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1.
Nutrients ; 16(10)2024 May 08.
Artigo em Inglês | MEDLINE | ID: mdl-38794653

RESUMO

Lutein (Lut) and zeaxanthin (Zeax) are found in the blood and are deposited in the retina (macular pigment). Both are found in the diet in free form and esterified with fatty acids. A high intake and/or status is associated with a lower risk of chronic diseases, especially eye diseases. There is a large global demand for Lut in the dietary supplement market, with marigold flowers being the main source, mainly as lutein esters. As the bioavailability of Lut from free or ester forms is controversial, our aim was to assess the bioavailability of Lut (free vs. ester) and visual contrast threshold (CT). Twenty-four healthy subjects (twelve women, twelve men), aged 20-35 and 50-65 years, were enrolled in a cross-sectional study to consume 6 mg lutein/day from marigold extract (free vs. ester) for two months. Blood samples were taken at baseline and after 15, 40, and 60 days in each period. Serum Lut and Zeax were analysed using HPLC, and dietary intake was determined with a 7-day food record at the beginning of each period. CT, with and without glare, was at 0 and 60 days at three levels of visual angle. Lut + Zeax intake at baseline was 1.9 mg/day, and serum lutein was 0.36 µmol/L. Serum lutein increased 2.4-fold on day 15 (up to 0.81 and 0.90 µmol/L with free and ester lutein, respectively) and was maintained until the end of the study. Serum Zeax increased 1.7-fold. There were no differences in serum Lut responses to free or ester lutein at any time point. CT responses to lutein supplementation (free vs. ester) were not different at any time point. CT correlated with Lut under glare conditions, and better correlations were obtained at low frequencies in the whole group due to the older group. The highest correlations occurred between CT at high frequency and with glare with serum Lut and Lut + Zeax. Only in the older group were inverse correlations found at baseline at a high frequency with L + Z and with Lut/cholesterol and at a low frequency with Lut/cholesterol. In conclusion, daily supplementation with Lut for 15 days significantly increases serum Lut in normolipemic adults to levels associated with a reduced risk of age-related eye disease regardless of the chemical form of lutein supplied. Longer supplementation, up to two months, does not significantly alter the concentration achieved but may contribute to an increase in macular pigment (a long-term marker of lutein status) and thus improve the effect on visual outcomes.


Assuntos
Disponibilidade Biológica , Luteína , Tagetes , Zeaxantinas , Humanos , Luteína/sangue , Luteína/administração & dosagem , Luteína/farmacocinética , Pessoa de Meia-Idade , Masculino , Feminino , Adulto , Zeaxantinas/sangue , Zeaxantinas/administração & dosagem , Estudos Transversais , Tagetes/química , Idoso , Adulto Jovem , Flores/química , Ésteres , Suplementos Nutricionais , Sensibilidades de Contraste
2.
Crit Rev Food Sci Nutr ; 62(9): 2375-2390, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33249868

RESUMO

Lutein, a potent antioxidant and the main macular pigment that protects the macula from light-initiated oxidative damage, has low bioavailability. Various nanoscale delivery systems have been developed for improving its bioavailability. This systematic review aims to evaluate the effectiveness of nanoscale delivery systems on improving lutein bioavailability in rodent models. Using EBSCOhost and PubMed, a total of eleven peer-reviewed articles published from 2000 to 2020 were identified. Plasma lutein concentration, pharmacokinetic parameters, including maximum concentration (Cmax), area under curve (AUC), and time to reach the maximum concentration (Tmax), and lutein accumulation in organs were extracted to evaluate the bioavailability of lutein using nanoscale delivery methods as compared with unencapsulated or raw lutein. Various nanoscale delivery systems, including polymer nanoparticles, emulsions, and lutein nanoparticles, significantly improved the bioavailability of lutein, as evidenced by increased plasma lutein concentrations, Cmax, or AUC. Additionally, five out of seven studies observed enhanced accumulation of lutein in the liver and the eyes. Polymer nanoparticles and emulsions improve the dispersibility and stability of lutein, thus lutein might be more accessible in the small intestine. Lutein nanoparticles shortened the Tmax. Further studies are warranted to evaluate the effectiveness of nanoscale delivery systems on improving the functionalities of lutein.


