Microencapsulation of fish oil by casein-pectin complexes and gum arabic microparticles: oxidative stabilisation.

This study was aimed to microencapsulate fish oil (FO) in two biocompatible polymeric blends: gum arabic (GA)-maltodextrin (MD) and casein-pectin (CP)-MD. GA-MD microparticles and CP-MD microparticles were produced by spray-drying and complex coacervation and spray-drying, respectively. Encapsulation efficiency, particle size, moisture content, oxidative stability, and morphological properties were analysed. Encapsulation efficiencies of 51.2-56.8% (w/v) for GA and 64.7-67.9% (w/v) for CP preparations were found. GA particle sizes varied from 2 to 100 µm and from 2 to 120 µm for CP microparticles. Spherical forms with depressions in the topography of both systems were evidenced by scanning electron microscopy. Confocal microscopy evidenced surface oil on GA microparticles, corroborating encapsulation efficiency. CP was more efficient than GA to reduce oxidation, with maximum peroxide values (PVs) of 17.40 mmol/kg oil after 28 d at 40 °C/75% relative humidity (RH). Thus, CP is a promising biopolymeric blend for encapsulation of FO that provides protection against lipid oxidation.

Fish oil attenuates persistent inflammatory pain in rats through modulation of TNF-α and resolvins.

UNLABELLED: Fish oil (FO), source of omega-3 fatty acids (FA), has been widely studied in the treatment of inflammatory diseases and inflammatory pain (IP). Omega-3 FA give rise to eicosapentaenoic (EPA) and docosahexaenoic (DHA) acids, metabolized to eicosanoids and converted to resolvins with important anti-inflammatory action. AIMS: This study investigates the effects of oral doses of omega-3 FA from FO and concentrated fish oil (CFO) in a model of sub-chronic IP, induced by Complete Freund's Adjuvant (CFA). MAIN METHODS: IP was induced by intraplantar injection of CFA into the right hind paw of Wistar rats. Three groups were pre-treated with omega-3 FA: two groups received CFO (460mg of EPA/360mg of DHA and 690mg of EPA/540mg of DHA) and one group received natural FO (460mg EPA/300mg DHA), for 7days before IP induction (pre-treatment) and 5days after induction (treatment). KEY FINDINGS: TNF-α levels were reduced by CFO 690 (67.9%; p<0.01), CFO 460 (57.7%; p<0.01), FO 460 (26.2%), compared to the augment promoted by CFA (549.7%; p<0.001). Resolvin levels were increased in treated groups with respect to the CFA control group (CFO 690=3196.3%, p<0.01; CFO 460=3347.1%, p<0.01; FO=1653.5%). SIGNIFICANCE: The results indicate that the tested doses reduced inflammatory pain effectively in a short pre-treatment period, through modulation of TNF-α and resolvins and that CFO presented better results than FO. Therefore, Ω-3 FA from FO can be proposed for use as complementary medicine in the treatment of painful and inflammatory diseases.

Impact of cross-linking and drying method on drug delivery performance of casein-pectin microparticles.

Pectin is a heteropolysaccharide which has been investigated for the development of colon-specific drug delivery systems. Polymers have been associated with pectin to reduce its aqueous solubility and improve the performance of drug delivery systems. Pectin-casein interaction is widely known in food research, but it has not been fully considered by pharmaceutical scientists. Thus, this study investigated the potential of casein-pectin microparticles as a drug delivery system and clarified the impact of cross-linking and drying methods on the in vitro release of indomethacin (IND) or acetaminophen (PCT) from microparticles. Microparticles were prepared by coacervation and dried by spray or spouted bed methods. Drug recovery, in vitro drug release, size, morphology, and the thermal and diffractometric properties of dried microparticles were determined. Spray-dried non-cross-linked microparticles were able to prolong IND release, and pectin was still degraded by pectinolytic enzymes. On the other hand, glutaraldehyde cross-linking prevented the enzymatic breakdown of pectin without improving IND release. Spouted bed drying reduced IND recovery from all microparticles when compared with spray drying, thus the successful spouted bed drying of microparticles depends on the chemical characteristics of both the drug and the polymer. Release data from PCT microparticles suggested that the microparticle formulation should be improved to bring about a more efficient delivery of water-soluble drugs. In conclusion, casein-pectin microparticles show great potential as a drug delivery system because casein reduces the water solubility of pectin. The drying method and cross-linking process had significant effects on the in vitro performance of these microparticles.

Anti-inflammatory activity of essential oils from Syzygium cumini and Psidium guajava.

CONTEXT: Despite the many biological activities reported for essential oils, their anti-inflammatory ability is relatively underexplored considering the wide variation in plant sources and in their volatile composition. Oils from Syzygium cumini Skells (SC) and Psidium guajava L. (PG) (Myrtaceae) have been described as having diverse pharmacological activities. OBJECTIVE: The current study seeks to evaluate the anti-inflammatory activity of the essential oils from the leaves of SC and PG, as well as some of their terpene-enriched fractions (+V = more volatile and -V = less volatile) obtained by vacuum distillation. Both the pharmacological responses and chemical compositions were correlated. MATERIALS AND METHODS: The relative contents of the oils and their fractions were evaluated by gas chromatography. Individual constituents in the oils were characterized by gas chromatography coupled to mass spectrometry. Anti-inflammatory activity was accessed in the lipopolysaccharide-induced pleurisy model, by measuring the inhibition of total leukocyte, neutrophil and eosinophil migration in the mice pleural lavage, after oil treatment with the oils at 100 mg/kg. RESULTS: Eosinophil migration was inhibited by SC (67%), SC (+V) (63%), PG (76%), PG (+V) (67%) and PG (-V) (74%). This efficacy was correlated with the presence of ß-pinene and ß-caryophyllene in the oils, a result that was reinforced by evaluating both these pure components (38 and 50% inhibition, respectively). Synergistic effects associated with the presence of α-pinene were speculated. DISCUSSION AND CONCLUSION: Essential oils from SC and PG may be useful to treat inflammatory diseases by mechanisms that include the inhibition of eosinophil migration.

Linalool from Lippia alba: study of the reproducibility of the essential oil profile and the enantiomeric purity.

A new chemotype of the aromatic Verbenaceae species Lippia alba Mill. N. E. Br. from southeastern Brazil has recently been shown to have a high content of linalool in the leaf essential oil. Vegetative propagation of this chemotype was conducted at six different locations in Brazil, and the variation of the content and the optical purity of linalool in the oils were verified. Yields (0.6-0.9%, hydrodistillation), chemical composition, linalool content, and optical purity of the oils from all the plants were compared, using GC-FID, GC-MS, chiral chromatography, and retention index calculation. No plant exceeded the matrix in linalool content (46.5 to 90.7%), and the chemical profile of the oils was the same for all the samples. Purification of linalool to a content close to 100% was effected by vacuum distillation of the crude oil. Chiral analysis showed exclusively the presence of S-linalool in all the crude oils and in the distilled samples.