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1.
Carbohydr Polym ; 227: 115337, 2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31590880

RESUMO

A gel delivery system was developed in the present work using whey protein isolate and lotus root amylopectin via regulating pH. The texture, thermodynamics, rheology and microstructure of gels were evaluated. Results showed that pH at 7.0 induced a more compact and stable gel structure than other pH. The composite gel formed at pH 7.0 was accordingly employed to encapsulate vitamin D3. Results exhibited that the encapsulation of composite gel of whey protein isolate and lotus root amylopectin could enhance the storage stability of vitamin D3 and protect vitamin D3 from photochemical degradation. Moreover, this encapsulation could control the release of vitamin D3 in simulated intestinal fluid. Animal experiments exhibited that the bioavailability was significantly increased after vitamin D3 was encapsulated by the composite gel. This work indicated that the whey protein isolate-lotus root amylopectin gel is a good delivery system to improve the stability and bioavailability of vitamin D3.


Assuntos
Amilopectina/administração & dosagem , Colecalciferol/administração & dosagem , Sistemas de Liberação de Medicamentos , Vitaminas/administração & dosagem , Proteínas do Soro do Leite/administração & dosagem , Amilopectina/química , Amilopectina/farmacocinética , Animais , Disponibilidade Biológica , Colecalciferol/química , Colecalciferol/farmacocinética , Estabilidade de Medicamentos , Géis , Absorção Intestinal/efeitos dos fármacos , Lotus , Masculino , Camundongos Endogâmicos C57BL , Raízes de Plantas , Vitaminas/química , Vitaminas/farmacocinética , Proteínas do Soro do Leite/química , Proteínas do Soro do Leite/farmacocinética
2.
Food Chem ; 303: 125416, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31472385

RESUMO

Calcium and vitamin D3 were co-encapsulated in three types of water-in-oil-in-water (W/O/W) double emulsions stabilized with biopolymers: gum arabic, sodium alginate (Alg) and chitosan (Ch). Three calcium salts with different solubility were used: calcium carbonate (CaC), tricalcium phosphate (CaP) and calcium gluconate (CaG). In order to study the bioavailability of calcium and vitamin D3, the W/O/W double emulsions were subjected to digestion in simulated conditions using in vitro gastrointestinal models. The size of the oil droplets of all double emulsions increased in oral phase and decreased in gastric and intestinal phases. In the intestinal phase, the average diameter of oil globules in the W/O/W(Alg) and W/O/W(Ch) was d23 = 6.56 ±â€¯0.09 and d23 = 5.33 ±â€¯0.01 and the electro-kinetic potential was: ζ ≈ -25 mV and ζ ≈ -17 mV, respectively. Presence of calcium ions in the intestinal fluid decreased the free fatty acids content and decreased the bioaccessibility of vitamin D3 due to the inhibition of micellization process.


Assuntos
Cálcio/química , Colecalciferol/química , Disponibilidade Biológica , Cálcio/metabolismo , Colecalciferol/metabolismo , Digestão , Composição de Medicamentos , Emulsões/química , Trato Gastrointestinal/metabolismo , Humanos , Cinética , Modelos Biológicos , Solubilidade , Água/química
3.
J Food Sci ; 84(11): 3213-3221, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31589344

RESUMO

Vitamin D3 was encapsulated in 10% wt soybean oil-in-water (O/W) Pickering emulsions stabilized by either nanofibrillated cellulose (NFC) or whey protein isolate (WPI) at 0.3%, 0.5%, and 0.7% w/w. The vitamin D3 -enriched emulsions were tested for their stability against temperature (30 °C to 90 °C), pH (2 to 8), and ionic strength (0 to 500 mM NaCl). The mean particle diameter (d32 ), ζ-potential, and creaming stability of the oil droplets in the emulsions were measured, as well as their vitamin D3 encapsulation efficiency (EE). After preparation, the oil droplet size (d32 ) of the emulsions stabilized by NFC increased with increasing emulsifier concentration, whereas the droplet size of emulsions stabilized by WPI decreased. NFC provided good stability to the emulsions through a combination of steric and electrostatic repulsion. The EE of vitamin D3 increased with increasing emulsifier concentration. Heating or ionic strength did not significantly (P < 0.05) affect the emulsions properties and EE. On the other hand, the NFC-stabilized emulsions were sensitive to highly acidic conditions (pH 2), with an increase in particle size and decrease in EE. The WPI-stabilized emulsions aggregated around the isoelectric point of the adsorbed proteins (pI ≈ 4.8). Increasing NFC or WPI concentration improved the stability and EE of the emulsions against environmental stresses. NFC-stabilized emulsions had good long-term stability. The results show that NFC can be used as an effective emulsifier for creating vitamin-enriched emulsions with good stability. PRACTICAL APPLICATION: This study can be used to develop more effective encapsulation technologies for fat-soluble vitamins in emulsion-based food products. Encapsulation using nanofibrillated cellulose effectively protected the encapsulated vitamins against environmental stresses which occur in industrial food production (such as pH changes, salt addition, and thermal processing). Moreover, nanofibrillated cellulose extracted from mangosteen rind is a nature-derived emulsifier that is environmental friendly.


