Alginate particles for encapsulation of phenolic extract from Spirulina sp. LEB-18: physicochemical characterization and assessment of in vitro gastrointestinal behavior

Encapsulation can be used as a strategy to protect and control the release of bioactive extracts. In this work, an extract from Spirulina sp. LEB-18, rich in phenolic compounds, was encapsulated in biopolymeric particles (i.e., composed of alginate) and characterized concerning their thermal behavior using differential scanning calorimetry (DSC), size, morphology, swelling index (S), and encapsulation efficiency (EE%); the release profile of the phenolic compounds at different pHs and the particle behavior under in vitro gastrointestinal digestion were also evaluated. It was shown that it is possible to encapsulate the phenolic extract from Spirulina sp. LEB-18 in alginate particles with high encapsulation efficiency (88.97%). It was also observed that the particles are amorphous and that the encapsulated phenolic compounds were released at a pH 7.2 but not at pH 1.5, which means that the alginate particles are able to protect the phenolic compounds from the harsh stomach conditions but lose their integrity under intestinal pH conditions. Regarding bioaccessibility, it was observed that the encapsulated phenolic compounds showed higher bioaccessibility compared to phenolic compounds in free form. This work increases the knowledge about the behavior of alginate particles encapsulating phenolic compounds during in vitro gastrointestinal digestion. It also provides essential information for designing biopolymeric particle formulations encapsulating phenolic compounds for application in pharmaceutical and food products.The study was financially supported by the following programs and institutions: Science Without Borders—CNPq (Conselho Nacional de Desenvolvimento Científico e Tecnológico), CSF (Ciência sem fronteiras), CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior), Brazil, the University of Minho, Braga, Portugal, and Foundation for Science and Technology (FCT, POPH-QREN and FSE Portugal). This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UIDB/04469/2020 unit, and by LABBELS–Associate Laboratory in Biotechnology, Bioengineering and Microelectromechanical Systems, LA/P/0029/2020.info:eu-repo/semantics/publishedVersio

Effects of consumption of galactooligosaccharides obtained through whey enzymatically modified on the faecal flora and nutritional parameters of hamsters

The aim of this research was to evaluate the influence of wheyenzymatically modified rich in galactooligosaccharides in thenutritional characteristics and effects in the microflora of cecumcontents by the study with Golden Syrian hamsters (Mesocricetusauratus) for 28 days (controlled conditions). Three isoproteic dietswere prepared (20% w/w): C (casein), W (whey) and G (wheymodified). The groups studied differed positively from the C regardingfeed and protein efficiency ratio. The relationships (w/w) oforgan/body were found proportional in all diets. The counts ofprobiotics from the cecum contents the groups showed no difference.The pHs of studied groups were lower than C, this acidity can atimpairs the ability of pathogens to grow in the intestine. Resultssuggest that using whey enzymatically modified rich ingalactooligosaccharides could replace the standard diet withnutritional efficiency and possible inhibit the microorganismspathogenic without induce damage in health.Fil: Dos Santos Da Fonseca, Renata Aline. Universidade Federal Do Rio Grande; Brasil. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; ArgentinaFil: Rodrigues Machado, Adriana. Universidade Federal Do Rio Grande; BrasilFil: Muniz Moreira, Lidiane. Universidade Federal Do Rio Grande; BrasilFil: Rodrigues, Rosane S.. Universidade Federal de Pelotas; BrasilFil: Machado, Mirian. Universidade Federal de Pelotas; BrasilFil: Souza Soares, Leonor A.. Universidade Federal Do Rio Grande; BrasilFil: Burkert, Carlos André V.. Universidade Federal Do Rio Grande; BrasilFil: Burkert, Janaína Fernandes de Medeiros. Universidade Federal Do Rio Grande; Brasi

Omecamtiv mecarbil in chronic heart failure with reduced ejection fraction, GALACTIC‐HF: baseline characteristics and comparison with contemporary clinical trials

