RESUMO
Omega-3 polyunsaturated fatty acids (n-3 PUFAs) play an important role in the development, maintenance, and function of the brain. Dietary supplementation of n-3 PUFAs in neurological diseases has been a subject of particular interest in preventing cognitive deficits, and particularly in age-related neurodegeneration. Developing strategies for the efficient delivery of these lipids to the brain has presented a challenge in recent years. We recently reported the preparation of n-3 PUFA-rich nanoliposomes (NLs) from salmon lecithin, and demonstrated their neurotrophic effects in rat embryo cortical neurons. The objective of this study was to assess the ability of these NLs to deliver PUFAs in cellulo and in vivo (in mice). NLs were prepared using salmon lecithin rich in n-3 PUFAs (29.13%), and characterized with an average size of 107.90 ± 0.35 nm, a polydispersity index of 0.25 ± 0.01, and a negative particle-surface electrical charge (-50.4 ± 0.2 mV). Incubation of rat embryo cortical neurons with NLs led to a significant increase in docosahexaenoic acid (DHA) (51.5%, p < 0.01), as well as palmitic acid, and a small decrease in oleic acid after 72 h (12.2%, p < 0.05). Twenty mice on a standard diet received oral administration of NLs (12 mg/mouse/day; 5 days per week) for 8 weeks. Fatty acid profiles obtained via gas chromatography revealed significant increases in cortical levels of saturated, monounsaturated, and n-3 (docosahexaenoic acid,) and n-6 (docosapentaenoic acid and arachidonic acid) PUFAs. This was not the case for the hippocampus or in the liver. There were no effects on plasma lipid levels, and daily monitoring confirmed NL biocompatibility. These results demonstrate that NLs can be used for delivery of PUFAs to the brain. This study opens new research possibilities in the development of preventive as well as therapeutic strategies for age-related neurodegeneration.
Assuntos
Ácidos Graxos Ômega-3/administração & dosagem , Ácidos Graxos Insaturados/sangue , Lecitinas/administração & dosagem , Neurônios/citologia , Salmão/metabolismo , Administração Oral , Animais , Disponibilidade Biológica , Células Cultivadas , Cromatografia Gasosa , Ácidos Docosa-Hexaenoicos/análise , Ácidos Graxos Ômega-3/farmacocinética , Feminino , Hipocampo/química , Lecitinas/farmacocinética , Lipossomos , Fígado/química , Masculino , Camundongos , Nanoestruturas , Neurônios/química , Ácido Oleico/análise , Ácido Palmítico/análise , Tamanho da Partícula , Cultura Primária de Células , RatosRESUMO
SCOPE: Synthetic emulsifiers have recently been shown to promote metabolic syndrome and considerably alter gut microbiota. Yet, data are lacking regarding the effects of natural emulsifiers, such as plant lecithins rich in essential α-linolenic acid (ALA), on gut and metabolic health. METHODS AND RESULTS: For 5 days, male Swiss mice are fed diets containing similar amounts of ALA and 0, 1, 3, or 10% rapeseed lecithin (RL) or 10% soy lecithin (SL). Following an overnight fast, they are force-fed the same oil mixture and euthanized after 90 minutes. The consumption of lecithin significantly increased fecal levels of the Clostridium leptum group (p = 0.0004), regardless of origin or dose, without altering hepatic or intestinal expression of genes of lipid metabolism. 10%-RL increased ALA abundance in plasma triacylglycerols at 90 minutes, reduced cecal bile acid hydrophobicity, and increased their sulfatation, as demonstrated by the increased hepatic RNA expression of Sult2a1 (p = 0.037) and cecal cholic acid-7 sulfate (CA-7S) concentration (p = 0.05) versus 0%-lecithin. CONCLUSION: After only 5 days, nutritional doses of RL and SL modified gut bacteria in mice, by specifically increasing C. leptum group. RL also increased postprandial ALA abundance and induced beneficial modifications of the bile acid profile. ALA-rich lecithins, especially RL, may then appear as promising natural emulsifiers.
Assuntos
Ácidos e Sais Biliares/análise , Brassica napus , Microbioma Gastrointestinal/efeitos dos fármacos , Glycine max , Lecitinas/administração & dosagem , Metabolismo dos Lipídeos/efeitos dos fármacos , Animais , Ácidos e Sais Biliares/metabolismo , Lipídeos/sangue , Masculino , Camundongos , Período Pós-Prandial/fisiologia , Ácido alfa-Linolênico/administração & dosagemRESUMO
Deoiled soy lecithin is a feed additive enriched in phospholipids. Our study evaluated the effects of dietary deoiled soy lecithin supplementation on (1) milk production and composition, (2) plasma and milk fatty acid (FA) content and yield, and (3) apparent FA digestibility and absorption in lactating dairy cows fed fractionated palm fat. In a split-plot Latin square design, 16 Holstein cows (160 ± 7 days in milk; 3.6 ± 1.2 parity) were randomly allocated to a main plot receiving a corn silage and alfalfa haylage-based diet with palm fat containing either moderate (MPA) or high palmitic acid (HPA) content at 1.75% of ration dry matter (72 or 99% palmitic acid, respectively; n = 8/palm fat diet). On each palm fat diet, deoiled soy lecithin was top-dressed at 0, 0.12, 0.24, or 0.36% of ration dry matter in a replicated 4 × 4 Latin square design. Following a 14-d covariate period, lecithin supplementation spanned 14 d, with milk and blood collected during the final 3 d. Milk composition and pooled plasma markers were measured. The statistical model included the fixed effects of palm fat type, lecithin dose, period, and the interaction between palm fat type and lecithin dose. The random effect of cow nested within palm fat group was also included. Lecithin linearly decreased dry matter intake. In cows fed HPA, lecithin feeding reduced milk fat content and tended to decrease milk fat yield. Although no changes in milk yield were observed, a quadratic reduction in 3.5% fat-corrected milk was observed with increasing lecithin dose. Lecithin linearly increased energy-corrected milk efficiency in cows fed MPA. Lecithin supplementation also decreased milk urea nitrogen, relative to unsupplemented cows. The proportion of 16-carbon FA in milk fat decreased linearly with lecithin dose, whereas 18-carbon FA increased linearly. Lecithin reduced de novo FA (<16-carbon) content and tended to increase preformed FA (>16-carbon) content in a linear manner. Compared with MPA, HPA diets reduced apparent total and 16-carbon FA digestibility and absorption. Deoiled soy lecithin feeding did not modify FA digestibility or absorption. Our observations suggest that soy lecithin feeding modifies rumen digestion to reduce dry matter intake and change milk composition.
