Annatto seeds (
Bixa orellana
L.) are a natural source of norbixin, a carotenoid with antioxidant activity and an intense yellow–orange color which is a commonly used food and beverage colorant. ...However, it is susceptible to environmental factors such as light, oxygen, and temperature. Microencapsulation presents an alternative for improving the bioactive compound’s stability. In this study, norbixin microcapsules (MCN) were added to isotonic tangerine soft drinks in a quantity not exceeding food additive regulations. The final concentration was 2.86 ± 0.02 µg norbixin/mL, and according to the CIELab system, the beverage acquired the expected orange tonality. The addition of MCN favorably affects beverage stability during storage under accelerated conditions (heat and light), and the half-life time was more significant (29.71 days) than when non-encapsulated norbixin was used (393.39 min). In conclusion, MCN should be considered as an additive with potential use in processed beverage industries instead of synthetic dyes.
Yerba-mate contains in its composition a high concentration of phenolic compounds. This class of secondary metabolites exhibits strong values of molar absorptivity on ultraviolet and visible ...wavelengths. This study evaluated the effect of yerba-mate extracts on the in vitro solar protection factor (SPF) value of sunscreen formulations. The sunscreen formulations were prepared to have non-ionic lotion as a basis and yerba-mate extract and/or avobenzone as active agents. The SPF and resveratrol protective effect of the formulations were determined by UV-vis spectrometry. A synergic effect between the yerba-mate extract and avobenzone on the SPF was found. Yerba-mate extract at 5% improved the SPF of the avobenzone 5% formulation from 28.46 ± 5.45 to 40.48 ± 0.84. Yerba-mate extract at 5% avoided resveratrol degradation by ultraviolet radiation. At this same concentration, avobenzone produced a smaller effect than yerba-mate extracts in resveratrol protection. The formulations with yerba-mate + avobenzone presented smaller changes in pH values during 12 days of storage. The spreadability profile of yerba-mate and avobenzone formulations was similar to the profile of avobenzone formulations. The results reported here show the suitability of the yerba-mate extract use in photoprotective formulations, highlighting their in vitro effect and opening possibilities for new investigations exploring this property.
LIPID-CORE NANOCAPSULES: PREPARATION, CHARACTERIZATION AND BIOLOGICAL APPLICATIONS. Lipid-core nanocapsules (LNCs) are core-shell structures, in which the core is an organogel formed by a solid lipid ...dispersed in a triglyceride, and the shell is a polymer. Those nanocapsules encapsulate poorly-water soluble drugs by dispersion in the core and/or interaction with the polymer. The core and the shell act as diffusional barriers differenting the LNC from previously developed polymeric nanocapsules containing an oily core and a polymer shell, which unique diffusional barrier is the shell. In this review, we discuss the supramolecular structure, the physico-chemical characterization, including sizing, surface potential, fluorescent labeling strategies, as well as the interfacial reactions in water to coat and functionalise the LNC surface. Different organometallic complexes have been synthesized to decorate the nanocapsules envisaging the treatment of atherosclerosis, cancer, mucopolysaccharidosis I, and hypertension. We also describe the main applications of the nanoformulations in the pharmaceutical, medical, and veterinary fields, including in vitro and in vivo evaluations of toxicity and efficacy.
Several studies have reported that orally ingested trans-resveratrol is extensively metabolized in the enterocyte before it enters the blood and target organs. Additionally, trans-resveratrol is ...photosensitive, easily oxidized and presents unfavorable pharmacokinetics. Therefore, it is of great interest to stabilize trans-resveratrol in order to preserve its biological activities and to improve its bioavailability in the brain. Here, trans-resveratrol was loaded into lipid-core nanocapsules and analyzed for particle size, polydispersity and zeta potential. The nanocapsule distribution in brain tissue was evaluated by intraperitoneal (i.p.) and gavage routes in healthy rats. The lipid-core nanocapsules had a mean diameter of 241 nm, a polydispersity index of 0.2, and a zeta potential of -15 mV. No physical changes were observed after 1, 2 and 3 months of storage at 25 degrees C. Lipid-core nanocapsules showed high entrapment of trans-resveratrol and displayed a higher trans-resveratrol concentration in the brain, the liver and the kidney after daily i.p. or gavage administration than that observed for the free trans-resveratrol. Because trans-resveratrol is a potent cyclooxygenase-1 inhibitor, gastrointestinal damage was evaluated. The animals that were administered with trans-resveratrol-loaded lipid-core nanocapsules showed significantly less damage when compared to those administered with free trans-resveratrol. In summary, lipid-core nanocapsules exhibited great trans-resveratrol encapsulation efficiency. trans-Resveratrol-loaded lipid-core nanocapsules increased the concentration of trans-resveratrol in the brain tissue. Gastrointestinal safety was improved when compared with free trans-resveratrol. Thus, trans-resveratrol-loaded lipid-core nanocapsules may be used as an alternative potential therapeutic for several diseases including Alzheimer's disease.