Assuntos
Celulose/química , Colecalciferol/química , Composição de Medicamentos/métodos , Emulsões/química , Garcinia mangostana/química , Composição de Medicamentos/instrumentação , Estabilidade de Medicamentos , Emulsificantes/química , Concentração Osmolar , Tamanho da Partícula , Cloreto de Sódio/química , Eletricidade Estática , Temperatura Ambiente , Água/química
4.
J Food Sci ; 84(9): 2475-2481, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31441511

RESUMO

Nowadays, fortified vegetable oils with vitamin D3 are widely available in different countries and are consumed daily. The reduction rate of added vitamin D3 in fortified canola oil during heating process, the changes in oxidative status, and the thermal kinetic degradation of vitamin D3 in the fortified oil were investigated. For this purpose, canola oil was fortified at two levels of vitamin D3 with 5.625 µg/mL (low concentration or LC) and 13.585 µg/mL (a high concentration or HC). Samples were heated isothermally at 100, 150, and 180 °C for 30 min. The vitamin D3 concentration was determined by the high-performance liquid chromatographic method. The retention of vitamin D3 in samples treated at 100 °C for 30 min showed no significant reduction. Samples treated at 150 and 180 °C depending on the initial concentration showed the retention of 67.5% to 72.97% and 33.16% to 40.35% of vitamin D3 , respectively. An inverse relationship was found between the increment of lipid oxidation products (peroxide and anisidine values) and the retention of vitamin D3 . Kinetic parameters such as rate constant, activation energy, decimal reduction time, and quotient indicator were also calculated. An Arrhenius relationship was used for the assessment of temperature dependence of vitamin D3 degradation. Activation energies for vitamin D3 in LC and HC between 100 and 180 °C were found to be 44.01 and 38.77 kJ/mol, respectively. PRACTICAL APPLICATION: The oil can be fortified with vitamin D3 at low cost and offers a good bioavailability. A high-temperature cooking method may not be appropriate for the fortified products containing high lipid content.


Assuntos
Colecalciferol/química , Óleo de Brassica napus/química , Culinária , Alimentos Fortificados/análise , Temperatura Alta , Cinética , Lipídeos/química , Oxirredução
5.
J Steroid Biochem Mol Biol ; 193: 105429, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31325498

RESUMO

A phase inversion based cold water dilution method was developed to encapsulate Vitamin D3 (Vit D) in nano-structured lipid carrier (NLC) by blending caprylic-/capric triglyceride, Leciva S70 and Kolliphor HS®15, Vit D and sodium chloride. To optimize the process; a total of forty one formulations prepared by varying in their composition were tested for presence of NLC. Out of forty one formulations, only thirteen formulations resulted in NLC formation which were further evaluated for their physico-chemical attributes (particle size, zeta potential, transmittance, encapsulation efficiency and Vit D release). During principal component analysis using XLstats it was found that NLC-19, fabricated with 20% (v/v) Kolliphor, 20% (v/v) CCTG and 60% (v/v) water, 2.5% (w/v) Leciva, 2% (w/v) Vit D and 5% (w/v) sodium chloride was the most suitable for purpose of encapsulating Vitamin D. Hence, NLC-19 formulation was further taken up for stability studies under the following environmental stress conditions: (a) Temperature and humidity: accelerated condition: 45 ±â€¯2 °C and RH 75 ±â€¯5%, ambient condition: 25 ±â€¯3 °C and RH 65 ±â€¯5% and refrigerated condition: 6 ±â€¯2 °C and RH 55 ±â€¯5%, (b) pH: 3, 4, 5, 6, and 7, and (c) Ionic strength (NaCl concentration): 0 mM, 250 mM, 500 mM and 750 mM. The sensory evaluation of 'Lassi' (fortified with NLC-19) and its acceptability further confirmed the suitability of NLC-19 for the purpose of fortification of Vitamin D3 in 'Lassi' (A milk based beverage).