Assuntos
Bovinos/metabolismo , Digestão/efeitos dos fármacos , Ácidos Graxos/metabolismo , Lactação/efeitos dos fármacos , Lecitinas/administração & dosagem , Ração Animal/análise , Animais , Dieta/veterinária , Suplementos Nutricionais , Ácidos Graxos/análise , Feminino , Leite/química , Leite/efeitos dos fármacos , Ácido Palmítico/administração & dosagem , Paridade , GravidezRESUMO
Dietary lecithin is a source of choline. Our objective was to evaluate the effects of dietary deoiled soy lecithin feeding on circulating choline, choline metabolites, and the plasma phospholipid profile in lactating dairy cows fed fractionated palm fatty acids. In a split-plot Latin square design, 16 Holstein cows (160 ± 7 d in milk; 3.6 ± 1.2 parity) were randomly allocated to a main plot receiving a corn silage and alfalfa haylage-based diet with palm fat containing either moderate or high palmitic acid content at 1.75% of ration dry matter (moderate and high palmitic acid containing 72 or 99% palmitic acid in fat supplement, respectively; n = 8/palm fat diet). Within each palm fat group, deoiled soy lecithin was top-dressed at 0, 0.12, 0.24, or 0.36% of ration dry matter in a replicated 4 × 4 Latin square design with 14-d experimental periods. A 14-d covariate period was used to acclimate cows to palm fat feeding without lecithin supplementation. Blood sampling occurred during the final 3 d of each experimental period. Plasma choline and choline metabolites were quantified using liquid chromatography and mass spectrometry. Plasma phospholipids were profiled using time-of-flight mass spectrometry. Whereas no effects of treatments were detected for plasma choline or methionine, lecithin feeding increased the plasma concentrations of choline metabolites trimethylamine N-oxide and dimethylglycine (24 and 11%, respectively). Plasma phosphatidylcholine (PC) and sphingomyelin (SM) concentrations increased with deoiled lecithin feeding (e.g., PC 16:0/22:6 and SM d18:1/18:3). Lecithin supplementation also increased plasma lysophosphatidylcholine (LPC) concentrations (e.g., LPC 18:0) while reducing plasma phosphatidylethanolamine (PE) concentrations (e.g., PE 16:0/20:5). Although increases in microbial-derived trimethylamine N-oxide suggest gastrointestinal lecithin degradation, elevations in plasma dimethylglycine, PC, LPC, and SM suggest that choline availability was improved by lecithin feeding in cows, thus supporting enhanced endogenous phospholipid synthesis.
Assuntos
Bovinos/sangue , Colina/sangue , Glycine max/química , Lecitinas/administração & dosagem , Ácido Palmítico/administração & dosagem , Fosfolipídeos/sangue , Animais , Dieta/veterinária , Suplementos Nutricionais , Feminino , Lactação , Medicago sativa , Gravidez , Silagem/análise , Zea maysRESUMO
In this study, the microbiological, physicochemical, and flavor changes of turbot (Scophthalmus maximus) coated with a composite active coating of locust bean gum (LBG) and sodium alginate (SA) supplemented with daphnetin emulsions (0.16, 0.32, 0.64 mg·mL-1) were determined during 18 days of refrigerated storage (4 ± 1 °C). Results showed that LBG-SA coatings containing 0.32 mg·mL-1 daphnetin emulsions could significantly lower the total viable count (TVC), psychrophiles, Pseudomonas spp. and H2S-producing bacteria counts, and inhibit the productions of off-flavor compounds including the total volatile basic nitrogen (TVB-N), trimethylamine (TMA) and ATP-related compounds. 32 volatile compounds were identified by solid phase microextraction combined with gas chromatography-mass spectrometer method (SPME-GC/MS) during refrigerated storage and the treated turbot samples significantly lowered the relative content of fishy flavor compounds. Further, the LBG-SA coatings containing daphnetin could also delay the myofibril degradation of the turbot samples. These results indicated that the LBG-SA coatings with 0.32 mg·mL-1 daphnetin were a potential alternative way to improve the quality of turbot during refrigerated storage.
