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1.
Carbohydr Polym ; 254: 117446, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33357916

RESUMO

Probiotics and curcumin can exhibit synergistic biological activities on the basis of a gut-brain axis, but are sensitive to environmental conditions, making it a challenge for their co-utilization. To meet the demand for high efficiency and convenience, both probiotics and curcumin were encapsulated within a propylene glycol alginate-based hydrogel delivery system, which was assembled using an ethanol-induced approach. The composite hydrogel was effective at sustaining the release of curcumin and protecting LGG cells in simulated gastrointestinal tract conditions. Moreover, it could also largely reduce the chemical degradation of curcumin and increase the survival of LGG during light exposure and long-term storage: up to 91.3 % of curcumin and 9.72 log CFU cm-3 remained present throughout 4 weeks of storage. Results in this work demonstrate a low-energy and green approach to assemble a composite hydrogel with remarkable biocompatibility, which is considered as a desired delivery vehicle for co-delivery of probiotics and curcumin.


Assuntos
Alginatos/química , Curcumina/metabolismo , Preparações de Ação Retardada , Lactobacillus rhamnosus/fisiologia , Lactoglobulinas/química , Probióticos/análise , Materiais Biomiméticos/química , Encapsulamento de Células/métodos , Curcumina/química , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Etanol/química , Suco Gástrico/química , Humanos , Hidrogéis , Concentração de Íons de Hidrogênio , Cinética , Lactobacillus rhamnosus/citologia , Soluções
2.
Carbohydr Polym ; 254: 117415, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33357899

RESUMO

Grapefruit peel nanofibrillated cellulose (GNFC) was used as fat substitute in ice cream. GNFC was characterized by TEM, SEM, and XRD. The effects of GNFC on textural profiles, rheological properties, melting resistance, sensory properties, microstructure, and gross energy (GE) of ice cream were investigated. The results showed that GNFC was short rod-shaped crystal. Ice cream added with GNFC exhibited elastic-dominated behavior and better textural properties. The sensory evaluation score reached the highest level with desirable three-dimensional network structure at 0.4 % GNFC addition. GE of ice cream significantly decreased with reducing fat with maximal reduction rate of 17.90 %. Furthermore, the results of in vitro simulated digestion showed that GNFC addition and fat reduction significantly inhibited fat digestibility of ice cream due to coalescence of fat droplets on GNFC. This study provides new sustainable perspectives for the application of GNFC prepared from agricultural waste as fat substitute in food products.


Assuntos
Celulose/química , Citrus paradisi/química , Substitutos da Gordura/química , Sorvetes , Nanofibras/química , Nanopartículas/química , Extratos Vegetais/química , Celulose/farmacologia , Óxidos N-Cíclicos/química , Digestão/efeitos dos fármacos , Elasticidade , Substitutos da Gordura/farmacologia , Ácidos Graxos não Esterificados/química , Manipulação de Alimentos/métodos , Congelamento , Suco Gástrico/química , Suco Gástrico/efeitos dos fármacos , Concentração de Íons de Hidrogênio , Leucina/química , Extratos Vegetais/farmacologia , Reologia/métodos , Paladar
3.
Carbohydr Polym ; 237: 116172, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-32241441

RESUMO

Albeit gelatin hard capsules were predominantly applied, their disadvantages call for endeavours on non-gelatin capsules in healthcare aspects. Herein, high molecular weight (Mw = 1 × 106) pullulan was purified from yeast fermentation broth. This high Mw pullulan and commercial low Mw pullulan were respectively co-blended with gellan to prepare the optimal solutions for capsule production. Further investigations, including loss-on-drying, brittleness and tightness, showed that the obtained pullulan-gellan capsules were of low water content, brittleness, leakage, and of high tightness. These capsules exhibited an extended release of amoxicillin over 60 min in simulated gastric fluid. Although the use of high and low Mw pullulan produced composite capsules with similar properties, the required concentration of high Mw pullulan was nearly half of that for low Mw pullulan, suggesting a cost-saving characteristic of using high Mw pullulan. This work proposes a potential substitution of gelatin with pullulan-gellan composites for preparing hard capsules.