Assuntos
Luteína , Nanopartículas , Animais , Disponibilidade Biológica , Emulsões , Luteína/farmacocinética , Roedores
3.
AAPS PharmSciTech ; 22(5): 169, 2021 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-34080086

RESUMO

Lutein has been used as a dietary supplement for the treatment of eye diseases, especially age-related macular degeneration. For oral formulations, we investigated lutein stability in artificial set-ups mimicking different physiological conditions and found that lutein was degraded over time under acidic conditions. To enhance the stability of lutein upon oral intake, we developed enteric-coated lutein solid dispersions (SD) by applying a polymer, hydroxypropyl methylcellulose acetate succinate (HPMCAS-LF), through a solvent-controlled precipitation method. The SD were characterized in crystallinity, morphology, and drug entrapment. In the dissolution profile of lutein SD, a F80 formulation showed resistance toward the acidic environment under simulated gastric conditions while exhibiting a bursting drug release under simulated intestinal conditions. Our results highlight the potential use of HPMCAS-LF as an effective matrix to enhance lutein bioavailability during oral delivery and to provide novel insights into the eye-care supplement industry, with direct benefits for the health of patients.


Assuntos
Luteína/síntese química , Luteína/farmacocinética , Metilcelulose/análogos & derivados , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão/métodos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Humanos , Metilcelulose/síntese química , Metilcelulose/farmacocinética , Polímeros/síntese química , Polímeros/farmacocinética , Solubilidade , Solventes , Difração de Raios X/métodos
4.
Nutr Res ; 91: 36-43, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-34134039

RESUMO

Lutein exhibits effective antioxidant activity conferring protective action against oxidative stress in age-related macular degeneration and cognitive decline. The inability to synthesize these compounds by the human body and the necessity to combat day-to-day oxidative stress prioritizes daily consumption of lutein. However, the bioavailability of the orally consumed lutein largely depends on its gastrointestinal absorption and subsequent metabolism which is in turn governed by various intrinsic and extrinsic factors. One of the most important yet least studied factors is the genetic make-up of an individual. The proteins that partake in the absorption, transportation, metabolism and excretion of lutein are encoded by the genes that experience inter-individual variability. Reports suggest that the unanimous effect of phenotypes resulting from such inter-individual variability in the genes of interest causes modulation of lutein bioavailability which is discussed in detail in this review article. However, despite the available reports, a community-based approach to a larger population is required to obtain a stronger understanding of the relationship between inter-individual variability among these genes and lutein bioavailability. Such an understanding of nutrigenetics could not only pave a way to decipher mechanisms that modulate lutein bioavailability but also help in setting the dosage requirements of each patient.


Assuntos
Variação Genética , Luteína/farmacocinética , Zeaxantinas/metabolismo , Disponibilidade Biológica , Humanos , Absorção Intestinal , Luteína/metabolismo , Fenótipo
5.
Exp Eye Res ; 209: 108680, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-34161819

RESUMO

Accumulation of bisretinoids such as A2E and its isomer iso-A2E is thought to mediate blue light-induced oxidative damage associated with age-related macular degeneration (AMD) and autosomal recessive Stargardt disease (STGD1). We hypothesize that increasing dietary intake of the macular carotenoids lutein and zeaxanthin in individuals at risk of AMD and STGD1 can inhibit the formation of bisretinoids A2E and iso-A2E, which can potentially ameliorate macular degenerative diseases. To study the beneficial effect of macular carotenoids in a retinal degenerative diseases model, we used ATP-binding cassette, sub-family A member 4 (Abca4-/-)/ß,ß-carotene-9',10'-oxygenase 2 (Bco2-/-) double knockout (KO) mice that accumulate elevated levels of A2E and iso-A2E in the retinal pigment epithelium (RPE) and macular carotenoids in the retina. Abca4-/-/Bco2-/- and Abca4-/- mice were fed a lutein-supplemented chow, zeaxanthin-supplemented chow or placebo chow (~2.6 mg of carotenoid/mouse/day) for three months. Visual function and electroretinography (ERG) were measured after one month and three months of carotenoid supplementation. The lutein and zeaxanthin supplemented Abca4-/-/Bco2-/- mice had significantly lower levels of RPE/choroid A2E and iso-A2E compared to control mice fed with placebo chow and improved visual performance. Carotenoid supplementation in Abca4-/- mice minimally raised retinal carotenoid levels and did not show much difference in bisretinoid levels or visual function compared to the control diet group. There was a statistically significant inverse correlation between carotenoid levels in the retina and A2E and iso-A2E levels in the RPE/choroid. Supplementation with retinal carotenoids, especially zeaxanthin, effectively inhibits bisretinoid formation in a mouse model of STGD1 genetically enhanced to accumulate carotenoids in the retina. These results provide further impetus to pursue oral carotenoids as therapeutic interventions for STGD1 and AMD.