Assuntos
Colecalciferol/química , Portadores de Fármacos/química , Alimentos Fortificados , Lipídeos/química , Nanopartículas/química , Vitamina D/química , Bebidas , Estabilidade de Medicamentos
6.
Clin Lab ; 65(5)2019 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-31115209

RESUMO

BACKGROUND: Pre-clinical toxicology studies of human Gc-protein (vitamin D binding protein) are of special interest as to the transport of vitamin D and its biological activities. We have demonstrated that the oral application of a special dimeric vitamin D complex reduces oxidative stress and increases the quality of life in autistic children. Therefore, safety and toxic effects of two dimeric cholecalciferol-N-acetyl-galactosamine-albumin complexes were evaluated in increasing intravenous (iv.) vitamin D levels administered in a pre-clinical trial in mice over a 5-week period. METHODS: Over a period of 5 weeks, two times a week, mice received iv. administration of one of the following: (a) 1.2 IE of vitamin D-N-acetyl-galactosamine-albumin (Vitamin D3 NAGA, ImmunoD® group), (b) 1.2 IE of vitamin-D-poly-N-acetyl-galactosamine-albumin (Poly-Nac group), or (c) isotonic saline solution (sham group). Before and after the trial, red and white blood cell panels (RBS, WBC and platelets) were determined. Furthermore, vitamin D levels, electrolytes, and C-reactive protein levels were measured directly before sacrificing. RESULTS: No toxic effects were observed during iv. injection with dimeric vitamin D complexes, neither in the sham group, nor in the two treatment groups. Vitamin D levels increased significantly within 5 weeks in the Poly-Nac group (26.6 ± 8.8 ng/mL; p = 0.001) compared to the sham group (3.1 ± 0.9 ng/mL), and the Poly-Nac group to the ImmunoD group (7.0 ± 3.6 ng/mL; p = 0.003). A significant increase of vitamin D was also obtained in favor of the ImmunoD group compared to the sham (p = 0.03). Electrolytes (K, Na, Cl, Mg, Ca) and C-reactive protein showed no significant differences after administration in all three mice groups. Also, no significant differences were observed between these three groups in the WBC and RBC blood panels. CONCLUSIONS: The two dimeric vitamin D complexes used in this pre-clinical study showed no side or toxic effects after iv. administration in mice, but a sole increase in vitamin D levels without any change in electrolytes or blood cells. Therefore, we assume this newly developed composition to be safe in oral or iv.-administration and further pre-clinical studies can be conducted to evaluate the value in treatment of various diseases related to vitamin D deficiencies.


Assuntos
Albuminas/administração & dosagem , Colecalciferol/administração & dosagem , Colecalciferol/sangue , Galactosamina/administração & dosagem , Deficiência de Vitamina D/sangue , Albuminas/química , Animais , Colecalciferol/química , Dimerização , Esquema de Medicação , Contagem de Eritrócitos , Galactosamina/química , Injeções Intravenosas , Contagem de Leucócitos , Camundongos , Resultado do Tratamento , Deficiência de Vitamina D/tratamento farmacológico
7.
Molecules ; 24(7)2019 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-30979093

RESUMO

The increased interest in functional materials of natural origin has resulted in a higher market demand for preservative-free, "clean label", or natural ingredients-based products. The gummy bear food supplements are more acceptable to consumers and have fewer limitations compared to other dosage forms. The aim of our study was to produce natural ingredients-based gummy bear composition, and evaluate the influence of the selected ingredients on the product's textural properties, its acceptance in vivo, and the gummy bear's quality. The optimal base composition was determined using a surface response design: gelatin 4.3 g and agave syrup 6.3 g. The investigated sweeteners did not affect the textural properties (p > 0.05). However, further studies demonstrated that a 100% increase of agave results in up to 27% higher flexibility (p < 0.05). The addition of calcium and cholecalciferol reduced firmness by 59.59 ± 1.45% (p < 0.05). On the other hand, acai berry extract had no significant effect. The presence of calcium resulted in a decreased smell and taste; however, the data indicated that experimental texture analysis is a more accurate technique than in vivo evaluation. The acai berry extract did not improve all of the tested sensory properties. We can conclude that the suggested gummy bear base can be supplemented with various active ingredients and commercialized, though further studies are needed to investigate the other natural sources to mask the unpleasant taste of active ingredients and avoid water loss.


Assuntos
Agave/química , Produtos Biológicos/química , Suplementos Nutricionais/análise , Extratos Vegetais/química , Produtos Biológicos/análise , Cálcio/química , Colecalciferol/química , Euterpe/química , Gelatina/química , Humanos , Extratos Vegetais/análise , Olfato , Edulcorantes/química
8.
J Steroid Biochem Mol Biol ; 190: 88-98, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-30923018