Assuntos
Glucanos/química , Polissacarídeos Bacterianos/química , Amoxicilina/química , Antibacterianos/química , Cápsulas , Preparações de Ação Retardada/química , Liberação Controlada de Fármacos , Suco Gástrico/química , Peso Molecular , Reologia
4.
Food Chem ; 318: 126449, 2020 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-32146306

RESUMO

Mulberry and chokeberry are rich sources of anthocyanins. In this study, the effect of the anthocyanin composition on the anthocyanin profile changes during in vitro digestion (mimicking the physiological conditions) was investigated by UHPLC-(ESI)-qTOF and UHPLC-(ESI)-QqQ. The antioxidant activity before and after in vitro digestion was elucidated. Cyanidin-3-O-glucoside and cyanidin-3-O-galactoside were dominant in mulberry and chokeberry, respectively. Moreover, the loss of cyanidin-3-O-galactoside in the chokeberry extract after digestion was greater than that of cyanidin-3-O-glucoside in the mulberry extract. After digestion, phenolic acids including protocatechuic acid and various cyanidin conjugates were newly formed because of decomposition and changes in the cyanidin-glycosides. The phenolic acid and cyanidin conjugate levels varied depending on the cyanidin glycoside sources in the colonic fraction. Finally, antioxidant activity before and after digestion was higher in the chokeberry extract than in the mulberry extract. Moreover, this activity continuously decreased until intestinal digestion but increased in the colonic fraction.


Assuntos
Antocianinas/química , Morus/química , Photinia/química , Antocianinas/metabolismo , Antioxidantes/química , Cromatografia Líquida de Alta Pressão/métodos , Análise por Conglomerados , Digestão , Frutas/química , Frutas/metabolismo , Suco Gástrico/química , Suco Gástrico/metabolismo , Humanos , Espectrometria de Massas/métodos , Morus/metabolismo , Fenóis/análise , Photinia/metabolismo , Extratos Vegetais/química , Análise de Componente Principal
5.
Food Funct ; 11(2): 1790-1797, 2020 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-32053124

RESUMO

The effect of sulfated polysaccharides on the digestion of dietary DNA by pepsin was studied using in vitro simulated gastric juice. The results showed that fucoidan (FUC), dextran sulfate (DS) and chondroitin sulfate (CS) could inhibit the digestion of DNA in a dose-dependent manner. Polysaccharides with high sulfate group content have stronger inhibition ability. Fluorescence spectroscopy results showed that polysaccharides could bind to pepsin, and transmission electron microscopy (TEM) confirmed that polysaccharides can interact with DNA, which not only is the main reason that polysaccharides inhibit the digestion of DNA by pepsin but also causes the digestion of DNA by DNase II to be inhibited. The finding suggests that the digestion of DNA should be reevaluated when eating foods rich in sulfated polysaccharides. This study enriched the known pharmacological properties of sulfated polysaccharides as pepsin inhibitors and provided inspiration for the use of sulfated polysaccharides as oligonucleotide drug delivery carriers.


Assuntos
DNA , Modelos Biológicos , Pepsina A , Polissacarídeos , Sulfatos , Animais , Sulfatos de Condroitina , DNA/química , DNA/metabolismo , Sulfato de Dextrana , Digestão/efeitos dos fármacos , Endodesoxirribonucleases/antagonistas & inibidores , Endodesoxirribonucleases/química , Endodesoxirribonucleases/metabolismo , Suco Gástrico/química , Suco Gástrico/metabolismo , Pepsina A/antagonistas & inibidores , Pepsina A/química , Pepsina A/metabolismo , Polissacarídeos/química , Polissacarídeos/metabolismo , Polissacarídeos/farmacologia , Sulfatos/química , Sulfatos/metabolismo , Sulfatos/farmacologia
6.
Rev. esp. enferm. dig ; 112(1): 23-26, ene. 2020. tab, lus, graf
Artigo em Espanhol | IBECS | ID: ibc-196004

RESUMO

INTRODUCCIÓN: el objetivo fue evaluar la exactitud diagnóstica de Endofaster(R) para la detección de Helicobacter pylori. MÉTODOS: se realizó estudio histológico de biopsias gástricas (patrón oro) y aspirado del jugo gástrico para análisis por Endofaster(R) (negativo si la concentración de amonio fue < 57 ppm, positivo si > 67 ppm y débilmente positivo entre 57-67). RESULTADOS: ochenta y seis pacientes fueron incluidos y Endofaster(R) fue positivo en el 33,7%, débilmente positivo en el 11,6% y negativo en el 54,7%. Las biopsias fueron positivas en el 38,4%. Se alcanzó una precisión del 81,4% y Kappa = 0.57. CONCLUSIONES: Endofaster(R) permitiría un diagnóstico rápido de la infección con una buena precisión diagnóstica (AUROC = 0.81)