Assuntos
Transportadores de Cassetes de Ligação de ATP/genética , Dioxigenases/genética , Regulação da Expressão Gênica , Luteína/farmacocinética , Degeneração Macular/tratamento farmacológico , Epitélio Pigmentado da Retina/efeitos dos fármacos , Zeaxantinas/farmacocinética , Transportadores de Cassetes de Ligação de ATP/biossíntese , Animais , Dioxigenases/biossíntese , Modelos Animais de Doenças , Eletrorretinografia , Degeneração Macular/metabolismo , Degeneração Macular/fisiopatologia , Camundongos Endogâmicos C57BL , Camundongos Knockout , Epitélio Pigmentado da Retina/metabolismo , Visão Ocular/efeitos dos fármacos
6.
Carbohydr Polym ; 254: 117409, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33357895

RESUMO

Aiming to enhance therapeutic efficiency of lutein, lutein loaded chitosan-sodium alginate (CS-SA) based nanocarrier system (LNCs) were prepared and evaluated for lutein bioavailability and pharmacokinetics in diabetic rats in comparison to micellar lutein (control). Further, cytotoxicity, cellular uptake and protective activity against H2O2 induced oxidative stress in ARPE-19 cells were studied. Results revealed that LNCs displayed maximal lutein AUC in plasma, liver and eye respectively in normal (3.1, 2.7 and 5.2 folds) and diabetic (7.3, 3.4 and 2.8 folds) rats. Lutein from LNCs exhibited a higher half-life time, mean residence time and slow clearance from the plasma, indicating prolonged circulation compared to control. In ARPE-19 cells, pre-treatment with LNCs (10 µM) have significantly attenuated H2O2 induced cell death, intracellular ROS and mitochondrial membrane potential compared to control. In conclusion, LNCs improve the lutein bioavailability in conditions like diabetes, diabetic retinopathy and cataract to curtail oxidative stress in retinal cells.


Assuntos
Alginatos/química , Quitosana/química , Diabetes Mellitus Experimental/tratamento farmacológico , Portadores de Fármacos/química , Ácidos Graxos/química , Absorção Gastrointestinal/efeitos dos fármacos , Peróxido de Hidrogênio/farmacologia , Luteína/administração & dosagem , Luteína/farmacocinética , Nanopartículas/química , Estresse Oxidativo/efeitos dos fármacos , Substâncias Protetoras/administração & dosagem , Substâncias Protetoras/farmacologia , Epitélio Pigmentado da Retina/efeitos dos fármacos , Animais , Disponibilidade Biológica , Linhagem Celular , Meia-Vida , Humanos , Luteína/sangue , Masculino , Micelas , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Ratos , Ratos Wistar , Epitélio Pigmentado da Retina/metabolismo
7.
Food Chem ; 344: 128623, 2021 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-33221100

RESUMO

Eggs' nutritional value has been enhanced by enriching hen's diet with bioactive compounds, but factors influencing bio-accessibility are unspecified. This study investigated the effect of hen breed, diet enrichment, and cooking methods in modulating the egg compounds' bio-accessibility after gastrointestinal (GI) digestion. White Leghorn (WLH) and Rhode Island Red (RIR) hens were fed a corn-soybean-based diet enriched with flaxseed and carotenoids; eggs were collected, cooked, and subjected to simulated GI digestion. The results showed that egg proteins were equally digestible with no change in the degree of hydrolysis (DH). The linolenic fatty acid in enriched-cooked samples remained bio-accessible after GI digestion. The lutein bio-accessibility in enriched eggs decreased after GI digestion except in RIR fried sample. Eggs from WLH and RIR achieved similar peptide content after GI digestion. These results elucidate the bio-accessibility of different bioactive compounds in cooked eggs and the use of eggs as potential functional foods.