RESUMO

A phase inversion based nanoemulsion fabrication process was developed to encapsulate vitamin D3 by blending caprylic-/capric triglyceride (CCTG), Leciva S70, Kolliphor® HS 15, vitamin D3 and aqueous phase (sodium chloride solution). In order to find out nanoparticle formation zone (NFZ), a ternary diagram was plotted with 41 possible combinations of three components CCTG, Kolliphor® HS 15 and aqueous phase. Out of forty one, only twelve combinations resulted in formation of stable nanoemulsion where the composition varied between 10%-40% (v/v), 10%-25% (v/v) and 35%-80% (v/v) for Kolliphor, CCTG and water respectively. Further, these 12 nanoemulsions were investigated for their particle size, zeta potential, emulsion stability, encapsulation efficiency and release kinetics (simulated digestion) of vitamin D. The nanoemulsion (NE-20) fabricated with 30% (v/v) Kolliphor, 20% (v/v) CCTG and 50% (v/v) aqueous phase was found to be the most suitable with respected to zeta potential, emulsion stability and encapsulation efficiency and also demonstrated high bioavailability of vitamin D as compared to other combinations and hence was selected for further physiochemical studies. The selected nanoemulsion was also investigated for particle size and zeta potential and stability of vitamin D3 retention under different environmental stress conditions (i) temperature and humidity: (a) accelerated condition: 45 ± 2 °C and RH 75 ± 5%, (b) ambient condition: 25 ± 3 °C and RH 65 ± 5% and (c) refrigerated condition: 6 ± 2 °C and RH 55 ± 5% (ii) pH (3-7) under refrigerated condition and (iii) ionic strength: NaCl concentration (0 mM, 250 mM, 500 mM and 750 mM) under crefrigerated condition. Fourier transform infrared spectroscopy and High Perfomance Liquid Chromatograpy technique were used to study physico-chemical stability of encapsulated vitamin D3 in the developed nanoemulsion. The sensory evaluation also indicated the acceptability of the selected nanoemulsion the purpose of fortification for beverages.


Assuntos
Colecalciferol/administração & dosagem , Emulsões/química , Aditivos Alimentares/administração & dosagem , Nanopartículas/química , Caprilatos/química , Colecalciferol/química , Composição de Medicamentos , Aditivos Alimentares/química , Tamanho da Partícula , Transição de Fase , Polietilenoglicóis/química , Estearatos/química , Triglicerídeos/química
9.
J Food Sci ; 84(4): 782-791, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30875433

RESUMO

Cholecalciferol, also known as vitamin D3 , is a recognized therapeutic agent for treatment of bone diseases and cancer. However, instability and poor bioavailability have been major challenges for delivering Vitamin D3 . The objective of this study was to formulate improved nanostructured lipid carrier (NLC) vitamin D3 emulsions. We tested the effect of different carrier oils and the use of a solid lipid nanoparticle emulsifier, polyglycerol polyricinoleate (PGPR) on the stability of the vitamin D3 emulsions. In contrast to the control that used glyceryl monostearate (GMS) the PGPR substitution resulted in relatively small particle sizes (0.30 to 0.43 µm), with high absolute value of zeta potentials (39.5 to 67.8 mV) and high encapsulation efficiency (85.2% to 90.4%). The stability of the NLC emulsions against environmental stresses was evaluated under varying conditions of ionic strength, pH, freeze-thaw cycles, and storage at different temperatures. Although NLC emulsions were stable at high ionic strengths, they were found to be unstable at low pH (<3), which led to aggregation and coalescence of emulsion droplets. In case of freeze-thaw stress, although relatively stable compared to control NLC, the PGPR substituted groups exhibited a slight increase in particle size and a decrease in zeta potential when the cycle was repeated five times. Additionally, we found that PGPR-substituted emulsions showed higher liquid dispersion stability than controls at 25 and 65 °C. Thus, we have formulated a modified NLC vitamin D3 emulsion that can be widely used in the food industry. PRACTICAL APPLICATION: Vitamin D3 , an essential micronutrient, is often added as supplements in food products and beverages for added health benefits. However, the stability of vitamin D3 emulsions that are used in the preparation of such products has been a major concern. We have developed a modified emulsion that has improved stability against environmental stresses. We believe, in future, this formulation can be efficiently used in the food industry.


Assuntos
Colecalciferol/química , Emulsões/química , Glicerol/análogos & derivados , Nanoestruturas/química , Ácidos Ricinoleicos/química , Composição de Medicamentos , Emulsificantes , Glicerol/química , Concentração Osmolar , Tamanho da Partícula
10.
Int J Pharm ; 563: 79-90, 2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-30825557

RESUMO

We present a systematic study of the role of poly(ethylene glycol) (PEG) content in NPs on drug skin absorption. Cholecalciferol-loaded NPs of 100 nm of diameter were prepared by flash nanoprecipitation from PLA-b-PEG copolymers of various PEG lengths. As PEG content increased in the polymer, we observed a transition from a frozen solid particle structure to a more dynamic particle structure. Skin absorption studies showed that polymer composition influenced drug penetration depending on skin condition (intact or impaired). In intact skin, highly PEGylated NPs achieved the best skin absorption, even if the penetration differences between the NPs were low. In impaired skin, on the contrary, non-PEGylated NPs (PLA NPs) promoted a strong drug deposition. Further investigations revealed that the strong drug accumulation from PLA NPs in impaired skin was mediated by aggregation and sedimentation of NPs due to the release of charged species from the skin. In contrast, the dynamic structure of highly PEGylated NPs promoted wetting of the surface and interactions with skin lipids, improving drug absorption in intact skin. Since NPs structure and surface properties determine the drug penetration mechanisms at the NP-skin interface, this work highlights the importance of properly tuning NPs composition according to skin physiopathology.