Schizophrenia (SCZ) response to pharmacological treatment is highly variable. Quetiapine (QTP) administered as QTP lipid core nanocapsules (QLNC) has been shown to modulate drug delivery to the brain ...of SCZ phenotyped rats (SPR). In the present study, we describe the brain concentration–effect relationship after administrations of QTP as a solution or QLNC to SPR and naïve animals. A semimechanistic pharmacokinetic (PK) model describing free QTP concentrations in the brain was linked to a pharmacodynamic (PD) model to correlate the drug kinetics to changes in dopamine (DA) medial prefrontal cortex extracellular concentrations determined by intracerebral microdialysis. Different structural models were investigated to fit DA concentrations after QTP dosing, and the final model describes the synthesis, release, and elimination of DA using a pool compartment. The results show that nanoparticles increase QTP brain concentrations and DA peak after drug dosing to SPR. To the best of our knowledge, this is the first study that combines microdialysis and PK/PD modeling in a neurodevelopmental model of SCZ to investigate how a nanocarrier can modulate drug PK and PD, contributing to the development of new treatment strategies for SCZ.
The main objective of this work was to develop a nanotechnology-based component containing substances of vegetable origin, such as butters and essential oils, whose properties may help balance the ...vulvovaginal microbiota and be applied in nonwovens for feminine hygiene products. The high-pressure homogenization technique was used to obtain the aqueous dispersion of these nanoparticles containing tea tree oil, alpha-bisabolol, resveratrol, grape seed oil and citric acid, namely VM-Theospheres (theospheres are nanoparticles formed by Theobroma grandiflorum butter). The average particle size range was 274 ± 5 nm. The stability tests indicated that formulation status remained stable at room temperature for 28 days. In vitro analysis of skin penetration and irritation showed that the VM-Theospheres can be considered safe for use in feminine hygiene products. The production of an absorbent layer was performed by impregnation of VM-Theospheres in nonwovens. The results revealed that spraying was the most effective method, without the need to treat the samples first.
Melatonin has been described in the literature as a potent antioxidant. However, melatonin presents variable, low bioavailability and a short half-life. The use of polymeric nanoparticulated systems ...has been proposed for controlled release. Thus, the purpose of this study was to investigate the action of melatonin-loaded lipid-core nanocapsules (Mel-LNC) in the antioxidant system of Caenorhabditis elegans, and the possible protective effect of this formulation against lipid peroxidation caused by paraquat (PQ).
The suspensions were prepared by interfacial deposition of the polymer and were physiochemically characterized. C. elegans N2 wild type and transgenic worm CF1553, muls84 sod-3p::gfp; rol6(su1006) were obtained from the Caenorhabditis Genetics Center (CGC). The worms were divided into 5 groups: Control, PQ 0.5 mM, PQ 0.5 mM + Mel-LNC 10 μg/mL, PQ + unloaded lipid-core nanocapsules (LNC), and PQ + free melatonin (Mel) 10 μg/mL. The lipid peroxidation was assessed through thiobarbituric acid (TBARS) levels and the fluorescence levels of the transgenic worms expressing GFP were measured.
The LNC and Mel-LNC presented a bluish-white liquid, with pH values of 5.56 and 5.69, respectively. The zeta potential was - 6.4 ± 0.6 and - 5.2 ± 0.2, respectively. The mean particle diameter was 205 ± 4 nm and 203 ± 3 nm, respectively. The total melatonin content was 0.967 mg/ml. The TBARS levels were significantly higher in the PQ group when compared to the control group (p < 0.001). Mel-LNC reduced TBARS levels to similar levels found in the control group. Moreover, only Mel-LNC significantly enhanced the SOD-3 expression (p < 0.05). Mel-LNC was capable of protecting C. elegans from lipid peroxidation caused by PQ and this was not observed when free melatonin was used. Moreover, Mel-LNC increased the fluorescence intensity of the transgenic strain that encodes the antioxidant enzyme SOD-3, demonstrating a possible mechanism of protection from PQ-induced damage.