Assuntos
Culinária/métodos , Proteínas Dietéticas do Ovo/farmacocinética , Ovos , Luteína/análise , Ração Animal , Animais , Disponibilidade Biológica , Carotenoides/análise , Carotenoides/farmacologia , Galinhas , Digestão , Proteínas Dietéticas do Ovo/análise , Ovos/análise , Ácidos Graxos/metabolismo , Ácidos Graxos Ômega-3/farmacocinética , Feminino , Linho , Hidrólise , Luteína/farmacocinética , Zea mays/química
8.
Food Chem ; 343: 128437, 2021 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-33162255

RESUMO

The effective delivery of bioactive compounds has recently been receiving attention. In this study, a conjugate with BSA and fucoidan synthesized via the Maillard reaction was confirmed through electrophoresis, the o-phthalaldehyde assay, and through changes in absorbance. Two moles of fucoidan were glycated with one mole of BSA at 60 °C and 79% relative humidity for 4 days. The droplet coated with B-F conjugate remained stable during storage at 4 and 25 °C and slightly increased only at 55 °C however, the droplet coated with intact BSA and B/F mixture significantly increased. L/Z were degraded about 82, 79, and 36% for 4, 25, and 55 °C, respectively, regardless of the type of emulsifier. Although the conjugates could not prevent the degradation of lutein and zeaxanthin during storage, they improved the stability of the emulsion and showed 4.20-fold and 1.32-fold higher bioaccessibility than intact BSA and B/F mixtures, respectively.


Assuntos
Luteína/química , Polissacarídeos/química , Soroalbumina Bovina/química , Zeaxantinas/química , Disponibilidade Biológica , Chlamydomonas reinhardtii/química , Digestão , Eletroforese em Gel de Poliacrilamida , Emulsificantes/química , Emulsões/química , Emulsões/farmacocinética , Umidade , Luteína/farmacocinética , Reação de Maillard , Polissacarídeos/farmacocinética , Temperatura
9.
Nutrients ; 12(10)2020 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-32998324

RESUMO

Improvements in macular pigment optical density (MPOD) and contrast sensitivity after administration of 12 mg lutein alone and the timing at which efficacy is observed remain unknown. Therefore, lutein (12 mg), a crystalline formulation, was used in this study, considering its bioaccessibility. This study aimed to determine the effects of lutein administration for 16 weeks on MPOD, contrast sensitivity, and glare sensitivity, and changes in serum lutein levels were determined. The study subjects comprised 59 healthy male and female adults aged 20-69 years. The study diet included a placebo (placebo group) or a diet supplemented with 12 mg of lutein (lutein group). Each study diet was continuously administered for 16 weeks. At weeks 8 and 16, MPOD, contrast sensitivity, glare sensitivity, and serum lutein levels were evaluated. Compared with the placebo group, the lutein group showed significantly improved MPOD, contrast sensitivity, and glare sensitivity at week 16 and significantly increased serum lutein levels at weeks 8 and 16. Continuous administration of lutein for 16 weeks, considering its bioaccessibility, increased MPOD; it made the outlines of visible objects clearer and was effective in inhibiting decreases in visual function caused by glare from light.


Assuntos
Sensibilidades de Contraste/efeitos dos fármacos , Suplementos Nutricionais , Luteína/sangue , Luteína/farmacocinética , Pigmento Macular/metabolismo , Adulto , Idoso , Disponibilidade Biológica , Método Duplo-Cego , Feminino , Ofuscação , Voluntários Saudáveis , Humanos , Degeneração Macular/prevenção & controle , Masculino , Pessoa de Meia-Idade , Acuidade Visual , Adulto Jovem
10.
Mol Nutr Food Res ; 64(21): e2000228, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-32966703

RESUMO

SCOPE: The specific effect of the food matrix structure on fat-soluble micronutrient bioavailability is only partly understood. Evaluating fat-soluble micronutrient bioavailability after consumption of foods displaying similar composition but different structure is aimed at. METHODS AND RESULTS: Twelve healthy subjects are enrolled in a randomized, open label, crossover postprandial trial. Four different model foods are tested: custard, pudding, sponge cake, and biscuit. Vitamin D3 , lutein, and triglyceride chylomicron responses, evaluated as postprandial areas under the curve, are then assayed. Custard triglyceride response is higher than pudding and biscuit responses (up to +122.7%, p < 0.0001). Sponge cake vitamin D3 response is higher than biscuit response (+26.6%, p = 0.047). No difference between the model foods are observed regarding lutein responses. Triglyceride responses peak at 3 h for all conditions, while vitamin D3 and lutein peaks are delayed by 1 h with the biscuit matrix compared to other model foods. CONCLUSION: Food structure can significantly impact on triglyceride and vitamin D3 bioavailability in terms of absorbed amounts and/or maximum absorption time. The data highlight positive correlations between triglyceride, vitamin D, and lutein nutrient responses. These results are of particular interest to develop functional foods for population subgroups such as the elderly.


