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1.
Foods ; 12(13)2023 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-37444270

RESUMO

Curcumin is a polyphenolic compound that has been widely investigated for its health benefits. However, the clinical relevance of curcumin is limited due to its low water solubility and inefficient absorption. Therefore, curcumin is often encapsulated in nanocarriers to improve its delivery and function. In this study, composite nanoparticles composed of stearic acid-modified chitosan (SA-CS) and sodium caseinate (NaCas) were formed using sodium periodate-oxidized dextran with different molecular weights as a crosslinking agent. The effects of oxidized dextran (Odex) with different molecular weights on the composite nanoparticles were compared. The optimal SA-CS/NaCas/Odex composite nanoparticle (NPO) was obtained using an Odex (150 kDa)-to-SA-CS mass ratio of 2:1. Its size, polydispersity index (PDI), and zeta potential (ZP) were 130.2 nm, 0.149, and 25.4 mV, respectively. The particles were highly stable in simulated gastric fluid (SGF) in vitro, and their size and PDI were 172.3 nm and 0.263, respectively. The encapsulation rate of NPO loaded with curcumin (Cur-NPO) was 93% under optimal ultrasonic conditions. Compared with free curcumin, the sustained release of Cur-NPO significantly reduced to 17.9%, and free-radical-scavenging ability improved to 78.7%. In general, the optimal prepared NPO exhibited good GI stability and has potential applications in the formulation of orally bioactive hydrophobic drugs.

2.
ACS Nano ; 17(9): 8586-8597, 2023 05 09.
Artigo em Inglês | MEDLINE | ID: mdl-37125693

RESUMO

Phytochemical nanoencapsulation for nutrient delivery and edible coatings for perishable food preservation are two emerging technologies. Leveraging the strong antimicrobial function of phytochemical nutrients, we propose convergent research to integrate the two technologies by embedding phytochemical-encapsulated nanoparticles in an edible coating on fresh fruits to achieve multiple functions. In particular, we report the study of an edible coating on strawberries that is composited of trans-resveratrol (R)-encapsulated nanoparticles (RNPs) embedded in a chitosan (CS) matrix. The biodegradable and biocompatible RNPs significantly increased the aqueous solubility of R by 150-fold and bioavailability by 3.5-fold after oral administration. Our results demonstrated the abilities of the RNP-embedded CS edible coating to diminish dehydration, prevent nutrient loss, inhibit microbe growth, increase nutraceutical value, preserve strawberry quality, and extend shelf life during storage at both 22 and 4 °C. Such a phytochemical nanoencapsulation-based edible coating is promising for the dual purposes of enhancing nutrient delivery and preserving perishable foods.


Assuntos
Quitosana , Filmes Comestíveis , Fragaria , Resveratrol , Quitosana/farmacologia , Suplementos Nutricionais
3.
Food Funct ; 13(24): 12966-12982, 2022 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-36448414

RESUMO

Metabolic-associated fatty liver disease (MAFLD) is becoming the key factor in causing chronic liver disease all over the world. Sulforaphane (SFN) has been proven to be effective in alleviating many metabolic diseases, such as obesity and type 2 diabetes. In this study, C57BL/6 mice were fed a high-fat diet for 12 weeks to induce MAFLD and given SFN (10 mg per kg bw) daily. Our results showed that SFN not only improved the excessive accumulation of fat in the liver cells but also ameliorated liver and serum inflammatory and antioxidant levels. In addition, SFN can regulate bile-acid metabolism and fatty-acid synthesis by affecting their farnesoid X receptor (FXR)/liver X receptor alpha (LXRα) signaling pathway, ultimately alleviating MAFLD. Our study provides a theoretical basis for the mechanism by which SFN alleviates hepatic steatosis.


