%) having a required HLB of 11. The Surfactant: EOC: Water ratio of 13:15:75 (%, w:w:w) produced the optimal formulation (particle size: 94.47 nm). The EOC-loaded nanoemulsion presented a pseudoplastic/thixotropic behavior with excellent shelf stability for 6 months. The anti-inflammatory effect of the nanoemulsion was more potent than that of the EOC, and statistically equal to diclofenac (50 mg/kg). The EOC-loaded nanoemulsion showed no oral acute toxicity (in mice) at 2000 mg/kg; hence, it is considered a nontoxic product. The development of the EOC-loaded nanoemulsion added value to both the COR and the EOC by providinga suitable formulation that could be used as an anti-inflammatory product.
El aceite esencial (EOC) fue extraído por hidrodestilación de oleoresina de Copaifera spp. El EOC fue caracterizado químicamente por GC/MS. Se formuló una nanoemulsión con EOC para mejorar la solubilidad del EOC y evaluar su utilidad como antiinflamatorio. El EOC contiene 14 compuestos volátiles (incluido el ß-cariofileno: 51,52%) con un HLB requerido de 11. La relación Tensioactivo: EOC: Agua de 13:15:75 (%, p:p:p) produjo la formulación óptima (tamaño de partícula: 94,47 nm).. La nanoemulsión cargada con EOC presentó un comportamiento pseudoplástico/tixotrópico con una excelente estabilidad en almacenamiento durante 6 meses. El efecto antiinflamatorio de la nanoemulsión fue más potente que el del EOC y estadísticamente igual al diclofenaco (50 mg/kg). La nanoemulsión cargada con COE no mostró toxicidad aguda oral (en ratones) a 2000 mg/kg; por lo tanto, se considera un producto no tóxico. El desarrollo de la nanoemulsión cargada con EOC agregó valor tanto al COR como al EOC al proporcionar una formulación adecuada que podría usarse como un producto antiinflamatorio.
Subject(s)
Animals , Mice , Oils, Volatile/pharmacology , Fabaceae/chemistry , Anti-Inflammatory Agents/pharmacology , Rheology , Surface-Active Agents , Temperature , Oils, Volatile/chemistry , Toxicity Tests, Acute , Emulsions/pharmacology , Nanoparticles , Polycyclic Sesquiterpenes/analysis , Hydrogen-Ion Concentration , Gas Chromatography-Mass SpectrometryABSTRACT
Abstract The main constituents of the Euterpe oleracea Mart., Arecaceae, fruits (açaí) are anthocyanins. This paper aimed to standardize the extraction process and characterize an anthocyanin-rich dry extract obtained from this fruit. A 23 full factorial design was used. The volumes of ethanol 92% and acetic acid and the extraction time were used as factors. Total solids and anthocyanins content were used as feedback. The dry extract was obtained by freeze-drying. The content of anthocyanins was determined spectrophotometrically. Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimeter, Thermogravimetry, Scanning Electron Microscopy, and Atomic Absorption Spectrometry were used for characterizingthe dry extract. The DPPH method was used for evaluating radical scavenging activity. The extraction conditions were established. The most influent factor was the volume of acetic acid. The dry extract moisture content was equal to 1.39 ± 0.25%, the evaporation residue 97.25 ± 1.28%, total ashes 0.62 ± 0.12%, and the anthocyanin content was 61.75 ± 3.28%. The elemental composition shows the presence of manganese 4.85 ppm, iron 1.62 ppm, zinc 0.05, copper 1.38 ppm, calcium 1.01 ppm, cadmium 0.003 ppm, nickel 0.37 ppm, and lead 0.38 ppm. The dried extract IC50 estimated by the radical scavenging assay with DPPH was 31.25 ± 2.31 ppm. The optimal extraction conditions were: the volume of ethanol 92%: 400 ml; volume of acetic acid: 75 ml; an extraction time: 4 h.