No disponible


Assuntos
Humanos , Masculino , Feminino , Adulto , Pessoa de Meia-Idade , Idoso , Infecções por Helicobacter/diagnóstico , Endoscopia do Sistema Digestório/métodos , Suco Gástrico/química , Compostos de Amônio/análise , Helicobacter pylori , Valor Preditivo dos Testes , Sensibilidade e Especificidade , Estudos Prospectivos
7.
Int J Pharm ; 575: 118875, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31765781

RESUMO

Drug administration failure has been often witnessed in pediatric due to children's resistance to take medicines with bitter taste. Taste-masking is the key requirement among the scanty drugs available for children. Solid taste-masking systems, such as tablets and capsules, are difficult to swallow for children. Therefore, a liquid taste-masking system based on lyotropic liquid crystalline nanoparticles (LLCNs) was developed in this study. Cefpodoxime proxetil (CFP), a typically bitter drug used as antibiotic in pediatric, was selected as the model drug, and the encapsulation of CFP into the LLCNs was envisaged to improve their taste. Pluronic F127 was added to improve the colloidal stability of CFP-LLCNs. The optimized CFP-LLCNs showed the particle size of 187.29 ± 4.12 nm and the encapsulation efficiency of 85.80%. The mesophase analysis by polarized light microscopy and small angle X-ray scattering confirmed the cubic phase of CFP-LLCNs. It showed a sustained-release profile well fitted to Higuchi model, indicating that diffusion and erosion were both responsible for the CFP release. The taste-masking ability of CFP-LLCNs was confirmed by electronic tongue, compared to CFP and commercial product. The colloidal stability was verified after 3 months storage in room condition (25 ± 2 °C, 70 ± 2%RH). To sum up, the taste-masking and colloidal-stable CFP-LLCNs showed great potential for pediatric oral delivery.


Assuntos
Antibacterianos/administração & dosagem , Ceftizoxima/análogos & derivados , Sistemas de Liberação de Medicamentos , Cristais Líquidos , Nanopartículas/administração & dosagem , Paladar , Administração Oral , Antibacterianos/química , Ceftizoxima/administração & dosagem , Ceftizoxima/química , Criança , Coloides , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Nariz Eletrônico , Suco Gástrico/química , Humanos , Secreções Intestinais/química , Nanopartículas/química
8.
Regul Toxicol Pharmacol ; 110: 104549, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31811877

RESUMO

This study investigated nickel and cobalt ion release from the metals and several alloys in synthetic gastric, as well as interstitial and lysosomal lung fluids. Results were used to calculate the relative bioaccessible concentrations (RBCs) of the metals. Nickel release from SS 316L powder in gastric fluid was >300-fold lower than from a simple mixture of powders of the same bulk composition. Gastric bioaccessibility data showed 50-fold higher metal releases per gram of sample from powder than massive forms. RBCs of nickel and cobalt in the alloy powders were lower, equal, or higher in all fluids tested than their bulk concentrations. This illustrates the fact that matrix effects can increase or decrease the metal ion release, depending on the metal ingredients, alloy type, and fluid, consistent with research by others. Acute inhalation toxicity studies with cobalt-containing alloy powders showed that the RBC of cobalt in interstitial lung fluid predicted acute toxicity better than bulk concentration. This example indicates that the RBC of a metal in an alloy may estimate the concentration of bioavailable metals better than the bulk concentration, and the approach may provide a means to refine the classification of alloys for several human health endpoints.


Assuntos
Ligas/química , Cobalto/química , Níquel/química , Administração por Inalação , Ligas/classificação , Ligas/farmacocinética , Ligas/toxicidade , Animais , Disponibilidade Biológica , Cobalto/farmacocinética , Cobalto/toxicidade , Eritrócitos/efeitos dos fármacos , Líquido Extracelular/química , Feminino , Suco Gástrico/química , Humanos , Dose Letal Mediana , Pulmão , Lisossomos/química , Masculino , Níquel/farmacocinética , Níquel/toxicidade , Ratos Sprague-Dawley , Medição de Risco/métodos
9.
Allergol Immunopathol (Madr) ; 48(1): 26-33, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31623945