Assuntos
Alginatos/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Criopreservação , Linguados , Conservação de Alimentos , Conservantes de Alimentos/farmacologia , Galactanos/farmacologia , Mananas/farmacologia , Carne , Gomas Vegetais/farmacologia , Umbeliferonas/farmacologia , Alginatos/administração & dosagem , Animais , Antibacterianos/administração & dosagem , Antioxidantes/administração & dosagem , Carga Bacteriana , Emulsões , Linguados/microbiologia , Aromatizantes/administração & dosagem , Aromatizantes/farmacologia , Microbiologia de Alimentos , Conservantes de Alimentos/administração & dosagem , Galactanos/administração & dosagem , Cromatografia Gasosa-Espectrometria de Massas , Lecitinas/administração & dosagem , Lecitinas/farmacologia , Mananas/administração & dosagem , Carne/microbiologia , Metilaminas/análise , Miofibrilas/efeitos dos fármacos , Nitrogênio/análise , Gomas Vegetais/administração & dosagem , Pseudomonas/efeitos dos fármacos , Umbeliferonas/administração & dosagem , Compostos Orgânicos Voláteis/análiseRESUMO
A 70-day experiment was carried out to assess the effect of different levels (0, 1 and 2%) of soy lecithin in the diet on growth, survival, antioxidant defense markers, immune gene expression and thermal tolerance limits of golden mahseer, Tor putitora fry. Percentage weight gain, specific growth rate (SGR %) and survival of mahseer fed lecithin supplemented diets were not significantly different from those of the control group. Also, the mRNA expression levels of different immune related genes such as tnfα, il-1ß, il-10, complement-3, interferon-gamma (ifnγ) and tlr4 were unaffected by dietary lecithin supplementation. Nevertheless, superoxide dismutase (SOD) activity was significantly greater in the lecithin-fed groups than the control fish. The glutathione-S-transferase (GST) activity was exceptionally high in the 2% lecithin supplemented group compared to the rest two groups. This increase in antioxidant status with dietary lecithin supplementation, however, was not reflected in the whole body malonaldehyde (MDA) levels, as it did not vary significantly among the dietary groups. Importantly, dietary inclusion of soy lecithin significantly increased upper thermal tolerance limits as evidenced by higher CTmax and LTmax values. Likewise, golden mahseer fry fed with lecithin supplemented diets (both 1 and 2%) registered significantly lower critical and lethal thermal minimum (CTmin and LTmin) values than the control group, indicating higher cold tolerance capacity. Our results thus demonstrate that the dietary inclusion of soy lecithin could enhance the upper and lower thermal tolerance limits and antioxidant status of golden mahseer fry and failed to enhance immune related gene expression.
Assuntos
Antioxidantes/metabolismo , Cyprinidae/imunologia , Imunidade Inata/genética , Lecitinas/metabolismo , Termotolerância , Ração Animal/análise , Animais , Cyprinidae/genética , Dieta/veterinária , Suplementos Nutricionais/análise , Relação Dose-Resposta a Droga , Espécies em Perigo de Extinção , Imunidade Inata/efeitos dos fármacos , Lecitinas/administração & dosagem , Distribuição Aleatória , Glycine max , Termotolerância/efeitos dos fármacosRESUMO
18-α-Glycyrrhetinic acid (GA) is a bioactive compound extracted from licorice that exhibits many biological and pharmacological effects such as anti-inflammatory and antioxidant activities on the skin. However, its lipophilic nature results in poor bioavailability that limits clinical applications. Liposomes, presenting the ability to carry both hydrophobic and hydrophilic payloads and a good cytocompatibility, are effective to overcome this barrier. Furthermore, the addition of permeation enhancers such as ethanol into liposomal formulations helps the diffusion of these systems through the skin barrier. Here, we aimed to formulate GA-loaded ethanolic liposomes, using a natural soybean lecithin via a microfluidic approach. Using a fused deposition modeling (FDM) 3D printer we customized a microfluidic chip, and manufactured vesicles that presented spherical shape with a size of 202 ± 5.2 nm, a narrow size distribution and a good stability over a period of 30 days. After reaching a drug encapsulation efficiency of 63.15 ± 2.2%, liposomes were evaluated for their cytocompatibility and skin permeation potentiality after hydrogelation using xanthan gum. The in vitro release and permeation studies were performed using Franz diffusion cells comparing two different media and three synthetic membranes including a polymeric skin-mimicking membrane. The selected formulation presented no cytotoxicity and an increased permeation compared to GA saturated hydrogel. It could perform therapeutically better effects than conventional formulations containing free GA, as prolonged and controlled release topical dosage forms, which may lead to improved efficiency and better patient compliance.