Assuntos
Alimentos , Luteína/farmacocinética , Triglicerídeos/farmacocinética , Vitamina D/farmacocinética , Disponibilidade Biológica , Culinária , Humanos , Luteína/sangue , Masculino , Triglicerídeos/sangue , Vitamina D/sangue , Adulto Jovem
11.
J Microencapsul ; 37(7): 502-516, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32842813

RESUMO

AIM: To prepare and characterise lutein-loaded polylactide-co-glycolide-polyethylene glycol-folate (PLGA-PEG-FOLATE) nanoparticles and evaluate enhanced uptake in SK-N-BE(2) cells. METHODS: Nanoparticles were prepared using O/W emulsion solvent evaporation and characterised using DLS, SEM, DSC, FTIR and in-vitro release. Lutein-uptake in SK-N-BE(2) cells was determined using flow-cytometry, confocal-microscopy and HPLC. Control was lutein PLGA nanoparticles. RESULTS: The size of lutein-loaded PLGA and PLGA-PEG-FOLATE nanoparticles were 189.6 ± 18.79 nm and 188.0 ± 4.06 nm, respectively. Lutein entrapment was ∼61%(w/w) and ∼73%(w/w) for PLGA and PLGA-PEG-FOLATE nanoparticles, respectively. DSC and FTIR confirmed encapsulation of lutein into nanoparticles. Cellular uptake studies showed ∼1.6 and ∼2-fold enhanced uptake of lutein from PLGA-PEG-FOLATE nanoparticles compared to PLGA nanoparticles and lutein, respectively. Cumulative release of lutein was higher in PLGA nanoparticles (100% (w/w) within 24 h) compared to PLGA-PEG-FOLATE nanoparticles (∼80% (w/w) in 48 h). CONCLUSION: Lutein-loaded PLGA-PEG-FOLATE nanoparticles could be a potential treatment for hypoxic ischaemic encephalopathy.


Assuntos
Portadores de Fármacos/química , Ácido Fólico/análogos & derivados , Luteína/administração & dosagem , Poliésteres/química , Polietilenoglicóis/química , Linhagem Celular Tumoral , Sistemas de Liberação de Medicamentos , Ácido Fólico/química , Humanos , Hipóxia-Isquemia Encefálica/tratamento farmacológico , Luteína/farmacocinética
12.
Int J Pharm ; 586: 119553, 2020 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-32561306

RESUMO

Present investigation explores cationic biopolymer core/shell nanoparticles (Chitosan@PLGA C/SNPs) for delivering carotenoids to brain via intranasal route for supressing oxidative stress in Alzheimer's disease (AD). The prepared C/SNPs exhibited particle size less than 150 nm with more than 80% of entrapment efficiency. Surface morphology confirmed uniform coating of shell (chitosan) over core PLGA NPs and suggested spherical nature and homogenous dispersion of C/SNPs. In-vitro release study demonstrated sustained release of lutein while C/SNPs permeation enhancement was confirmed by ex-vivo diffusion study. The study also investigated effect of cationic-shell with respect to anionic-core NPs on biocompatibility, cellular uptake, uptake mechanism, reactive-oxygen species (ROS) generation, ROS scavenging activity, blood-brain-barrier (BBB) permeation. The cellular uptake revealed enhanced internalization of nanoparticles via caveolae-mediated endocytosis. In-vitro co-culture model of BBB demonstrated efficient passage for C/SNPs through BBB. Antioxidant assay demonstrated significant ROS scavenging activity of C/SNPs. In-vivo pharmacokinetic and bio-distribution was performed along with in-vivo toxicity and stability. In-vivo toxicity demonstrated absence of any significant toxicity. Photo and thermal stability confirmed protection of lutein by C/SNPs. C/SNPs were highly deposited in brain following intranasal route. The obtained results demonstrate the potential application of cationic C/SNPs for attenuating oxidative stress in brain for effective AD therapy.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Luteína/farmacologia , Nanopartículas , Estresse Oxidativo/efeitos dos fármacos , Administração Intranasal , Doença de Alzheimer/fisiopatologia , Animais , Antioxidantes/administração & dosagem , Antioxidantes/farmacologia , Biopolímeros/química , Cátions , Linhagem Celular , Quitosana/química , Preparações de Ação Retardada , Cães , Portadores de Fármacos/química , Humanos , Luteína/administração & dosagem , Luteína/farmacocinética , Masculino , Camundongos , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Ratos , Ratos Sprague-Dawley , Distribuição Tecidual
13.
Nutrients ; 12(6)2020 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-32526861