Assuntos
Diabetes Mellitus Tipo 2 , Hepatopatia Gordurosa não Alcoólica , Camundongos , Animais , Dieta Hiperlipídica/efeitos adversos , Receptores Citoplasmáticos e Nucleares/genética , Receptores Citoplasmáticos e Nucleares/metabolismo , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Camundongos Endogâmicos C57BL , Fígado/metabolismo , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Hepatopatia Gordurosa não Alcoólica/etiologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Ácidos e Sais Biliares/metabolismo
4.
J Food Biochem ; 46(7): e14145, 2022 07.
Artigo em Inglês | MEDLINE | ID: mdl-35348219

RESUMO

This study aims to explore the hypoglycemic effect of lyophilized broccoli microgreens on type 2 diabetes (T2D) in mice. The experiment lasted 18 weeks, including 1 week of adaptation (normal diet) and 17-week experimental period (high-fat diet). After ingestion of broccoli microgreens, the body weight and glucose homeostasis were improved. Meanwhile, the blood lipid status, antioxidant indexes, and inflammatory factors level were improved. Moreover, the insulin resistance and the pathological changes in mice organs were reversed. In addition, the composition of gut microbiota and the production of propionic acid in intestinal content were improved. Our experiment proved that broccoli microgreens have the ability to regulate T2D and improve symptoms of mice T2D induced by high-fat diet and streptozotocin (STZ). PRACTICAL APPLICATIONS: For years, the functionality of broccoli microgreens has attracted much attention. This article will prove the therapeutic effect of broccoli microgreens on T2D and explain its principle of action in the management of T2D.


Assuntos
Brassica , Diabetes Mellitus Tipo 2 , Microbioma Gastrointestinal , Animais , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/farmacologia , Lipídeos , Camundongos , Camundongos Endogâmicos C57BL
5.
J Food Biochem ; 45(12): e13991, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34778991

RESUMO

L-arabinose is a good and healthy food additive. This study was conducted to investigate the effect of L-arabinose in a mouse model of type 2 diabetes mellitus (T2DM) induced by exposure to a high-fat diet (HFD) and streptozotocin (STZ). The model mice received L-arabinose at 20 and 60 mg (kg body weight [bw])-1 d-1 , metformin at 300 mg (kg bw)-1 d-1 (positive control) or sterile water (control) via oral gavage. Compared with the model group, mice treated with L-arabinose exhibited attenuated symptoms of diabetes mellitus, including a slower rate of body weight loss, increased homeostasis model assessment of ß-cell function index levels, decreased blood glucose, alleviation of steatosis, and repair of pancreatic islet cells. L-arabinose also exerted an anti-inflammatory effect and partially mitigated dyslipidemia. A 16S-rRNA sequence analysis of the gut microbiota revealed that at the phylum level, treatment with L-arabinose significantly reduced the ratio of Firmicutes to Bacteroidetes due to a decreased relative abundance of Firmicutes; at the genus level, it reversed the increase in the relative abundance of Allobaculum and the decrease abundance of Oscillospira caused by exposure to an HFD and STZ. And the model mice received L-arabinose at 20 mg (kg bw)-1 d-1 had a better effect on improving T2DM than the high-dose group supplemented L-arabinose at 60 mg (kg bw)-1 d-1 . These results strongly suggest L-arabinose as an excellent candidate supplement to prevent or treat T2DM. PRACTICAL APPLICATIONS: L-arabinose, xylitol and sucralose are well-known substitutes for sucrose. L-arabinose has been reported to have beneficial effects on hyperglycemia, glycemic index, and fat accumulation. In this study, we found that low-dose (20 mg (kg bw)-1 d-1 ) supplementation of L-arabinose significantly improved glucose intolerance and gut microbiota incoordination in T2DM caused by HFD and STZ.