Assuntos
Sistemas de Liberação de Medicamentos , Etanol/química , Ácido Glicirretínico/química , Lecitinas/química , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Liberação Controlada de Fármacos , Etanol/administração & dosagem , Ácido Glicirretínico/administração & dosagem , Humanos , Lecitinas/administração & dosagem , Lipossomos , Microfluídica , Polissacarídeos Bacterianos/química , Impressão Tridimensional , Pele/metabolismo , Absorção Cutânea , Tecnologia FarmacêuticaRESUMO
Surfactants are important ingredients in pharmaceutical and cosmetic formulations, as in creams, shampoos or shower gels. As conventional emulsifiers such as sodium dodecyl sulfate (SDS) have fallen into disrepute due to their skin irritation potential, the naturally occurring lecithins are being investigated as a potential alternative. Thus, lecithin-based nanoemulsions with and without the drug curcumin, known for its wound healing properties, were produced and characterised in terms of their particle size, polydispersity index (PDI) and zeta potential and compared to SDS-based formulations. In vitro toxicity of the produced blank nanoemulsions was assessed with primary human keratinocytes and fibroblasts using two different cell viability assays (BrdU and EZ4U). Further, we investigated the penetration profiles of the deployed surfactants and oil components using combined ATR-FTIR/tape stripping experiments and confirmed the ability of the lecithin-based nanoemulsions to deliver curcumin into the stratum corneum in tape stripping-UV/Vis experiments. All manufactured nanoemulsions showed droplet sizes under 250 nm with satisfying PDI and zeta potential values. Viability assays with human skin cells clearly indicated that lecithin-based nanoemulsions were superior to SDS-based formulations. ATR-FTIR tests showed that lecithin and oil components remained in the superficial layers of the stratum corneum, suggesting a low risk for skin irritation. Ex vivo tape stripping experiments revealed that the kind of oil used in the nanoemulsion seemed to influence the depth of curcumin penetration into the stratum corneum.
Assuntos
Bromodesoxiuridina/metabolismo , Curcumina/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Lecitinas/metabolismo , Absorção Cutânea/fisiologia , Tensoativos/metabolismo , Adulto , Idoso , Animais , Bromodesoxiuridina/administração & dosagem , Bromodesoxiuridina/química , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Curcumina/administração & dosagem , Curcumina/química , Citotoxinas/administração & dosagem , Citotoxinas/química , Citotoxinas/metabolismo , Emulsões/administração & dosagem , Emulsões/química , Emulsões/metabolismo , Feminino , Aromatizantes/administração & dosagem , Aromatizantes/química , Aromatizantes/metabolismo , Humanos , Lecitinas/administração & dosagem , Lecitinas/química , Masculino , Pessoa de Meia-Idade , Nanopartículas/administração & dosagem , Nanopartículas/química , Nanopartículas/metabolismo , Absorção Cutânea/efeitos dos fármacos , Tensoativos/administração & dosagem , Tensoativos/química , Suínos , Fatores de Tempo , Adulto JovemRESUMO
Vegetable lecithins, widely used in the food industry as emulsifiers, are a mixture of naturally occurring lipids containing more than 50% of phospholipids (PL). PL exert numerous important physiological effects. Their amphiphilic nature notably enables them to stabilise endogenous lipid droplets, conferring them an important role in lipoprotein transport, functionality and metabolism. In addition, beneficial effects of dietary lecithin on metabolic disorders have been reported since the 1990s. This review attempts to summarize the effects of various vegetable lecithins on lipid and lipoprotein metabolism, as well as their potential application in the treatment of dyslipidemia associated with metabolic disorders. Despite controversial data concerning the impact of vegetable lecithins on lipid digestion and intestinal absorption, the beneficial effect of lecithin supplementation on plasma and hepatic lipoprotein and cholesterol levels is unequivocal. This is especially true in hyperlipidemic patients. Furthermore, the immense compositional diversity of vegetable lecithins endows them with a vast range of biochemical and biological properties, which remain to be explored in detail. Data on the effects of vegetable lecithins alternative to soybean, both as supplements and as ingredients in different foods, is undoubtedly lacking. Given the exponential demand for vegetable products alternative to those of animal origin, it is of primordial importance that future research is undertaken in order to elucidate the mechanisms by which individual fatty acids and PL from various vegetable lecithins modulate lipid metabolism. The extent to which they may influence parameters associated with metabolic disorders, such as intestinal integrity, low-grade inflammation and gut microbiota must also be assessed.
Assuntos
Doenças Cardiovasculares/prevenção & controle , Aditivos Alimentares/metabolismo , Lecitinas/metabolismo , Transtornos do Metabolismo dos Lipídeos/prevenção & controle , Metabolismo dos Lipídeos/efeitos dos fármacos , Tecido Adiposo/efeitos dos fármacos , Tecido Adiposo/metabolismo , Animais , Doenças Cardiovasculares/metabolismo , Doenças Cardiovasculares/patologia , Suplementos Nutricionais/análise , Aditivos Alimentares/administração & dosagem , Aditivos Alimentares/química , Aditivos Alimentares/isolamento & purificação , Microbioma Gastrointestinal/fisiologia , Humanos , Absorção Intestinal/fisiologia , Lecitinas/administração & dosagem , Lecitinas/química , Lecitinas/isolamento & purificação , Gotículas Lipídicas/química , Gotículas Lipídicas/metabolismo , Transtornos do Metabolismo dos Lipídeos/metabolismo , Transtornos do Metabolismo dos Lipídeos/patologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Verduras/químicaRESUMO
A total of 270 one-d-old Ross 308 broiler chicks were randomly allotted to 9 experimental diets (3 replicates of 10 birds each), including three types of supplemental lipotropic factors (control, 0.1% or 0.2% choline and 0.5% or 1% lecithin) in a 3 × 3 factorial arrangement. Supplementation of lecithin improved FCR values during 1-21 days of age. Although no differences were noticed for mortality index among different diets, the group supplemented with a combination of choline (0.1) and lecithin (0.5) showed the highest (P < 0.0001) production index. Choline (0.1% or 0.2%) significantly decreased serum total cholesterol by 11%, triglycerides by 21%, low-density lipoprotein (LDL) by 20%, and very low-density lipoprotein (VLDL) by 20%, while increased the glucose and high-density lipoprotein (HDL) values by 11% and 6%, respectively. On the other hand, lecithin significantly increased glucose, total cholesterol, triglycerides, HDL, LDL and VLDL by 4%, 9%, 7%, 24%, and 25%, respectively. Choline supplementation decreased the aspartate amino transferase (AST), alanine amino transferase (ALT), and alkaline phosphatase (AP); however, the lecithin addition increased their respective proportions. This study concluded that the combinations of 0.1% choline and 0.5% lecithin is the best among all other treatments because of the highest production index and least mortality.