RESUMO

Lutein is one of the few xanthophyll carotenoids that is found in high concentration in the macula of human retina. As de novo synthesis of lutein within the human body is impossible, lutein can only be obtained from diet. It is a natural substance abundant in egg yolk and dark green leafy vegetables. Many basic and clinical studies have reported lutein's anti-oxidative and anti-inflammatory properties in the eye, suggesting its beneficial effects on protection and alleviation of ocular diseases such as age-related macular degeneration, diabetic retinopathy, retinopathy of prematurity, myopia, and cataract. Most importantly, lutein is categorized as Generally Regarded as Safe (GRAS), posing minimal side-effects upon long term consumption. In this review, we will discuss the chemical structure and properties of lutein as well as its application and safety as a nutritional supplement. Finally, the effects of lutein consumption on the aforementioned eye diseases will be reviewed.


Assuntos
Oftalmopatias/tratamento farmacológico , Luteína/administração & dosagem , Animais , Disponibilidade Biológica , Catarata , Retinopatia Diabética/tratamento farmacológico , Dieta , Suplementos Nutricionais/efeitos adversos , Humanos , Luteína/química , Luteína/farmacocinética , Macula Lutea/química , Degeneração Macular/tratamento farmacológico , Miopia/tratamento farmacológico , Plantas Comestíveis/química , Retinopatia da Prematuridade/tratamento farmacológico
14.
Int J Biol Macromol ; 150: 578-594, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-32057885

RESUMO

Lutein is a hydrophobic antioxidant carotenoid with proven retinal and macular protection against oxidative stress. However, low aqueous solubility and bioavailability limit its clinical application. Hence, focus of the study was to improve the solubility and bioavailability of lutein by using a chitosan-oleic acid-sodium alginate-based nano-carrier system (LNCs). LNCs were prepared by ionic gelation and optimized by Plackett-Burman factorial algorithm. The size and zeta potential of LNCs were characterized by electron microscopy and dynamic light scattering. LNCs were within a size range of 40-160 nm with a desired zeta potential of +45 ± 5 mV and PDI of 0.174 ± 0.02. Further, LNCs displayed 1000-fold higher aqueous solubility with controlled and sustained release kinetics in vitro. Compared to micellar lutein, higher intracellular transport (40%) of lutein from LNCs in Caco-2 cells. Oral gavage of single dose of LNCs in rats resulted in higher (128.3%) bioavailability of lutein compared to micellar lutein. Further, a dose-dependent increase in plasma (135.20, 165.30 nmol/mL) and eyes (1.51 & 3.98 µg/g) was observed upon oral gavage of LNCs (10 and 100 mg/kg BW). Results demonstrate higher solubility and bioavailability of lutein from LNCs and hence could be an efficient therapeutic tool to conquer macular degeneration and retinopathy.


Assuntos
Alginatos/química , Quitosana/química , Portadores de Fármacos/química , Luteína/administração & dosagem , Luteína/farmacocinética , Nanopartículas/química , Ácido Oleico/química , Animais , Disponibilidade Biológica , Células CACO-2 , Cromatografia Líquida de Alta Pressão , Estabilidade de Medicamentos , Humanos , Luteína/química , Espectrometria de Massas , Micelas , Nanopartículas/ultraestrutura , Tamanho da Partícula , Ratos , Solubilidade , Análise Espectral , Termodinâmica
15.
Nutr Rev ; 78(9): 709-724, 2020 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-31925437

RESUMO

Lutein, a potent dietary carotenoid, has considerable biological activity and confers protection against age-related macular degeneration. Its bioavailability following consumption, however, depends on its rate of degradation. Nanodelivery systems with improved efficacy and stability are currently being developed to increase the bioavailability of lutein. This review examines nutraceutical approaches used in the development of such nanodelivery systems. It describes the methods of lutein preparation, the characteristics of various delivery systems, and the lutein delivery profile. In order to enhance lutein loading, provide electrostatic stabilization, and achieve the controlled release of lutein, adjuvants such as dextran moieties, whey proteins, medium-chain triglycerides, and chitosan polymers can be used to effectively reduce the particle size (< 70 nm) and improve encapsulation efficiency (to 99.5%). The improved bioavailability of lutein via nanocrystals incorporated into rapidly dissolving films for oral consumption is a new area of exploratory research. This review aims to provide clarity about current research aimed at enhancing the bioavailability of lutein through the development of nanodelivery systems.