RESUMO

INTRODUCTION AND OBJECTIVES: The production and consumption of oysters is increasing annually because it can provide essential nutrients and benefit for human health, leading to frequent occurrence of severe allergic reactions observed in sensitized individuals. The aim of the present study was to investigate the effects of acid and protease treatment on the conformation and IgE-binding capacity of recombinant Crassostrea gigas tropomyosin (Cra g 1). RESULTS: Under acidic conditions, Cra g 1 did not undergo degradation, however, the changes obvious in the intensity of CD signal and ANS-binding fluorescence were observed, which was associated with a decrease in antibody reactivity. In simulated gastrointestinal fluid (SGF) and simulated intestinal fluid (SIF) digestion system, acid-treated Cra g 1 was relatively resistant to digestion, but the degradative patterns were very different. Moreover, owing to alterations of secondary structure and hydrophobic surface of the protein during digestive processing, antigenicity of acid-induced Cra g 1 reduced in SGF while it increased significantly in SIF. CONCLUSION: To our knowledge, this is the first study reporting that antigenicity of acid-treated oyster tropomyosin increased after SIF digestion. These results revealed that treatment with acid and pepsin, rather than trypsin, was an effective way of reducing IgE-binding capacity of tropomyosin from oyster.


Assuntos
Ácidos/metabolismo , Alérgenos/imunologia , Imunoglobulina E/imunologia , Tropomiosina/imunologia , Ácidos/análise , Alérgenos/química , Alérgenos/metabolismo , Afinidade de Anticorpos , Suco Gástrico/química , Suco Gástrico/metabolismo , Humanos , Secreções Intestinais/química , Secreções Intestinais/metabolismo , Pepsina A/análise , Pepsina A/metabolismo , Conformação Proteica , Proteínas Recombinantes/química , Proteínas Recombinantes/imunologia , Proteínas Recombinantes/metabolismo , Tropomiosina/química , Tropomiosina/metabolismo , Tripsina/análise , Tripsina/metabolismo
10.
Curr Microbiol ; 77(3): 343-352, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31832842

RESUMO

The aim of this study was to evaluate probiotic properties of ten Streptococcus thermophilus strains (st1 to st10) isolated from pickles in China. These strains all had ß-galactosidase activity, which laid foundation for studying their probiotic properties. In this study, the bile salt hydrolase activity, lysozyme resistance, tolerance to simulated gastric juice, bile salt tolerance, and bacterial adhesion capacity to the Caco-2 cells of these selected strains were detected in vitro conditions. The results indicated that the bile salt hydrolase activities of st2, st6, and st9 were higher than that for other strains. St10 showed the greatest lysozyme resistance (> 80% survival), followed by st9, st8, st7, st5, and st6. As for the tolerance to simulated gastric juice, st5 possessed the highest survival rate (35%), followed by st6 (30%). St6 was the best performer in both bile salt tolerance and bacterial adhesion capacity to the Caco-2 cells. The results of fluorescence microscope and electron microscope further confirmed previous studies and more intuitively demonstrated the st6 strain's tolerance to harsh environments. Overall, these strains were expected to possess beneficial properties and have the potentiality to be probiotics.


Assuntos
Aderência Bacteriana , Microbiologia de Alimentos , Probióticos/isolamento & purificação , Streptococcus thermophilus/classificação , Ácidos e Sais Biliares/química , Células CACO-2 , Suco Gástrico/química , Humanos , Streptococcus thermophilus/enzimologia , Streptococcus thermophilus/isolamento & purificação , beta-Galactosidase/metabolismo
11.
Vet Microbiol ; 239: 108462, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31767100

RESUMO

In contrast to human influenza viruses that replicate in the respiratory tract and are airborne transmitted, avian viruses also replicate in gut epithelial cells and are transmitted via the fecal-oral route. On this route, the virus is exposed to destructive fluids of the digestive tract, which are acidic and contain the proteases pepsin (gizzard) or chymotrypsin and trypsin (intestine). Only the latter enzyme activates virus by cleaving hemagglutinin (HA) into HA1 and HA2 subunits. We mimicked the passage of viruses through the gastrointestinal tract by treating them with digestive fluids from chicken and determined titers and integrity of HA by western-blot. Gizzard fluid completely inactivated virions and degrades HA even at a high dilution, but only if the pH was kept acidic. If the fluid is diluted with neutral buffer (mimicking virus uptake with seawater) particles were more resistant. Virions containing an uncleaved HA were even activated suggesting that gastric juice contains a trypsin-like protease. Undiluted intestinal fluid inactivated particles and destroyed HA, but diluted fluid activated virions. A virus isolated from the duck´s intestine is more tolerant against intestinal fluid compared to fowl plague virus suggesting that the former is better adapted to grow in the intestine. We also demonstrate that influenza viruses replicate to high titers in a novel chicken epithelial gut cell line. While viruses with a monobasic HA cleavage site require addition of trypsin, these cells effectively process HA with a polybasic cleavage site, which could be blocked with an inhibitor of the cellular furin protease.