Aims: The safety and efficacy of the novel selective cardiac myosin activator, omecamtiv mecarbil, in patients with heart failure with reduced ejection fraction (HFrEF) is tested in the Global Approach to Lowering Adverse Cardiac outcomes Through Improving Contractility in Heart Failure (GALACTIC‐HF) trial. Here we describe the baseline characteristics of participants in GALACTIC‐HF and how these compare with other contemporary trials. Methods and Results: Adults with established HFrEF, New York Heart Association functional class (NYHA) ≥ II, EF ≤35%, elevated natriuretic peptides and either current hospitalization for HF or history of hospitalization/ emergency department visit for HF within a year were randomized to either placebo or omecamtiv mecarbil (pharmacokinetic‐guided dosing: 25, 37.5 or 50 mg bid). 8256 patients [male (79%), non‐white (22%), mean age 65 years] were enrolled with a mean EF 27%, ischemic etiology in 54%, NYHA II 53% and III/IV 47%, and median NT‐proBNP 1971 pg/mL. HF therapies at baseline were among the most effectively employed in contemporary HF trials. GALACTIC‐HF randomized patients representative of recent HF registries and trials with substantial numbers of patients also having characteristics understudied in previous trials including more from North America (n = 1386), enrolled as inpatients (n = 2084), systolic blood pressure < 100 mmHg (n = 1127), estimated glomerular filtration rate < 30 mL/min/1.73 m2 (n = 528), and treated with sacubitril‐valsartan at baseline (n = 1594). Conclusions: GALACTIC‐HF enrolled a well‐treated, high‐risk population from both inpatient and outpatient settings, which will provide a definitive evaluation of the efficacy and safety of this novel therapy, as well as informing its potential future implementation

Development and In Vitro Cytotoxicity of Citrus sinensis Oil-Loaded Chitosan Electrostatic Complexes

Electrostatic complexes based on chitosan, lecithin, and sodium tripolyphosphate were produced and evaluated with respect to their encapsulation capacity and cytotoxicity. Physical chemical properties were determined by zeta potential values and size distributions. For encapsulation assays, the emulsification method was followed, and Citrus senensis peel oil was utilized as volatile compound model. Morphology of complexes with oil incorporated was observed by scanning electron microscopy. The cytotoxicity of complexes was related to cell viability of zebrafish hepatocytes. The complexes produced presented positive Zeta potential values and size distributions dependent on the mass ratio between compounds. Higher concentrations of sodium tripolyphosphate promote significant changes (p < 0.05) in zeta values, which did not occur at smaller concentrations of the crosslinking agent. These complexes were able to encapsulate Citrus sinensis peel oil, with encapsulation efficiency higher than 50%. Cytotoxicity profiles showed that in a range of concentrations (0.1–100 μg/mL) studied, they did not promote cellular damage in zebrafish liver cells, being potential materials for food and pharmaceutical applications

Development and In Vitro Cytotoxicity of <i>Citrus sinensis</i> Oil-Loaded Chitosan Electrostatic Complexes

Electrostatic complexes based on chitosan, lecithin, and sodium tripolyphosphate were produced and evaluated with respect to their encapsulation capacity and cytotoxicity. Physical chemical properties were determined by zeta potential values and size distributions. For encapsulation assays, the emulsification method was followed, and Citrus senensis peel oil was utilized as volatile compound model. Morphology of complexes with oil incorporated was observed by scanning electron microscopy. The cytotoxicity of complexes was related to cell viability of zebrafish hepatocytes. The complexes produced presented positive Zeta potential values and size distributions dependent on the mass ratio between compounds. Higher concentrations of sodium tripolyphosphate promote significant changes (p < 0.05) in zeta values, which did not occur at smaller concentrations of the crosslinking agent. These complexes were able to encapsulate Citrus sinensis peel oil, with encapsulation efficiency higher than 50%. Cytotoxicity profiles showed that in a range of concentrations (0.1–100 μg/mL) studied, they did not promote cellular damage in zebrafish liver cells, being potential materials for food and pharmaceutical applications

Liposomes loaded with phenolic extracts of Spirulina LEB-18: Physicochemical characterization and behavior under simulated gastrointestinal conditions