Assuntos
Suplementos Nutricionais , Sistemas de Liberação de Medicamentos , Luteína/administração & dosagem , Nanopartículas/administração & dosagem , Animais , Disponibilidade Biológica , Humanos , Luteína/farmacocinética , Tamanho da Partícula
16.
Biosci Biotechnol Biochem ; 83(12): 2372-2374, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31382835

RESUMO

Lutein is poorly absorbed owing to their high hydrophobicity and crystallinity. This double-blind crossover trial involved eight healthy males who were administrated capsules containing either a lutein water-soluble formulation or a lutein oil suspension for 8 days. In the formulation group, plasma and erythrocytes lutein concentrations and baseline-corrected AUC were two-fold higher than those in the oil suspension group.


Assuntos
Luteína/administração & dosagem , Disponibilidade Biológica , Estudos Cross-Over , Suplementos Nutricionais , Método Duplo-Cego , Composição de Medicamentos , Meia-Vida , Humanos , Luteína/sangue , Luteína/química , Luteína/farmacocinética , Masculino , Solubilidade , Água/química
17.
Int J Nanomedicine ; 14: 2667-2681, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31043780

RESUMO

BACKGROUND: Lutein ester (LE) is an important carotenoid fatty acid ester. It is a form in which lutein is present in nature and is produced by free non-esterification and fatty acid esterification. LE is one of the safe sources of lutein. Increasing lutein intake can prevent and treat age-related macular degeneration. In addition, it can effectively inhibit gastric cancer, breast cancer, and esophageal cancer. However, the poor aqueous solubility of LE has impeded its clinical applications. OBJECTIVE: The objective of this study was to prepare lutein ester nanoparticles (LE-NPs) by liquid antisolvent precipitation techniques to improve the bioavailability of LE in vivo and improve eye delivery efficiency. MATERIALS AND METHODS: The physical characterization of LE-NPs was performed, and their in vitro dissolution rate, in vitro antioxidant capacity, in vivo bioavailability, tissue distribution, and ocular pharmacokinetics were studied and evaluated. RESULTS: The LE freeze-dried powder obtained under the optimal conditions possessed a particle size of ~164.1±4.3 nm. The physical characterization analysis indicated the amorphous form of LE-NPs. In addition, the solubility and dissolution rate of LE-NPs in artificial gastric juice were 12.75 and 9.65 times that of the raw LE, respectively. The bioavailability of LE-NPs increased by 1.41 times compared with that of the raw LE. The antioxidant capacity of LE-NPs was also superior to the raw LE. The concentration of lutein in the main organs of rats treated with the LE-NPs was higher than that in rats treated with the raw LE. The bioavailability of LE-NPs in rat eyeballs was found to be 2.34 times that of the original drug. CONCLUSION: LE-NPs have potential application as a new oral pharmaceutical formulation and could be a promising eye-targeted drug delivery system.


Assuntos
Precipitação Química , Sistemas de Liberação de Medicamentos/métodos , Ésteres/administração & dosagem , Luteína/administração & dosagem , Solventes/química , Administração Oftálmica , Administração Oral , Animais , Antioxidantes/farmacologia , Disponibilidade Biológica , Ésteres/química , Ésteres/farmacocinética , Luteína/química , Luteína/farmacocinética , Camundongos , Nanopartículas/administração & dosagem , Tamanho da Partícula , Ratos Sprague-Dawley , Solubilidade , Distribuição Tecidual
18.
Food Chem ; 286: 678-685, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-30827663

RESUMO

The effects of co-digestion of a carotenoid-rich vegetable such as carrot, cherry tomato or baby spinach with an anthocyanin-rich vegetable such as red cabbage with and without salad dressing on the intestinal cellular bioaccessibility (cBAC) of carotenoids and the resultant cellular antioxidant and anti-inflammatory activities were investigated. The % cBAC of lutein from the tested vegetables was 0.23-1.42%, lycopene 0.07-0.39%, α-carotene 0.01-0.12% and ß-carotene 0.03-0.61% respectively. The % cBAC of each of these carotenoids from the co-digested vegetables was significantly higher (p < 0.05) than from carrot, cherry tomato or baby spinach digested alone. % cBAC of total carotenoids was significantly increased by 46-191% (p < 0.05) as a result of the co-digestion. The vegetable co-digestion did not result in any impairment on the resultant cellular anti-oxidation and anti-inflammation (NO, IL-8 secretion). Among the tested vegetables, baby spinach co-digested with red cabbage showed synergistic bioactivities in all tested assays.