Assuntos
Trato Gastrointestinal/virologia , Hemaglutininas/metabolismo , Influenza Aviária/virologia , Animais , Galinhas , Células Epiteliais/citologia , Células Epiteliais/virologia , Suco Gástrico/química , Suco Gástrico/enzimologia , Concentração de Íons de Hidrogênio , Técnicas In Vitro , Secreções Intestinais/química , Secreções Intestinais/enzimologia , Inativação de Vírus , Replicação Viral/fisiologia
12.
Int J Pharm ; 572: 118801, 2019 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-31678529

RESUMO

This study was aimed to monitor the transit through the intestine by X-ray imaging using barium sulfate (BS) as tracer. The in vitro features of monolithic tablets were correlated with their in vivo behavior in order to provide a tool for the development of targeted formulations containing macromolecular bioactive agents. The impact of BS on various matrices (neutral, ionic) was studied in simulated fluids using the disintegration time (DT) as main parameter. Dry tablets were characterized by spectroscopic methods (X-ray diffraction and Infra-Red) and scanning electron microscopy (SEM). The selected formulations were followed in a beagle dog model. The in vivo and in vitro DT of tablets formulated with BS were compared. Results: anionic excipients carboxymethylcellulose (CMC) and carboxymethylstarch (CMS) protected the active ingredient from the gastric acidity, ensuring its targeted delivery in the intestine. The SEM analysis, before and after transit in simulated fluids, showed that BS remained in the tablets allowing their good follow-up in vivo. The incorporation of 30% protein in tablets with 40% BS had no impact on their behavior. In conclusion, BS and X-ray imagery could be a good alternative to scintigraphy for development of targeted formulations containing high molecular weight bioactive agents.


Assuntos
Sulfato de Bário/administração & dosagem , Carboximetilcelulose Sódica/química , Meios de Contraste/administração & dosagem , Excipientes/química , Intestinos/diagnóstico por imagem , Soroalbumina Bovina/administração & dosagem , Amido/análogos & derivados , Animais , Sulfato de Bário/química , Meios de Contraste/química , Cães , Composição de Medicamentos , Liberação Controlada de Fármacos , Suco Gástrico/química , Trânsito Gastrointestinal , Concentração de Íons de Hidrogênio , Secreções Intestinais/química , Soroalbumina Bovina/química , Amido/química , Comprimidos , Fatores de Tempo
13.
Molecules ; 24(20)2019 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-31627423

RESUMO

Myricetin (Myr) is a phytochemical with many functional properties. However, its hydrophobicity, low bioavailability, and stability limit its application. In this study, octadecanoate oat ß-glucan (OGE) was synthesized and gained recognition as a self-assembled micelle forming a polymer with a critical micelle concentration (CMC) of 59.4 µg/mL. The Myr-loaded OGE micelle was then prepared and characterized by dynamic light scattering (DLS), transmission electron microscope (TEM), X-ray diffractometer (XRD), and Fourier-transform infrared spectroscopy (FT-IR) spectra. The water solubility of Myr was greatly enhanced by forming the Myr/OGE inclusion complex. Consequently, compared to free Myr, the retention of Myr in Myr-loaded OGE micelle was effectively increased during the intestinal digestion phase, and its antioxidant activity was also improved. Overall, our findings demonstrated the potential applications of OGE polymer for the development of prospective micelle in health food, cosmetics, and pharmaceutical fields because they can aid in the delivery of hydrophobic functional compounds like Myr.


Assuntos
Antioxidantes/química , Portadores de Fármacos , Flavonoides/química , beta-Glucanas/química , Materiais Biomiméticos/química , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Composição de Medicamentos/métodos , Suco Gástrico/química , Humanos , Interações Hidrofóbicas e Hidrofílicas , Radical Hidroxila/antagonistas & inibidores , Radical Hidroxila/química , Micelas , Estrutura Molecular , Picratos/antagonistas & inibidores , Picratos/química , Solubilidade , Água/química
14.
Klin Lab Diagn ; 64(8): 484-489, 2019.
Artigo em Russo | MEDLINE | ID: mdl-31479604