Assuntos
Colecalciferol/administração & dosagem , Lactatos/administração & dosagem , Nanopartículas/administração & dosagem , Polietilenoglicóis/administração & dosagem , Absorção Cutânea , Pele/metabolismo , Animais , Colecalciferol/química , Feminino , Técnicas In Vitro , Lactatos/química , Peso Molecular , Nanopartículas/química , Polietilenoglicóis/química , Pele/lesões , Suínos
11.
Biomed Chromatogr ; 33(7): e4538, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30912169

RESUMO

A liquid chromatography/electrospray ionization-tandem mass spectrometry-based method was developed for the identification of the conjugation positions of the monoglucuronides of 25-hydroxyvitamin D3 [25(OH)D3 ] and 24,25-dihydroxyvitamin D3 [24,25(OH)2 D3 ] in human urine. The method employed derivatization with 4-(4-dimethylaminophenyl)-1,2,4-triazoline-3,5-dione to convert the glucuronides into fragmentable derivatives, which provided useful product ions for identifying the conjugation positions during the MS/MS. The derivatization also enhanced the assay sensitivity and specificity for urine sample analysis. The positional isomeric monoglucuronides, 25(OH)D3 -3- and -25-glucuronides, or 24,25(OH)2 D3 -3-, -24- and -25-glucuronides, were completely separated from each other under the optimized LC conditions. Using this method, the conjugation positions were successfully determined to be the C3 and C24 positions for the glucuronidated 25(OH)D3 and 24,25(OH)2 D3 , respectively. The 3-glucuronide was not present for 24,25(OH)2 D3 , unlike 25(OH)D3 , thus we found that selective glucuronidation occurs at the C24-hydroxy group for 24,25(OH)2 D3 .


Assuntos
Colecalciferol/urina , Cromatografia Líquida/métodos , Glucuronídeos/urina , Espectrometria de Massas em Tandem/métodos , Colecalciferol/química , Colecalciferol/metabolismo , Glucuronídeos/química , Glucuronídeos/metabolismo , Humanos , Espectrometria de Massas por Ionização por Electrospray/métodos
12.
Food Funct ; 10(4): 1826-1835, 2019 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-30874272

RESUMO

The influence of carrier oil type (corn, fish, or flaxseed oil) on the production, stability, and simulated gastrointestinal behavior of vitamin-fortified nanoemulsions was studied. The nanoemulsions were formulated using pea protein as an emulsifier since there is increasing interest in substituting artificial and animal-based food ingredients with natural plant-based alternatives. Lipid digestion and vitamin D3 bioaccessibility were measured when the nanoemulsions were subjected to a three-stage in vitro gastrointestinal tract: oral, gastric, and small intestinal. The majority of all three lipids were digested within the first few minutes in the simulated small intestine, with the corn oil nanoemulsions being digested faster than the fish or flaxseed oils. Moreover, a greater fraction of triglycerides were digested by the end of the small intestine for the corn oil than for the fish and flaxseed oils. For the different carrier oils, vitamin bioaccessibility was ranked: corn oil > flaxseed oil ≈ fish oil. These results suggest that monounsaturated-rich oils (such as corn oil) are better for encapsulating and delivering vitamin D3 than polyunsaturated-rich ones (such as flaxseed or fish oil). The insights gained here may aid in the formulation of more efficacious vitamin-fortified foods and beverages from plant-derived ingredients.


Assuntos
Colecalciferol/química , Colecalciferol/metabolismo , Óleo de Milho/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Óleos de Peixe/química , Óleo de Semente do Linho/química , Proteínas de Plantas/química , Disponibilidade Biológica , Óleo de Milho/metabolismo , Digestão , Portadores de Fármacos/metabolismo , Sistemas de Liberação de Medicamentos/instrumentação , Emulsões/química , Emulsões/metabolismo , Óleos de Peixe/metabolismo , Alimentos Fortificados/análise , Humanos , Óleo de Semente do Linho/metabolismo , Nanoestruturas/química , Ervilhas/química , Proteínas de Plantas/metabolismo
13.
Food Chem ; 286: 289-296, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-30827608