Assuntos
Diabetes Mellitus Tipo 2 , Microbioma Gastrointestinal , Animais , Arabinose , Diabetes Mellitus Tipo 2/tratamento farmacológico , Dieta Hiperlipídica/efeitos adversos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Camundongos , Camundongos Endogâmicos C57BL , Estreptozocina
6.
Int J Biol Macromol ; 192: 360-368, 2021 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-34634328

RESUMO

We incorporated oxidized dextran (Odex) into nanoparticles composed of gallic acid-modified chitosan (GA-CS) and sodium caseinate (NaCas). The mass ratio of GA-CS to NaCas and the pH of the reaction solution were optimized to obtain nanoparticles with excellent performance and stability. The interactions among various nanomaterials were confirmed by Fourier-transform infrared spectroscopy (FT-IR) and fluorescence spectrometer. The optimized complex nanoparticles had a diameter of approximately 131.2 nm with a polydispersity index (PDI) of 0.14, and a zeta potential of 26.2 mV. Our results showed that Odex enhanced the stability and function of GA-CS/NaCas nanoparticles (NP). At a curcumin loading of 10%, the encapsulation efficiency of Odex-crosslinked GA-CS/NaCas (NP (Odex)) was 96.2%, whereas that for uncrosslinked nanoparticles was 66.9%. Compared to the burst release profile of free curcumin in simulated GI fluids, the sustained release profile of encapsulated curcumin was observed. Radical-scavenging assays confirmed that the nanoparticles had excellent antioxidant activity themselves due to the grafting of phenolic acid on chitosan backbone. Overall, NP (Odex) with good GI stability and antioxidant activity hold promising for the oral delivery of hydrophobic bioactives.


Assuntos
Caseínas/química , Quitosana/química , Dextranos/química , Ácido Gálico/química , Nanopartículas/química , Curcumina/administração & dosagem , Curcumina/farmacocinética , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Concentração de Íons de Hidrogênio , Cinética , Tamanho da Partícula , Análise Espectral
7.
Int J Biol Macromol ; 183: 2282-2292, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34102238

RESUMO

The carriers for hydrophobic bioactives have been extensively studied, while those for hydrophilic bioactives are still challenging. The partition of bioactives in the particles depends greatly on their solubility, interaction with carrier materials, as well as structure of carriers. In this study, chitosan-coated hollow zein particles using calcium phosphate as a sacrificing template (CS-HZ) were fabricated to co-encapsulate folic acid (FA) and caffeic acid (CA). Partition, photostability, and antioxidant capacity of bioactive compounds were also studied. The size, polydispersity index and ζ-potential of optimized CS-HZ were 176.3 nm, 0.14 and +39.3 mV, respectively, indicating their small and uniform dimension with excellent colloidal stability. FA interacted with chitosan to form complexes and then coated on the zein particles where CA was encapsulated. After co-encapsulation in CS-HZ, the photostability of both FA and CA was improved in comparison with encapsulation of single compound, with 85% of FA remaining after 240 min of UVA irradiation, and 90% of CA remaining after 80 min. Antioxidant activity of CA decreased upon encapsulation, but significantly increased after irradiation. Findings in this study shed some light on the design of carriers for co-delivery of hydrophilic compounds in acidic condition.


Assuntos
Antioxidantes/química , Ácidos Cafeicos/química , Quitosana/química , Portadores de Fármacos , Ácido Fólico/química , Zeína/química , Antioxidantes/farmacologia , Ácidos Cafeicos/farmacologia , Fosfatos de Cálcio/química , Composição de Medicamentos , Estabilidade de Medicamentos , Ácido Fólico/farmacologia , Concentração de Íons de Hidrogênio , Fotólise , Propriedades de Superfície
8.
Food Chem ; 360: 130007, 2021 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-33993075

RESUMO

Brassica vegetables are widely consumed mostly after processing and cooking. These processing and cooking methods not only can affect the taste, texture, flavor and nutrients of these vegetables, but also influence the levels of some important bioactive compounds, such as glucosinolates (GLSs). Glucoraphanin (GLR) is the most abundant GLSs and its hydrolyzed component, sulforaphane (SLR), is the most powerful anti-cancer compound in brassica vegetables. In this review, we find out that varied treatments impact the retention of GLR and the formation of SLR differently. Be specific, 1) freezing can avoid the losses of GLR while short-time microwaving, short-time steaming and fermentation promote the biotransformation from GLR to SLR; 2) Boiling and blanching cause the largest losses of GLR and SLR, while freezing significantly protect their losses.; 3) Stir-frying varies the levels of GLR and SLR in different cooking conditions.