RESUMO

The aim of research was to evaluate the effectiveness of the effect of eradication therapy on the cytokine status of gastric juice in patients with chronic non-atrophic gastritis (CNG) and duodenal ulcer (DU) associated with Helicobacter pylori. Clinical observations and laboratory-instrumental studies performed in 95 patients aged 20 to 55 years with CNG and duodenal ulcer with determination of cytokine content of IL-1ß, IL-6 and TNF-α in the fasting portion of gastric juice. The most pronounced decrease in the content of proinflammatory cytokines in gastric juice on the background of treatment was found in patients of the 1st group who received combined therapy according to the scheme omeprazole + clarithromycin + amoxicillin. Analysis of the content of proinflammatory cytokines (IL-1ß, IL-6 and TNF-α) in gastric juice in patients with acute exacerbation showed that their concentration in all 8 patients after the course of therapy exceeded the norm (P < 0.05) and was IL -1ß - 30,30 + 1,15 pg/l, IL-6 - 10,4 + 0,83 pg / l and TNF-α - 32,5 + 1,13 pg / l. At the same time, the level of proinflammatory cytokines in gastric juice correlated with the degree of dissemination of H. pylori in the mucosa of the gastroduodenal zone. Helicobacter pylori infection in inflammation and ulceration in the mucous membrane of the stomach and duodenum, possibly in addition to other mechanisms, affects the activation of pro-inflammatory cytokines (IL-1beta, IL-6, TNF-alpha) in gastric juice. Incomplete eradication of H. Pylori after treatment during clinical endoscopic remission in patients with duodenal ulcer in the vast majority of cases is accompanied by the preservation of an increased level of pro-inflammatory cytokines in gastric juice, which may be one of the reasons for the relapse of the disease.


Assuntos
Citocinas/análise , Suco Gástrico/química , Gastrite/terapia , Infecções por Helicobacter/terapia , Adulto , Mucosa Gástrica , Gastrite/microbiologia , Helicobacter pylori , Humanos , Pessoa de Meia-Idade , Adulto Jovem
15.
J Control Release ; 311-312: 74-84, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31487499

RESUMO

This research aimed to develop a pH-responsive organic-inorganic hybrid nanocomposite as an effective oral delivery system for protein drugs. Three different nanocomposites were prepared by using bovine serum albumin (BSA) as a model protein. A nanocomplex of BSA with 3-aminopropyl functionalized magnesium phyllosilicate (AC-BSA) was obtained via the spontaneous co-assembly and then sequentially coated with glycol-chitosan (GAC-BSA) and the pH sensitive polymer, Eudragit®L100-55 (EGAC-BSA). These organic-inorganic hybrid nanocomposites exhibited high entrapment efficiency (86-99%) and their structural characteristics were confirmed by using energy dispersive X-ray spectroscopy, Fourier transform infrared spectroscopy, and circular dichroism analysis, indicating that the secondary structure of BSA was well retained in the nanocomposites. At pH 1.2, AC-BSA achieved rapid drug release of about 80% within 2 h, while GAC-BSA and EGAC-BSA exhibited slow drug release of 30% and 15%, respectively, indicating that the surface-coated nanocomposites were more stable in the gastric condition. Furthermore, the conformational stability of BSA entrapped in EGAC-BSA was well retained in the presence of proteolytic enzymes, suggesting that EGAC-BSA should be effective in protecting the protein against gastrointestinal harsh environment. Compared to free BSA, all of tested nanocomposites demonstrated 2.1-3.8-fold higher cellular uptake in Caco-2 cells. Furthermore, energy-dependent endocytosis and paracellular pathway contributed to the cellular transport of nanoparticles. After oral administration in rats, EGAC-BSA significantly enhanced the intestinal permeation of BSA compared to free BSA. In conclusion, EGAC-BSA appears to be promising as an effective oral delivery system for proteins with enhanced intestinal absorption.


Assuntos
Quitosana/administração & dosagem , Sistemas de Liberação de Medicamentos , Nanocompostos/administração & dosagem , Ácidos Polimetacrílicos/administração & dosagem , Soroalbumina Bovina/administração & dosagem , Administração Oral , Animais , Células CACO-2 , Quitosana/química , Liberação Controlada de Fármacos , Suco Gástrico/química , Humanos , Concentração de Íons de Hidrogênio , Absorção Intestinal , Secreções Intestinais/química , Masculino , Nanocompostos/química , Ácidos Polimetacrílicos/química , Ratos Sprague-Dawley , Soroalbumina Bovina/química , Silicatos/administração & dosagem , Silicatos/química
16.
Food Chem Toxicol ; 133: 110778, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31472224