RESUMO

ß-Casein, a phosphoprotein representing 37% of the bovine milk caseins, has specific features promoting its application as a nanocarrier for hydrophobic bioactives. In this study, the interactions of ß-casein with curcumin and vitamin D3 under the same physico-chemical conditions were investigated. The interaction kinetics have been studied by surface plasmon resonance (SPR) and fluorescence spectroscopy. The KD value for curcumin-ß-casein interaction has been successfully evaluated (4.1 ±â€¯0.7 × 10-4 M) using SPR by fitting data to a 1:1 Langmuir interaction model. Conversely, the SPR responses obtained for vitamin D3 show that the interactions between this hydrophobic compound and the ß-casein immobilized on the sensor chip were below the sensitivity of the SPR apparatus. Moreover, the fluorescence quenching data show that curcumin has higher affinity to ß-casein (KA = 23.5 ±â€¯1.9 × 104 M-1) than vitamin D3 (KA = 5.8 ±â€¯1.1 × 104 M-1).


Assuntos
Caseínas/metabolismo , Colecalciferol/metabolismo , Curcumina/metabolismo , Espectrometria de Fluorescência , Ressonância de Plasmônio de Superfície , Animais , Caseínas/química , Bovinos , Colecalciferol/química , Curcumina/química , Interações Hidrofóbicas e Hidrofílicas , Micelas , Leite/metabolismo , Ligação Proteica
14.
Chin J Nat Med ; 16(10): 766-773, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30322610

RESUMO

Several chemical compounds can restore pigmentation in vitiligo through mechanisms that vary according to disease etiology. In the present study, we investigated the melanogenic activity of six structurally distinct compounds, namely, scopoletin, kaempferol, chrysin, vitamin D3, piperine, and 6-benzylaminopurine. We determined their effectiveness, toxicity, and mechanism of action for stimulating pigmentation in B16F10 melanoma cells and in a zebrafish model. The melanogenic activity of 6-benzylaminopurine, the compound identified as the most potent, was further verified by measuring green fluorescent protein concentration in tyrp1 a: eGFP (tyrosinase-related protein 1) zebrafish and mitfa: eGFP (microphthalmia associated transcription factor) zebrafish and antioxidative activity. All the tested compounds were found to enhance melanogenesis responses both in vivo and in vitro at their respective optimal concentration by increasing melanin content and expression of TYR and MITF. 6-Benzyamino-purine showed the strongest re-pigmentation action at a concentration of 20 µmol·L-1in vivo and 100 µmol·L-1in vitro, and up-regulated the strong fluorescence expression of green fluorescent protein in tyrp1a: eGFP and mitfa: eGFP zebrafish in vitro. However, its relative anti-oxidative activity was found to be very low. Overall, our results indicated that 6-benzylaminopurine stimulated pigmentation through a direct mechanism, by increasing melanin content via positive regulation of tyrosinase activity in vitro, as well as up-regulating the expression of the green fluorescent protein in transgenic zebrafish in vivo.


Assuntos
Alcaloides/farmacologia , Benzodioxóis/farmacologia , Compostos de Benzil/farmacologia , Colecalciferol/farmacologia , Flavonoides/farmacologia , Quempferóis/farmacologia , Melaninas/metabolismo , Piperidinas/farmacologia , Alcamidas Poli-Insaturadas/farmacologia , Purinas/farmacologia , Escopoletina/farmacologia , Vitiligo/metabolismo , Alcaloides/química , Animais , Benzodioxóis/química , Compostos de Benzil/química , Colecalciferol/química , Flavonoides/química , Humanos , Quempferóis/química , Melaninas/genética , Monofenol Mono-Oxigenase/genética , Monofenol Mono-Oxigenase/metabolismo , Pigmentação/efeitos dos fármacos , Piperidinas/química , Alcamidas Poli-Insaturadas/química , Purinas/química , Escopoletina/química , Vitiligo/tratamento farmacológico , Vitiligo/enzimologia , Peixe-Zebra
15.
Am J Hum Biol ; 30(5): e23166, 2018 09.
Artigo em Inglês | MEDLINE | ID: mdl-30198140

RESUMO

OBJECTIVES: The purpose of this study was (1) to elucidate any reciprocal seasonal relationship that might exist between red cell folate (RCF) and serum vitamin D3 Levels; (2) to explore whether folate-related gene variants that influence/alter DNA-thymidylate and methyl group biosynthesis modify any associations detected in objective 1; and (3) to consider whether these processes might influence reproductive success consistent with the "folate-vitamin D-UV hypothesis of skin pigmentation" evolutionary model. METHODS: A large (n = 649) Australian cross-sectional study population was examined. Polymerase chain reaction (PCR)/Restriction fragment length polymorphism (RFLP) analysis was used to genotype C677T-MTHFR, C1420T-SHMT, T401C-MTHFD and 2R > 3R-TS. RCF was measured by chemiluminescent immunoassay and vitamin D2 and D3 by HPLC. RESULTS: RCF and photosynthesized vitamin D3 , but not RCF and dietary vitamin D2 , exhibit a significant reciprocal association in spring and summer. Three folate genes (C677T-MTHFR, C1420T-SHMT, and 2R > 3R-TS) strengthen this effect in spring, and another (T401C-MTHFD) in summer. Effects are seasonal, and do not occur over the whole year. CONCLUSIONS: Findings are consistent with what might be required for the "folate-vitamin D-UV hypothesis of skin pigmentation" model. It suggests genetic influence in provision of one-carbon units by 5,10-methylene-H4 folate, may be an important factor in what appears to be a clear seasonal relationship between vitamin D3 and folate status.