Liposomes composed of rice (RL) and soybean (SL) lecithins were produced by reverse phase evaporation and used for the encapsulation of phenolic extracts from Spirulina LEB-18 (S-RL and S-SL for liposomes of rice and soybean lechitin, respectively). Liposomes were characterized in terms of size distribution, polydispersity index, and ?-potential; the chemical interactions between the phenolic compounds from Spirulina and liposomes were evaluated by Fourier Transform Infrared Spectroscopy (FTIR), and X-ray diffraction (XRD) and differential scanning calorimetry (DSC) were used to evaluate their crystallinity pattern. The release behavior of phenolic extracts was evaluated under two different pH conditions. Afterwards, in vitro digestibility of liposomes was evaluated in a dynamic gastrointestinal system. Liposomes exhibited high encapsulation efficiency (88.28% and 97.35% for S-RL and S-SL, respectively) and sizes ranging between 250 and 291?nm, showing to be good candidates for the encapsulation of phenolic extracts obtained from microalgae. Results showed that liposomes are stable at low pH values and that they are able to resist to the stomach conditions but they lose their integrity under intestinal conditions. This work increases the knowledge about the effects of in vitro gastrointestinal digestion on liposomes and provides important information for the design of liposome formulations aiming their application in pharmaceutical and food applications.The authors thank FURG and, FAPERGS, RS, Brasil; Science Without Borders -CNPq, CSF, Brasil; University of Minho, Braga, Portugal; and Fundação para a Ciência Tecnologia (FCT, POPH-QREN and FSE Portugal). The author Ana C. Pinheiro is recipient of a fellowship from the Fundação para a Ciência Tecnologia (FCT, Portugal) through grant SFRH/BPD/101181/2014.info:eu-repo/semantics/publishedVersio

Alginate Particles for Encapsulation of Phenolic Extract from Spirulina sp. LEB-18: Physicochemical Characterization and Assessment of In Vitro Gastrointestinal Behavior

Encapsulation can be used as a strategy to protect and control the release of bioactive extracts. In this work, an extract from Spirulina sp. LEB-18, rich in phenolic compounds, was encapsulated in biopolymeric particles (i.e., composed of alginate) and characterized concerning their thermal behavior using differential scanning calorimetry (DSC), size, morphology, swelling index (S), and encapsulation efficiency (EE%); the release profile of the phenolic compounds at different pHs and the particle behavior under in vitro gastrointestinal digestion were also evaluated. It was shown that it is possible to encapsulate the phenolic extract from Spirulina sp. LEB-18 in alginate particles with high encapsulation efficiency (88.97%). It was also observed that the particles are amorphous and that the encapsulated phenolic compounds were released at a pH 7.2 but not at pH 1.5, which means that the alginate particles are able to protect the phenolic compounds from the harsh stomach conditions but lose their integrity under intestinal pH conditions. Regarding bioaccessibility, it was observed that the encapsulated phenolic compounds showed higher bioaccessibility compared to phenolic compounds in free form. This work increases the knowledge about the behavior of alginate particles encapsulating phenolic compounds during in vitro gastrointestinal digestion. It also provides essential information for designing biopolymeric particle formulations encapsulating phenolic compounds for application in pharmaceutical and food products

Design, Immune Responses and Anti-Tumor Potential of an HPV16 E6E7 Multi-Epitope Vaccine

<div><p>Cervical cancer is a common type of cancer among women worldwide and infection with high-risk human papillomavirus (HPVs) types represents the major risk factor for the etiopathogenesis of the disease. HPV-16 is the most frequently identified HPV type in cervical lesions and expression of E6 and E7 oncoproteins is required for the uncontrolled cellular proliferation. In the present study we report the design and experimental testing of a recombinant multi-epitope protein containing immunogenic epitopes of HPV-16 E6 and E7. Tumor preventive assays, based on the engraftment of TC-1 cells in mice, showed that the E6E7 multi-epitope protein induced a full preventive anti-tumor protection in wild-type mice, as well as in mice deficient in expression of CD4⁺ T cells and TLR4 receptor. Nonetheless, no anti-tumor protection was observed in mice deficient in CD8⁺ T cells. Also, the vaccine promoted high activation of E6/E7-specific T cells and in a therapeutic-approach, E6E7 protein conferred full anti-tumor protection in mice. These results show a potential use of this E6E7 multi-epitope antigen as a new and promising antigen for the development of a therapeutic vaccine against tumors induced by HPV.</p></div