RESUMO

This study was to investigate the structure of a polysaccharide fraction from the Fortunella margarita and the relationship between its digestibility and structure. A novel polysaccharide fraction extracted by graded precipitation at ethanol concentrations of 20% from F. margarita (named FP20) comprised mainly glucose, galactose, and mannose. The unit composition was →4)-ß-Glcp-(1 → 2)-α-Glcp-(1 → 2)-α-Galp-(1 → 4)-α-Galp-(1→ bone, and in →2)-α-Galp-(1→) with a branching point at C6 of ß-Manp. FP20 was identified as a mannogalactoglucan with a different monosaccharide composition ratio and side-chain sugar residues compared with other plant polysaccharides. Moreover, FP20 had a spherical aggregations by atomic force microscope test. FP20 had an island-shaped structures with a smooth surface revealed by field emission scanning electron microscopy. Furthermore, in vitro digestive test, FP20 was resistance to a digestion system of saliva-gastric-small intestinal. The digestibility of FP20 was related to its backbone unit, structure and tight, uniform, and spherical chain conformation in aqueous.


Assuntos
Digestão , Galactanos/química , Glucanos/química , Rutaceae/química , Sequência de Carboidratos , Suco Gástrico/química , Hidrólise , Secreções Intestinais/química , Manose/química , Peso Molecular , Saliva/química
17.
Curr Drug Deliv ; 16(8): 759-767, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31475897

RESUMO

BACKGROUND: Coenzyme Q10 is a fundamental endogenous factor involved in cell energy production that shows protective properties in oxidative stress, mainly in skeletal and heart muscle. Coenzyme Q10 supplementation appears to benefit athletes in strenuous training and in the elderly, demonstrating ant-inflammatory properties by reducing inflammatory cytokines. Improved absorption of coenzyme Q10 via a new delivery system would represent an important step forward in the use of coenzyme Q10 as a dietary supplement. OBJECTIVE: The aim of the study was to evaluate the solubility and oral absorption in human healthy volunteers of a new food grade coenzyme Q10 phytosome formulation. METHODS: Solubility studies were performed in vitro in simulated gastrointestinal fluids; human studies were conducted in healthy volunteers to evaluate oral absorption in a Single dose study, in comparison with the coenzyme Q10 capsules, and in a repeated study at two increasing doses. RESULTS: The highest solubility shown by coenzyme Q10 phytosome in simulated intestinal fluids results in an improvement in oral absorption of coenzyme Q10 in healthy volunteers, three times more than the coenzyme Q10 according to AUC (area under the time/concentration curve) values. When two increasing doses (one and two capsules) were administered to healthy volunteers within a two-week schedule, the plasmatic levels of coenzyme Q10 resulted in 0.864±0.200 µg/ml (Mean±S.D.+41%) and 1.321±0.400 µg/ml (+116%), respectively versus baseline (0.614±0.120 µg/ml one capsule, 0.614±0.160 µg/ml two capsules). This detected dose-related bioavailability of coenzyme Q10 phytosome was even observed with no alterations in vital signs, neither in the physical examination nor in ECG, and no changes of clinical and biochemical parameters were observed. CONCLUSION: These findings, taken together, support the safety profile and significantly improved coenzyme Q10 oral absorption in humans with this new phytosome delivery formulation.


Assuntos
Ubiquinona/análogos & derivados , Adolescente , Adulto , Disponibilidade Biológica , Suplementos Nutricionais , Relação Dose-Resposta a Droga , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Feminino , Suco Gástrico/química , Voluntários Saudáveis , Humanos , Masculino , Pessoa de Meia-Idade , Solubilidade , Ubiquinona/administração & dosagem , Ubiquinona/química , Ubiquinona/farmacocinética , Adulto Jovem
18.
Biomed Res Int ; 2019: 6424651, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31531361

RESUMO

DPPH• scavenging peptides (<3kDa) from underutilized Dunaliella salina protein were obtained by the following successive treatment, i.e., ultrasound extraction, simulated in vitro gastrointestinal digestion hydrolyzation, and membrane ultrafiltration classification. The optimal condition for ultrasound-assisted extraction was an ultrasound wave with 800 W of power treating a mixture of 60 mL of 1.0 mol L-1 NaOH and 2 g algae powder for 15 min. A high correlation (r=0.8146) between DPPH• scavenging activity and yield of the intact peptides showed their antioxidant capacity. Simulated in vitro digestion assay resulted in excellent DPPH• scavenging activity of the total peptide, amounting to (86.5 ± 10.1)%, comparing with the nondigestion samples at (46.8 ± 6.5)%. After fractionation, the 500-1000 Da fraction exhibited the highest DPPH• scavenging activity (81.2 ± 4.0)%, increasing 1.5 times due to digestion. Then, the 500-1000 Da fraction was analyzed by RPLC-Q Exactive HF mass spectrometer, and 4 novel peptides, i.e., Ile-Leu-Thr-Lys-Ala-Ala-Ile-Glu-Gly-Lys, Ile-Ile-Tyr-Phe-Gln-Gly-Lys, Asn-Asp-Pro-Ser-Thr-Val-Lys, and Thr-Val-Arg-Pro-Pro-Gln-Arg, were identified. From these amino acid sequences, hydrophobic residues accounted for 56%, which indicated their high antioxidant property. The results indicated that underutilized protein of Dunaliella salina could be a potential source of antioxidative peptides through simulated in vitro gastrointestinal digestion.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Clorofíceas/química , Suco Gástrico/química , Peptídeos/química , Peptídeos/farmacologia , Proteínas/química , Compostos de Bifenilo/química , Microalgas/química , Picratos/química
19.
Int J Pharm ; 569: 118602, 2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31394182