Assuntos
Antocianinas/farmacocinética , Carotenoides/farmacocinética , Verduras/química , Antioxidantes/análise , Antioxidantes/farmacologia , Disponibilidade Biológica , Brassica/metabolismo , Células CACO-2 , Carotenoides/análise , Digestão , Humanos , Luteína/farmacocinética , Licopeno/farmacocinética , Solanum lycopersicum/química , Spinacia oleracea/química , beta Caroteno/farmacocinética
19.
Yakugaku Zasshi ; 139(3): 341-347, 2019.
Artigo em Japonês | MEDLINE | ID: mdl-30828009

RESUMO

Preventive medicine and anti-aging medicine have received much attention recently due to an increase in the proportion of elderly people in the population, and to an increase in patients with lifestyle diseases. Oxidative stress is involved in the onset of lifestyle diseases, and various antioxidant supplements and antioxidant-fortified functional foods have recently become available. Many epidemiological studies have shown relationships between the consumption of polyphenol and carotenoid-rich foods and the prevention of lifestyle diseases. We have focused on the absorption mechanism of these food components that show low bioavailability, and have made efforts to improve their poor absorption based on their pharmacokinetic properties. In this report, as examples, we describe the enhancement of the absorption of coenzyme Q10 (CoQ10) and lutein. To improve the absorption of CoQ10, we focused on the component of emulsion. We found that a higher plasma concentration of CoQ10 could be obtained by creating an emulsion containing a surfactant with a higher hydrophile-lipophile balance (HLB) value. For the improvement of lutein absorption, we prepared a solid dispersion and self-emulsifying drug delivery system. It was shown that the plasma concentrations of lutein in these two formulation groups were increased compared with that in the powder group. The absorption of lutein was also evaluated by its cumulative amount in the lymph system. Our data showed that lutein is transferred from the small intestine into the lymph stream, rather than into the blood stream. Further investigations to improve the absorption of these components are in progress.


Assuntos
Antioxidantes/administração & dosagem , Antioxidantes/farmacocinética , Suplementos Nutricionais , Alimento Funcional , Luteína/administração & dosagem , Luteína/farmacocinética , Ubiquinona/análogos & derivados , Animais , Disponibilidade Biológica , Carotenoides/administração & dosagem , Carotenoides/farmacocinética , Sistemas de Liberação de Medicamentos , Emulsões , Alimento Funcional/análise , Humanos , Interações Hidrofóbicas e Hidrofílicas , Absorção Intestinal , Estilo de Vida , Sistema Linfático/metabolismo , Estresse Oxidativo , Polifenóis/administração & dosagem , Polifenóis/farmacocinética , Ratos , Tensoativos , Ubiquinona/administração & dosagem , Ubiquinona/farmacocinética
20.
Nutrients ; 12(1)2019 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-31892138

RESUMO

Sea buckthorn oil, derived from the fruits of the shrub, also termed seaberry or sandthorn, is without doubt a strikingly rich source of carotenoids, in particular zeaxanthin and ß-carotene. In the present study, sea buckthorn oil and an oil-in-water emulsion were subjected to a simulated gastro-intestinal in vitro digestion, with the main focus on xanthophyll bioaccessibility. Zeaxanthin mono- and di-esters were the predominant carotenoids in sea buckthorn oil, with zeaxanthin dipalmitate as the major compound (38.0%). A typical fatty acid profile was found, with palmitic (49.4%), palmitoleic (28.0%), and oleic (11.7%) acids as the dominant fatty acids. Taking into account the high amount of carotenoid esters present in sea buckthorn oil, the use of cholesterol esterase was included in the in vitro digestion protocol. Total carotenoid bioaccessibility was higher for the oil-in-water emulsion (22.5%) compared to sea buckthorn oil (18.0%) and even higher upon the addition of cholesterol esterase (28.0% and 21.2%, respectively). In the case of sea buckthorn oil, of all the free carotenoids, zeaxanthin had the highest bioaccessibility (61.5%), followed by lutein (48.9%), making sea buckthorn oil a potential attractive source of bioaccessible xanthophylls.


Assuntos
Hippophae/química , Óleos de Plantas/química , Xantofilas/farmacocinética , Disponibilidade Biológica , Digestão , Emulsões/química , Ácidos Graxos/análise , Frutas/química , Suco Gástrico/enzimologia , Humanos , Intestino Delgado/enzimologia , Luteína/farmacocinética , Esterol Esterase/metabolismo , Xantofilas/análise , Zeaxantinas/farmacocinética , beta Caroteno/farmacocinética
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