Assuntos
Brassica/química , Culinária , Glucosinolatos/análise , Isotiocianatos/análise , Oximas/análise , Sulfóxidos/análise , Humanos , Micro-Ondas
9.
Carbohydr Polym ; 264: 117999, 2021 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-33910733

RESUMO

As a natural polysaccharide, dextran and its derivatives have gained great attention in the development of delivery systems for pharmaceutical and medical applications. In recent years, numerous dextran-based delivery systems with tailor properties and geometries have been developed, including self-assembled micelles and nanoparticles, nanoemulsions, magnetic nanoparticles, microparticles, and hydrogels. The first part of this review discusses the physicochemical properties of dextran and its various derivatives via chemical modifications, as pertinent to the preparation of delivery systems. Then, the state-of-the-art fabrication strategies of dextran-based delivery systems and their colloidal properties, i.e. particle diameter, surface charge, morphology, as well as release profiles, are highlighted. Lastly, applications of dextran-based drug delivery systems in biomedicine are explicitly summarized with detailed elaborations on their biological efficacy and mechanism of action, including cancer treatment, magnetic resonance imaging, insulin oral delivery, spinal cord injury therapy, and bacterial skin infection treatment.


Assuntos
Dextranos/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Administração Oral , Dextranos/farmacologia , Portadores de Fármacos/farmacologia , Humanos , Hidrogéis/química , Insulina/química , Insulina/uso terapêutico , Imageamento por Ressonância Magnética/métodos , Micelas , Nanopartículas/química , Neoplasias/terapia , Tamanho da Partícula , Dermatopatias Bacterianas/terapia
10.
Int J Biol Macromol ; 179: 125-135, 2021 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-33667554

RESUMO

To overcome the poor aqueous solubility and bioavailability of curcumin, emphasize its functional features, and broaden its applications in the food and pharmaceutical industries, many nanoscale systems have been widely applied for its encapsulation and delivery. Over many decades, chitosan as a natural biopolymer has been extensively studied due to its polycationic nature, biodegradability, biocompatibility, non-toxicity, and non-allergenic. Various chitosan-based nanocarriers with unique properties for curcumin delivery, including but not limited to, self-assembled nanoparticles, nanocomposites, nanoemulsions, nanotubes, and nanofibers, have been designed. This review focuses on the most-recently reported fabrication techniques of different types of chitosan-based nanocarriers. The functionalities of chitosan in each formulation which determine the physicochemical properties such as surface charge, morphology, encapsulation driving force, and release profile, were discussed in detail. Moreover, the current pharmaceutical applications of curcumin-loaded chitosan nanoparticles were elaborated. The role of chitosan in facilitating the delivery of curcumin and improving the therapeutic effects on many chronic diseases, including cancer, bacterial infection, wound healing, Alzheimer's diseases, inflammatory bowel disease, and hepatitis C virus, were illustrated. Particularly, the recently discovered mechanisms of action of curcumin-loaded chitosan nanoparticles against the abovementioned diseases were highlighted.