RESUMO

An innovative abuse-deterrent composition was developed to deter the most dangerous route of drug abuse, the intravenous route. The composition is based on a crosslinked sodium starch glycolate (X-SSG) that can effectively complex with cationic drugs in aqueous solutions and minimize the amount of the free drug available for extraction. Furthermore, the crosslinked polymer swells in and entraps a portion of the drug solution by which it reduces the available volume for syringing and subsequent injection. Two deterrent compositions were prepared, a drug-polymer physical blend and a drug-polymer chemical complex. The composition in its complexed form showed greater deterrence capacity than the physical blend except in solvents with ionic moieties, where the deterrence remained almost the same. The studies revealed that the complexation with the drug played a major role in total drug entrapment. Tablets prepared from the drug-polymer complex showed a complete and immediate drug release in 0.1 N HCl within the first 15 min. Moreover, the dissolution studies in the simulated intestinal media ruled out the re-complexation potential between the drug and the polymer. The proposed X-SSG composition provides a desirable drug release in the gastric and intestinal media under the legitimate use while deterring an intravenous abuse.


Assuntos
Formulações de Dissuasão de Abuso , Amido/análogos & derivados , Liberação Controlada de Fármacos , Suco Gástrico/química , Secreções Intestinais/química , Amido/química , Comprimidos
20.
Colloids Surf B Biointerfaces ; 183: 110414, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31404790

RESUMO

Pickering emulsions have received widespread attention for encapsulating lipophilic guests in the biomedical and food fields. However, control of the stabilities and demulsification of Pickering emulsions to allow the release of encapsulated species remains a challenge in gastrointestinal conditions. In this work, phosphatidylcholine-kaolinite was prepared by modification of natural kaolinite with phosphatidylcholine and was used as an emulsifier to stabilize medium-chain triglyceride (MCT)/water Pickering emulsions for encapsulating curcumin, a natural antioxidant drug. Simulated gastric and intestinal digestion and a cell uptake assay were implemented for the curcumin-loaded MCT/water Pickering emulsion to study its demulsification and the bioavailability of curcumin. The results revealed that the wettability of phosphatidylcholine-kaolinite could be tailored by controlling the modification temperature so that it could control the emulsion stability. The prepared phosphatidylcholine-kaolinite, with a three-phase contact angle of 123°, was an optimal emulsifier for the enhanced stabilization of the MCT/water Pickering emulsion, especially in the presence of gastric acid. The phosphatidylcholine-kaolinite distributed at the water-oil interface and formed a dense shell structure on the surfaces of the emulsion droplets, controlling the demulsification efficiency to release the encapsulated curcumin. Only 18.9% of the curcumin was released in the simulated gastric conditions after 120 min of digestion due to the demulsification of the MCT/water Pickering emulsion, while it was completely released after 150 min of digestion in simulated intestinal conditions, as expected. This Pickering emulsion stabilized by phosphatidylcholine-kaolinite is a promising delivery system for lipophilic foods or drugs to enhance their bioavailability.


Assuntos
Antioxidantes/metabolismo , Curcumina/metabolismo , Preparações de Ação Retardada , Composição de Medicamentos/métodos , Caulim/química , Fosfatidilcolinas/química , Antioxidantes/química , Antioxidantes/farmacologia , Materiais Biomiméticos/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Curcumina/química , Curcumina/farmacologia , Liberação Controlada de Fármacos , Emulsificantes/química , Emulsões , Células Epiteliais/citologia , Células Epiteliais/efeitos dos fármacos , Suco Gástrico/química , Humanos , Cinética , Temperatura , Triglicerídeos/química , Água/química
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