Assuntos
Gordura Abdominal/efeitos dos fármacos , Ração Animal , Galinhas , Colina , Lecitinas , Animais , Galinhas/crescimento & desenvolvimento , Galinhas/fisiologia , Colesterol/sangue , Colina/administração & dosagem , Colina/farmacologia , Dieta/veterinária , Enzimas/sangue , Lecitinas/administração & dosagem , Lecitinas/farmacologia , Masculino , Estresse Fisiológico/efeitos dos fármacosRESUMO
Surfactants have been used as a tool to improve the properties of polymeric nanoparticles (NPs) and to increase the rate of hydrophobic drug release by means of these nanoparticles. In this context, this study evaluated the effect of lecithin on the characteristics of chitosan (CHI) and chondroitin sulfate (CS) nanoparticles, when applied in curcumin (Curc) release. CHI/CS NPs and CHI/CS/Lecithin NPs were prepared by the ionic gelation method, both as standards and containing curcumin. Simultaneous conductimetric and potentiometric titrations were employed to optimize the interaction between the polymers. NPs with hydrodynamic diameter of â¼130â¯nm and zeta potential of +60â¯mV were obtained and characterized by HRTEM; their pore size and surface area were also analyzed by BET method, DLS, FTIR, XPS, and fluorescence spectroscopy techniques to assess morphological and surface properties, stability and interaction between polymers and to quantify the loading of drugs. The final characteristics of NPs were directly influenced by lecithin addition, exhibiting enhanced encapsulation efficiency of curcumin (131.8⯵g curcumin per mg CHI/CS/Lecithin/Curc NPs). The release of curcumin occurred gradually through a two-stage process: diffusion-controlled dissolution and release of curcumin controlled by dissolution of the polymer. However, the release of curcumin in buffer solution at pH 7.4 was achieved faster in CHI/CS/Lecithin/Curc NPs than in CHI/CS/Curc NPs. in vitro cytotoxic activity evaluation of the curcumin was determined by the MTT assay, observing that free curcumin and curcumin nanoencapsulated in CHI/CS/Curc and CHI/CS/Lecithin/Curc NPs reduced the viability of MCF-7 cells in the 72â¯h period (by 28.4, 36.0 and 30.7%, Pâ¯<â¯0.0001, respectively). These results indicate that CHI/CS/Lecithin NPs have more appropriate characteristics for encapsulation of curcumin.
Assuntos
Quitosana/química , Sulfatos de Condroitina/química , Curcumina/química , Lecitinas/química , Nanopartículas/química , Sobrevivência Celular/efeitos dos fármacos , Quitosana/administração & dosagem , Sulfatos de Condroitina/administração & dosagem , Curcumina/administração & dosagem , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/química , Liberação Controlada de Fármacos , Humanos , Lecitinas/administração & dosagem , Células MCF-7 , Nanopartículas/administração & dosagemRESUMO
Alcoholic liver disease (ALD) is associated with significant morbidity and mortality globally. In this study, the soybean lecithin-gallic acid complex was synthesized, and its physicochemical properties were evaluated, which confirmed the complex formation. Compared with the free state of the drug, gallic acid exhibited significantly different physicochemical properties after it was complexed with soybean lecithin. To clarify the binding mode between two monomers, computational investigation was performed. From the computational data, we deduced the structure of the compound and predicted that it has a high affinity for human phosphatidylcholine transfer protein and exhibits strong pharmacological activities in vivo. The complex not only effectively ameliorated liver fibrosis, lipid peroxidation, and oxidative stress, but also reduced liver iron overload in a mouse ALD model induced by alcohol (p < 0.05). Additionally, it regulated iron metabolism by inhibiting TfR1 expression (p < 0.05) and promoting hepcidin expression (p < 0.05). These results suggest that the soybean lecithin-gallic acid complex ameliorates hepatic damage and iron overload induced by alcohol and exert hepatoprotective effects.