Assuntos
Ácido Fólico/sangue , Vitamina D/sangue , Vitaminas/sangue , Austrália , Colecalciferol/sangue , Colecalciferol/química , Estudos Transversais , Ergocalciferóis/sangue , Ergocalciferóis/química , Eritrócitos/química , Feminino , Ácido Fólico/genética , Humanos , Masculino , Reação em Cadeia da Polimerase , Polimorfismo de Fragmento de Restrição , Estações do Ano , Soro/química , Vitamina D/genética , Vitaminas/genética
16.
AAPS PharmSciTech ; 19(5): 2418-2425, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29869312

RESUMO

Vitamin D3 supplementation is important to prevent and treat hypovitaminosis that is a worldwide public health issue. Most types of supplementation are by oral route or fortification foods. The alternative route must be investigated, as transdermal route, for people with fat malabsorption or other diseases that impair the absorption of vitamin D3. This study focused on verifying the feasibleness of vitamin D3 skin retention and permeation with the presence of chemical penetration enhancers (soybean lecithin, isopropyl palmitate, propylene glycol, ethoxydiglycol, and cereal alcohol) at different pharmaceutical forms (gel and cream) through a human skin. The integrity of skin was evaluated by transepidermal water loss (TEWL) during the skin retention and permeation test. The combination of chemical penetration enhancers presented in cream did not compromise the skin, different from the gel that association of cereal alcohol and propylene glycol compromised the skin in 24 h. Gel formulation showed vitamin D3 detection at stratum corneum in 4 h and at epidermis and dermis in 24 h. Vitamin D3 demonstrated an affinity with the vehicle in the cream formulation and was detected at the skin surface. No active was found at receptor fluid for both formulations. In conclusion, the vitamin D3 did not indicate feasibleness for transdermal use probably due to its physical-chemical characteristics such as high lipophilicity since it was not permeated through a human skin. Nevertheless, the transdermal route should be continuously investigated with less lipophilic derivates of vitamin D3 and with different combination of penetration enhancers.


Assuntos
Conservadores da Densidade Óssea/química , Conservadores da Densidade Óssea/metabolismo , Colecalciferol/química , Colecalciferol/metabolismo , Absorção Cutânea/fisiologia , Administração Cutânea , Conservadores da Densidade Óssea/farmacologia , Colecalciferol/farmacologia , Composição de Medicamentos , Epiderme/efeitos dos fármacos , Epiderme/metabolismo , Feminino , Humanos , Técnicas de Cultura de Órgãos/métodos , Permeabilidade/efeitos dos fármacos , Pele/efeitos dos fármacos , Pele/metabolismo , Absorção Cutânea/efeitos dos fármacos , Água/metabolismo
17.
J Photochem Photobiol B ; 185: 169-175, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29936410

RESUMO

Ultraviolet (UV) light is absorbed by nucleic acids, proteins or other endogenous chromophores, such as porphyrins, flavins and melanin, triggering biological processes in skin cells. Both UV-induced mutations in melanocytes and changes in the immune microenvironment are understood to play a role in the development of cutaneous melanoma. The degree of UV-induced stress and the protection against this stress are influenced by both intracellular and intercellular molecular interactions. The present review summarizes the known major molecular biological changes induced by UV light in the skin that play a role in melanoma initiation and promotion. Nevertheless, cutaneous melanoma is not a homogenous disease, and the interaction of variable environmental exposure and different genetic susceptibility and other host factors lead to the formation of melanomas with different biological behavior and clinical characteristics. This review highlights the challenges in the understanding of how UV radiation contributes to the formation of cutaneous melanoma, and reviews the new results of photobiology and their link to tumor genetics and tumor immunology with potential implications on melanoma prevention and therapeutic strategies. The information presented here is expected to add clarity to ongoing research efforts in this field to aid the development of novel strategies to prevent and treat melanoma.