These findings demonstrated that melatonin, when associated with nanocapsules, had improved antioxidant properties and the protective activity against PQ-induced lipid peroxidation could be associated with the activation of antioxidant enzymes by Mel-LNC in C. elegans.
The use of carotenoids in foods is limited due to their poor solubility in water-rich matrices, and the nanoencapsulation emerges as an alternative to allowing the solubilization and to protect the ...carotenoids against degradation. The aims of this study were to produce, by the interfacial deposition of the preformed polymer, to characterize, and evaluate the stability of nanocapsules obtained from a blend of β-carotene, α-carotene, and lutein (BALNs) and nanocapsules of synthetic β-carotene (BNs). The encapsulation efficiency, transmission electron microscopy, and the logarithm of the distribution of the coefficient of the BALNs and BNs, with 26 μg/mL of carotenoids, were performed after preparation. During 100 days of storage (4 °C) for the BALNs and BNs, the carotenoids retention, hydrogen potential, color, particle diameter, and the zeta potential were analyzed. The
z
-average and zeta potential after 100 days of storage for the BALNs and BNs were, respectively, 166.53 ± 4.71 nm/−18.37 ± 2.06 mV and 190.90 ± 7.87 nm/−9.08 ± 1.23 mV. At the end of storage, the β-carotene content was 67.62 ± 7.77 % (BALNs) and 11.69 ± 1.65 % (BNs). The β-carotene retention in the BALNs was higher than in the BNs probably due to the synergism that occurs among the compounds. Regardless of the decrease in the pH values and the b* coordinate, the formulations of the BALNs and BNs were considered physically stable during the storage. Nevertheless, beyond the physical stability, the BALNs presented a satisfactory carotenoid retention at end of storage.
Coccidiosis is a disease caused by intracellular protozoan parasites of the genus
that affect the intestinal tract of poultry. However, strain resistance and drug residue in the carcass have drawn ...the attention of the productive sector. The nanotechnology can improve the biological effect of drugs, reducing of administered doses and toxic effects. Due to this, toltrazuril-load polymeric nanoparticles based on Eudragit
S100 (NCt) or poly-ε-caprolactone (LNCt) were developed to prevent coccidiosis in broilers. Nanoformulations were produced and showed homogeneous particle diameter distribution in the nanometer range (
-average and D (4.3) < 200 nm), negative zeta potential (<-8.93 mV), drug content ~100%, and encapsulation efficiency >90%. Cell viability assays using avian fibroblasts showed that LNCt presented no relevant toxicity up to 72 h. LNCt was then prophylactically administrated to chicken followed by challenge with
oocysts. The evaluation of the small intestine and cecum showed that the treatment with LNCt (3.5 mg/kg/day) in drinking water reduced the lesion scores and oocysts excretion, similar to the reference medicine containing toltrazuril (Baycox
, 7 mg/kg/day). The current study shows the potential protective use of nanoencapsulating anticoccidial drugs as a promising approach for the control of coccidiosis in poultry.
Glioblastoma (GB) is a histological and genetically heterogeneous brain tumor that is highly proliferative and vascularized. The prognosis is poor with currently available treatment. In this study, ...we evaluated the cytotoxicity and antiangiogenic activity of doxorubicin-loaded-chitosan-coated-arginylglycylaspartic acid-functionalized-poly(ε-caprolactone)-alpha bisabolol-LNC (AB-DOX-LNC-L-C-RGD). The nanoformulation was prepared by self-assembling followed by interfacial reactions, physicochemically characterized and evaluated in vitro against GB cell lines (U87MG and U138MG) and in vivo using the chicken chorioallantoic membrane assay (CAM). Spherical shape nanocapsules had a hydrodynamic mean diameter of 138 nm, zeta potential of +13.4 mV, doxorubicin encapsulation of 65%, and RGD conjugation of 92%. After 24 h of treatment (U87MG and U138MG), the median inhibition concentrations (IC50) were 520 and 490 nmol L−1 doxorubicin-equivalent concentrations, respectively. The treatment induced antiproliferative activity with S-phase cell-cycle arrest and apoptosis in the GB cells. Furthermore, after 48 h of exposure, evaluation of antiangiogenic activity (CAM) showed that the relative vessel growth following treatment with the nanocapsules was 5.4 times lower than that with the control treatment. The results support the therapeutic potential of the nanoformulation against GB and, thereby, pave the way for future preclinical studies.
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