Assuntos
Ácido Gálico/administração & dosagem , Sobrecarga de Ferro/tratamento farmacológico , Lecitinas/administração & dosagem , Hepatopatias Alcoólicas/tratamento farmacológico , Animais , Biologia Computacional , Ácido Gálico/química , Hepcidinas/genética , Hepcidinas/metabolismo , Humanos , Ferro/metabolismo , Sobrecarga de Ferro/genética , Sobrecarga de Ferro/metabolismo , Lecitinas/química , Fígado/metabolismo , Hepatopatias Alcoólicas/genética , Hepatopatias Alcoólicas/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Receptores da Transferrina/genética , Receptores da Transferrina/metabolismo , Glycine max/químicaRESUMO
Nanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare the influence of different inner structure of tacrolimus-loaded NLC and corresponding NE on physicochemical characteristics, stability, entrapment efficiency, in vitro drug release and overall skin performance. Solid/liquid lipid ratio, total amount of lipids, homogenization pressure and cooling after the preparation were identified as critical variables in NLC development. Moreover, tacrolimus-loaded NLC emerged as more stabile carrier than NE. Differential stripping performed on porcine ear skin revealed significantly higher tacrolimus amount in stratum corneum from nanocarriers compared to referent ointment (Protopic®). Similarly the highest amount of tacrolimus in hair follicles was obtained using NLC (268.54⯱â¯92.38â¯ng/cm2), followed by NE (128.17⯱â¯48.87â¯ng/cm2) and Protopic® (77.61⯱â¯43.25â¯ng/cm2). Contrary, the highest permeation rate through full-thickness porcine ear skin was observed for Protopic®, implying that the selection of experimental setup is critical for reliable skin performance assessment. Overall, developed NLC could be suggested as promising carrier in a form of lotion for tacrolimus dermal delivery.
Assuntos
Portadores de Fármacos/administração & dosagem , Imunossupressores/administração & dosagem , Lecitinas/administração & dosagem , Nanoestruturas/administração & dosagem , Tacrolimo/administração & dosagem , Administração Cutânea , Animais , Caprilatos/administração & dosagem , Caprilatos/química , Portadores de Fármacos/química , Composição de Medicamentos , Liberação Controlada de Fármacos , Emulsões , Imunossupressores/química , Lecitinas/química , Lipídeos/administração & dosagem , Lipídeos/química , Nanoestruturas/química , Pomadas , Propilenoglicóis/administração & dosagem , Propilenoglicóis/química , Pele/metabolismo , Absorção Cutânea , Suínos , Tacrolimo/químicaRESUMO
Rapamycin as a novel macrolide immunosuppressive agent has been commonly used in organ transplantation owing to its stronger immunosuppressive effect, non-nephrotoxicity and lower side effect. However its drawbacks of low bioavailability and big individual difference remain to be improved in clinical application. Here rapamycin loaded TPGS-Lecithins-Zein nanoparticles (RTLZ-NPs) with core-shell structure were prepared by the phase separation method. The RTLZ-NPs were approximately 190.3â¯nm in size, with PDI and zeta potential about 0.256 and -19.71â¯mV respectively. Drug entrapment and loading achieved were about 86.64 and 25.73% respectively. Meanwhile RTLZ-NPs exhibited favorable enzymolysis resistance abilities in gastrointestinal environments and enhanced uptake in Caco-2 cells. The optimum absorption sites of rapamycin in the intestine were duodenum and jejunum as single-pass intestinal perfusion assay. Upon also considering the results of Caco-2 cell assay, it could be speculated that the transport of rapamycin in vivo involved active transport as well as P-glycoprotein (P-gp) based efflux. Finally, the relative oral bioavailability of RTLZ-NPS was 4.33 fold higher than free rapamycin in SD rat. Altogether the designed nanoparticles can be an efficient oral delivery strategy for rapamycin analogues to prevent the attacks from destructive enzymes, reduce cell efflux, increase cell uptake, and then enhance the oral bioavailability.
Assuntos
Portadores de Fármacos/administração & dosagem , Lecitinas/administração & dosagem , Nanopartículas/administração & dosagem , Sirolimo/administração & dosagem , Vitamina E/administração & dosagem , Zeína/administração & dosagem , Administração Oral , Animais , Células CACO-2 , Sobrevivência Celular/efeitos dos fármacos , Cumarínicos/administração & dosagem , Cumarínicos/química , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Liberação Controlada de Fármacos , Humanos , Absorção Intestinal/efeitos dos fármacos , Lecitinas/química , Lecitinas/farmacocinética , Masculino , Nanopartículas/química , Ratos Sprague-Dawley , Sirolimo/química , Sirolimo/farmacocinética , Tiazóis/administração & dosagem , Tiazóis/química , Vitamina E/química , Vitamina E/farmacocinética , Zeína/química , Zeína/farmacocinéticaRESUMO
Lipids play multiple roles in preserving neuronal function and synaptic plasticity, and polyunsaturated fatty acids (PUFAs) have been of particular interest in optimizing synaptic membrane organization and function. We developed a green-based methodology to prepare nanoliposomes (NL) from lecithin that was extracted from fish head by-products. These NL range between 100-120 nm in diameter, with an n-3/n-6 fatty acid ratio of 8.88. The high content of n-3 PUFA (46.3% of total fatty acid content) and docosahexanoic acid (26%) in these NL represented a means for enrichment of neuronal membranes that are potentially beneficial for neuronal growth and synaptogenesis. To test this, the primary cultures of rat embryo cortical neurons were incubated with NL on day 3 post-culture for 24 h, followed by immunoblots or immunofluorescence to evaluate the NL effects on synaptogenesis, axonal growth, and dendrite formation. The results revealed that NL-treated cells displayed a level of neurite outgrowth and arborization on day 4 that was similar to those of untreated cells on day 5 and 6, suggesting accelerated synapse formation and neuronal development in the presence of NL. We propose that fish-derived NL, by virtue of their n-3 PUFA profile and neurotrophic effects, represent a new innovative bioactive vector for developing preventive or curative treatments for neurodegenerative diseases.