Assuntos
Quitosana , Curcumina , Portadores de Fármacos , Nanopartículas , Quitosana/química , Quitosana/farmacocinética , Quitosana/uso terapêutico , Curcumina/química , Curcumina/farmacocinética , Curcumina/uso terapêutico , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/uso terapêutico , Humanos , Nanopartículas/química , Nanopartículas/uso terapêutico
11.
Int J Biol Macromol ; 151: 747-756, 2020 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-32084488

RESUMO

Astaxanthin (ASTX) has been reported as a potential therapeutic agent for hepatic fibrosis treatment. However, its therapeutic effect is limited due to low bioavailability and poor aqueous solubility. In this study, biopolymer-based nanoparticles were fabricated using stearic acid-chitosan conjugate (SA-CS) and sodium caseinate (NaCas) via ionic gelation. Its nanostructure was cross-linked using oxidized dextran (Odex) via Schiff base reaction. Concentration of cross-linker, cross-linking temperature and time were systematically optimized by response surface methodology (RSM) to achieve superior particulate properties and colloidal stability. The optimized nanoparticles exhibited a diameter of 120 nm with homogeneous size distribution. A good ASTX encapsulation capacity with up to 6% loading ratio and high encapsulation efficiency was obtained. The final ASTX concentration in nanoparticles was 140 µM. The aqueous dispersibility of encapsulated ASTX was greatly improved, which was confirmed by significantly increased ABTS radical scavenging capacity. Compared to the anti-fibrogenic effect of free ASTX in LX-2 cells, the encapsulated ASTX demonstrated dramatically enhanced cellular bioactivity, as evidenced by significantly lower TGFß1-induced fibrogenic gene (ACTA2 and COL1A1) expression level, as well as α-SMA and COL1A1 protein levels. This study suggests that the as-prepared biopolymer nanoparticles hold promising features as an oral delivery vehicle for lipophilic bioactives.


Assuntos
Caseínas/química , Quitosana/química , Dextranos/química , Portadores de Fármacos/química , Nanopartículas/química , Animais , Disponibilidade Biológica , Sobrevivência Celular , Cromatografia Líquida de Alta Pressão , Fibrinolíticos/administração & dosagem , Fibrinolíticos/farmacocinética , Nanopartículas/ultraestrutura , Tamanho da Partícula , Espectroscopia de Infravermelho com Transformada de Fourier , Análise Espectral , Xantofilas/administração & dosagem , Xantofilas/farmacocinética
12.
Molecules ; 24(22)2019 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-31717559

RESUMO

In this study, we prepared complex nanoparticles from a combination of two proteins and one polysaccharide for the encapsulation and delivery of lipophilic bioactive compounds. Two proteins, zein and sodium caseinate (NaCas), provided a hydrophobic core for the encapsulation of a lipophilic compound (curcumin), while a polysaccharide dialdehyde, oxidized dextran, served as the coating material and macromolecular crosslinker to create covalent linkage with two proteins for stabilization purposes. The heating time and crosslinker concentration were optimized to achieve the desirable colloidal stability in simulated gastric and intestinal fluids. Our results suggested that heating time played a more important role than the concentration of oxidized dextran. The optimized complex nanoparticles had a particle size of around 150 nm with a PDI < 0.1 and negative surface charge. Morphological observation by transmission electron microscopy revealed a spherical shape and uniform size distribution. Fourier transform infrared and fluorescence spectroscopies evidenced the formation of Schiff base complex, confirming the validity of covalent crosslinking. Furthermore, the complex nanoparticles demonstrated superior encapsulation properties for curcumin, showing an efficiency of >90% at 10% loading. A rather slow kinetic release profile of curcumin from complex nanoparticles was observed under simulated gastrointestinal conditions. The complex nanoparticles prepared from zein, NaCas, and oxidized dextran hold promising potential for the oral delivery of lipophilic bioactive compounds.