Assuntos
Melanoma/etiologia , Neoplasias Cutâneas/etiologia , Pele/efeitos da radiação , Raios Ultravioleta , Animais , Colecalciferol/química , Colecalciferol/metabolismo , Dano ao DNA/efeitos da radiação , Humanos , Melaninas/química , Melaninas/metabolismo , Melanoma/imunologia , Melanoma/metabolismo , Espécies Reativas de Oxigênio/química , Espécies Reativas de Oxigênio/metabolismo , Pele/metabolismo , Neoplasias Cutâneas/imunologia , Neoplasias Cutâneas/metabolismo
18.
Food Chem ; 261: 149-156, 2018 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-29739575

RESUMO

Vitamin D3 levels are known to sometimes decline in fortified products, which could be due to its degradation, although the exact mechanism is unknown. In this study, the influence of processing and storage conditions on lipid oxidation and vitamin D3 degradation were studied. Simulated whole milk powders with and without heat treatment were stored for 12 months at two different storage temperatures (20 °C and 40 °C). Stored samples without heat treatment showed higher lipid oxidation products analyzed by PV and TBARS values compared to those with heat treatment. Higher storage temperature also resulted in higher levels of lipid oxidation products. The concentration of vitamin D3 was also analyzed using UHPLC-MS/MS after PTAD derivatization in stored samples. An inverse relationship was observed between lipid oxidation products and vitamin D3 content. Finally, previtamin D3 and vitamin D3 oxidation products were quantified in stored samples using MRM analysis.


Assuntos
Colecalciferol/química , Manipulação de Alimentos , Armazenamento de Alimentos , Lipídeos/química , Leite/química , Animais , Temperatura Alta , Oxirredução , Pós
19.
Pharm Res ; 35(6): 117, 2018 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-29663141

RESUMO

PURPOSE: Poor corneal permeability, nasolacrimal drainage and requirement of chronic administration are major drawbacks of existing therapies for ocular inflammation. Hence, we designed topical micelles of PEG2000 conjugated with cholecalciferol (PEGCCF). METHODS: Integrin targeted tacrolimus loaded PEGCCF micelles (TTM) were prepared by solvent diffusion evaporation method and characterized for particle size, osmolality, encapsulation efficiency and drug loading. Therapeutic potential of TTM was evaluated in benzalkonium chloride induced ocular inflammation model in BALB/c mice. Corneal flourescein staining and histopathological analysis of corneal sections was performed. RESULTS: TTM had a particle size of 45.3 ± 5.3 nm, encapsulation efficiency (88.7 ± 0.9%w/w) and osmolality of 292-296 mOsmol/Kg. TTM significantly reduced the corneal fluorescence as compared to tacrolimus suspension (TACS). H&E staining showed that TTM could restore corneal epithelial thickness, reduce stromal edema (p < 0.05) and decrease number of inflammatory cells (p < 0.01) compared with TACS. Immunohistochemistry analysis demonstrated lower expression of Ki67 + ve cells (p < 0.05) and IL-6 throughout the cornea against TACS (p < 0.01) and the control (p < 0.001). CONCLUSIONS: TTM is an innovative delivery system for improving ocular inflammation due to a) integrin targeting b) PEGCCF in the form of carrier and c) anti-inflammatory and synergistic effect (due to Pgp inhibition) with TAC.


Assuntos
Portadores de Fármacos/química , Oftalmopatias/tratamento farmacológico , Inflamação/tratamento farmacológico , Tacrolimo/administração & dosagem , Administração Oftálmica , Animais , Compostos de Benzalcônio/toxicidade , Colecalciferol/química , Modelos Animais de Doenças , Composição de Medicamentos/métodos , Olho/efeitos dos fármacos , Olho/patologia , Oftalmopatias/induzido quimicamente , Oftalmopatias/patologia , Feminino , Humanos , Inflamação/induzido quimicamente , Inflamação/patologia , Integrinas/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Micelas , Polietilenoglicóis/química , Tacrolimo/farmacocinética
20.
Org Biomol Chem ; 16(14): 2448-2455, 2018 04 04.
Artigo em Inglês | MEDLINE | ID: mdl-29560490

RESUMO

Both 2α- and 2ß-hydroxypropyl substituted 14-epi-1α,25-dihydroxy-19-nortachysterols were synthesized to study the human vitamin D receptor (hVDR) binding affinity, binding configurations, and interactions with amino acid residues in the ligand binding domain of hVDR by X-ray co-crystallographic analysis. In conjunction with our previous results on 14-epi-19-nortachysterol, 2-methylidene-, 2α-methyl-, 2ß-methyl, and 2α-hydroxypropoxy-14-epi-19-nortachysterol, we propose a variety of effects of substitution at the C2 position in the 14-epi-19-nortachysterol skeleton on biological activities.


Assuntos
Colecalciferol/análogos & derivados , Receptores de Calcitriol/química , Sítios de Ligação , Colecalciferol/síntese química , Colecalciferol/química , Cristalografia por Raios X , Humanos , Ligantes , Estrutura Molecular
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