Assuntos
Ácidos Graxos Ômega-3/administração & dosagem , Lecitinas/administração & dosagem , Neurônios/efeitos dos fármacos , Salmão , Sinapses/efeitos dos fármacos , Animais , Células Cultivadas , Córtex Cerebral/citologia , Composição de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos , Embrião de Mamíferos , Química Verde/métodos , Lipossomos , Nanopartículas/química , Plasticidade Neuronal/efeitos dos fármacos , Cultura Primária de Células , RatosRESUMO
Two experiments were conducted to evaluate the use of crude soybean lecithin (L) as an alternative energy source in broiler feeding and to study its influence on performance, fatty acid (FA) digestibility between 9 to 11 D and 36 to 37 D, feed AME content, and the FA profile of the abdominal fat pad (AFP). A basal diet was supplemented at 3% with soybean oil (S; experiment 1) or a monounsaturated vegetable acid oil (A; experiment 2) and increasing amounts of L (1, 2, and 3%) were included in replacement. The inclusion of L did not modify performance results (P > 0.05). In starter diets, the replacement of S by L reduced feed AME content (P < 0.001) and lowered PUFA digestibility (P = 0.028), whereas in the grower-finisher phase, a blend of 2% of S and 1% of L did not modify feed AME content or FA digestibility. When L was included instead of A, no effects on feed AME value and total FA digestibility (P > 0.05) were shown in the starter phase, whereas in grower-finisher diets, a blending of 2% of A and 1% of L enhanced feed AME content (P < 0.001) and total FA digestibility (P = 0.001). The FA profile of the AFP reflected the FA composition of the diets. Crude soybean lecithin represents an alternative energy source for broiler chickens, and it can be used in growing-finishing diets in replacement of 1% S. The best option to include both alternative fats (L and A) was 2% of L with 1% of A in starter diets and 1% of L with 2% of A in grower-finisher diets because they showed positive synergic effects. The results suggest that dietary FA profile have a bigger impact on the AFP saturation degree than the different dietary lipid molecular structures.
Assuntos
Galinhas/fisiologia , Digestão/efeitos dos fármacos , Ácidos Graxos Monoinsaturados/metabolismo , Glycine max/química , Lecitinas/metabolismo , Óleo de Soja/metabolismo , Tecido Adiposo/química , Ração Animal/análise , Fenômenos Fisiológicos da Nutrição Animal/efeitos dos fármacos , Animais , Dieta/veterinária , Suplementos Nutricionais/análise , Relação Dose-Resposta a Droga , Metabolismo Energético/efeitos dos fármacos , Feminino , Lecitinas/administração & dosagem , Óleos de Plantas/metabolismo , Distribuição Aleatória , Óleo de Soja/administração & dosagemRESUMO
Skin carcinogenesis is a common malignancy affecting humans worldwide, which could benefit from nutraceuticals as a solution to the drawbacks of conventional skin cancer treatment. (-)-epigallocatechin-3-gallate (EGCG) is a promising nutraceutical in this regard; however, it suffers chemical instability and low bioavailability resulting in inefficient delivery. Therefore, EGCG encapsulation in ultradeformable colloidal vesicular systems, namely: penetration enhancer-containing vesicles (PEVs), ethosomes and transethosomes (TEs) for topical administration has been attempted in this study to overcome the problems associated with the use of free EGCG. The prepared vesicles were characterized for their entrapment efficiency, TEM visualization, chemical compatibility, antioxidant properties, ex-vivo skin deposition, photodegradation and physical stability after storage. Most of the prepared vesicles exhibited reasonable skin deposition and preservation of the inherent antioxidant properties of EGCG with good physical stability. EGCG-loaded PEVs and TEs exhibited an inhibitory effect on epidermoid carcinoma cell line (A431) in addition to reduced tumor sizes in mice, confirmed with histopathological analysis and biochemical quantification of skin oxidative stress biomarkers; glutathione, superoxide dismutase and catalase, as well as lipid peroxidation. EGCG PEVs succeeded in offering an effective delivery system targeting skin cancer, which is worthy of further experimentation.
Assuntos
Catequina/análogos & derivados , Portadores de Fármacos/administração & dosagem , Neoplasias Cutâneas/tratamento farmacológico , Neoplasias Cutâneas/prevenção & controle , Animais , Catequina/administração & dosagem , Linhagem Celular Tumoral , Coloides , Humanos , Lecitinas/administração & dosagem , Masculino , Camundongos Endogâmicos BALB C , Camundongos Nus , Polissorbatos/administração & dosagemRESUMO
Ovaries (O) are specialized tissues that play critical roles in producing oocytes and hormones. The crustacean hepatopancreas (H) is a metabolic organ that plays important functions including absorption, storage of nutrients and vitellogenesis during growth and ovarian development. However, genetic information on the biological functions of the crustacean ovaries and hepatopancreas are limited. This study compared the transcriptome in the ovary and the hepatopancreas of female P. trituberculatus fed two different diets containing 0% (SL0) and 4% soybean lecithin (SL4), respectively during the growth and ovarian maturation stages by Illumina HiSeq4000 sequencer. The differences between ovary and hepatopancreas of P. trituberculatus were also compared at transcriptional level. A total of 55,667 unigenes were obtained with mean length of 962â¯bps across the four treatment groups (SL0_O, SL4_O, SL0_H and SL4_H). In ovary, there were 257 differentially expressed genes (DEGs) between SL0_O and SL4_O, with 145 down- and 112 up-regulated genes in the SL4_O group. Candidate genes involved in ovarian development were detected in SL4_H group. In hepatopancreas, 146 DEGs were found between SL0_H and SL4_H, including 43 down- and 103 up-regulated genes in the SL4_H group. The specific DEGs were mainly involved with lipid related metabolism pathways, including fat digestion and absorption, PPAR signaling pathway and insulin resistance. 14,725 DEGs were found in the comparison between SL0_O and SL4_H, including 7250 up- and 7475 down-regulated genes in the SL4_H group. The specific DEGs were mainly involved with lipid (fat digestion and absorption, linoleic acid metabolism), hormone (steroid hormone biosynthesis, ovarian steroidogenesis, etc), and amino acid (phenylalanine metabolism, arginine biosynthesis, tyrosine) related metabolism pathways. Crabs fed the SL4 diet exhibited higher gene expression of cryptocyanin 1 (cc1), cryptocyanin 2 (cc2) and neuroparsin 1 (np1) in hepatopancreas and ovarian than those fed the SL0 diet, however, crab fed SL4 diet showed higher gene expression of fatty acid-binding protein 1 (fabp1), vitellogenin (vtg) and Delta-6 desaturase-like protein (fadsd6) in hepatopancreas than those fed the SL0 diet. Moreover, crabs fed the SL0 diet had lower gene expression of vtg, extracellular copperzinc superoxide dismutase (cuznsod) and estrogen sulfotransferase (ests) in ovary compared to those fed the diet containing 4% soybean lecithin. These results might provide important clues with respect to elucidating the molecular mechanisms underlying the regulation of phospholipid on the gonadal development and lipid metabolism of P. trituberculatus.
Assuntos
Braquiúros/genética , Dieta , Glycine max/química , Hepatopâncreas/metabolismo , Lecitinas/administração & dosagem , Ovário/metabolismo , Transcriptoma , Animais , Feminino , Metabolismo dos LipídeosRESUMO
As constituents of cellular membranes, lecithins feature high biocompatibility and great emulsifying properties due to their amphiphilicity. Additionally, there are expectations that these naturally occurring emulsifying agents can replace other skin damaging emulsifiers like sodium dodecyl sulfate or sodium laureth sulfate. However, cytotoxicity data of lecithin-based formulations on primary human skin cells are scarce. Thus, we developed nanoemulsions with different kinds of surfactants (amphoteric, anionic and non-ionic), studied the skin permeation of a model drug from this formulations employing Franz-type diffusion cells and monitored their cytotoxicity potential on primary human keratinocytes and fibroblasts using a cell proliferation assay. The skin diffusion studies demonstrated that the amphoteric lecithin-based emulsifiers were superior to non-ionic surfactants in terms of skin permeation, but inferior to anionic emulsifiers. Further, we found that the nanoemulsions containing the amphoteric lecithins as emulsifying agents lead to significantly higher viability rates of both epidermal keratinocytes and dermal fibroblasts than the investigated anionic and non-ionic surfactants. This renders them a promising alternative to conventional emulsifiers used in daily products.
Assuntos
Emulsificantes/administração & dosagem , Fibroblastos/efeitos dos fármacos , Queratinócitos/efeitos dos fármacos , Lecitinas/administração & dosagem , Nanopartículas/administração & dosagem , Pele/metabolismo , Adulto , Idoso , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Emulsões , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pele/citologia , Absorção Cutânea , Suínos , Adulto JovemRESUMO
A feeding experiment was conducted to evaluate the effects of dietary soybean lecithin (SBL) supplementation on performance, hemato-immunological parameters, lipid biochemistry, antioxidant status, digestive enzymes activity and intestinal histomorphometry of Caspian brown trout, Salmo trutta caspius in the pre-spawning stage. The basal diet was supplemented with 0% (control), 3%, 6%, 9% and 12% of SBL to obtain five experimental diets. Fish with an average weight of 350⯱â¯10â¯g were randomly distributed among five experimental groups and fed for 90 days. Dietary SBL resulted in better performance including specific growth rate (SGR), weight gain (WG) and feed conversion ratio (FCR) (pâ¯<â¯0.05). Among the different hemato-immunological parameters, white blood cell counts (WBC), lysozyme, alternative complement activity (ACH50) and total immunoglobulin (IgM) content of serum were significantly increased with dietary SBL inclusion (pâ¯<â¯0.05). For antioxidant enzymes, glutathione S-transferase (GST) and catalase (CAT) showed significant differences among various experimental diets (pâ¯<â¯0.05). Furthermore, digestive enzymes activity including alkaline protease, lipase and amylase were increased in those fish received SBL supplemented diets (pâ¯<â¯0.05). Our results revealed that the dietary SBL improved some physiological responses of the fish and indicate 6-9% dietary SBL supplementation would improve the physiological competence of the pre-spawning Caspian brown trout breeders.