Assuntos
Caseínas/química , Curcumina/química , Dextranos/química , Nanopartículas/química , Zeína/química , Varredura Diferencial de Calorimetria/métodos , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Interações Hidrofóbicas e Hidrofílicas , Cinética , Microscopia Eletrônica de Transmissão/métodos , Tamanho da Partícula
13.
Int J Biol Macromol ; 120(Pt A): 775-782, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30170057

RESUMO

Diabetes mellitus is a highly prevalent metabolic and chronic disease affecting millions of people in the world. The most common route of insulin therapy is the subcutaneous injection due to its low bioavailability and enzymatic degradation. The search for effective and high patient compliance insulin delivery systems has been a major challenge over many decades. The polysaccharide-based nanoparticles as delivery vehicles for insulin oral administration have recently attracted substantial interests. The present review highlights the recent advances on the development of nanoparticles prepared from polysaccharides, including chitosan, alginate, dextran and glucan, for oral delivery of insulin, overcoming multiple barriers in gastrointestinal tract. The aims of this review are first to summarize the strategies that have been applied in the past 5 years to fabricate polysaccharide-based nanoparticles for insulin oral delivery, and then to provide in-depth understanding on the mechanisms by which such nanoparticles protect insulin against degradation in the digestive tract and provide sustained release to enhance mucus permeation and transepithelial transport of insulin administered via oral route.


Assuntos
Diabetes Mellitus/tratamento farmacológico , Insulina/uso terapêutico , Nanopartículas/uso terapêutico , Polissacarídeos/química , Administração Oral , Alginatos/síntese química , Quitosana/química , Quitosana/uso terapêutico , Diabetes Mellitus/patologia , Sistemas de Liberação de Medicamentos , Humanos , Insulina/química , Nanopartículas/química , Polissacarídeos/uso terapêutico
14.
J Agric Food Chem ; 66(36): 9473-9480, 2018 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-30130387

RESUMO

Solid lipid-polymer hybrid nanoparticles (SLPN) are nanocarriers made from a combination of polymers and lipids, integrating the advantages of biocompatible lipid-based nanoparticles and gastrointestinal (GI)-stable polymeric nanoparticles. In this study, a novel preparation strategy was proposed to fabricate GI-stable SLPN through in situ conjugation between oxidized dextran and bovine serum albumin. Effects of molecular weight of dextran (20, 40, 75, and 150 kDa), conjugation temperature (65 °C, 75 °C, and 85 °C), and time (30, 60, 120 min) on the particulate characteristics and stability were comprehensively investigated and optimized. As heating temperature increased from 65 °C to 75 °C, the particle size of SLPN increased from 139 to 180 nm with narrow size distribution, but when the temperature reached 85 °C severe aggregation was observed after 60 min. SLPN prepared with 40 kDa oxidized dextran under 85 °C/30 min heating condition exhibited excellent GI stability with no significant changes in particle size and PDI after incubation in simulated GI fluids. The prepared SLPN were then used to encapsulate astaxanthin, a lipophilic bioactive compound, studied as a model nutrient. After encapsulation in SLPN, antioxidant activity of astaxanthin was dramatically enhanced in aqueous condition and a sustained release was achieved in simulated GI fluids. Therefore, the SLPN developed in this study are a promising oral delivery system for lipophilic compounds, such as astaxanthin.


Assuntos
Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Lipídeos/química , Nanopartículas/química , Administração Oral , Sistemas de Liberação de Medicamentos/instrumentação , Estabilidade de Medicamentos , Tamanho da Partícula , Polímeros/administração & dosagem , Polímeros/química , Xantofilas/administração & dosagem , Xantofilas/química
15.
Int J Biol Macromol ; 120(Pt A): 859-864, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30165144

RESUMO

Alginate hydrogel beads have been extensively investigated as drug delivery systems due to promising gastric environment stability. In the present study, alginate hydrogel beads were prepared with Ca2+ or Fe3+ to serve as the loading vehicles for egg yolk low density lipoprotein (LDL)/pectin nanogels. Scanning electron microscope was carried out to confirm the successful incorporation of nanogels into the beads. The FT-IR spectra and swelling ratio analyses proved that incorporation of nanogels did not affect the physicochemical properties of the hydrogel beads. The developed hydrogel beads exhibited pH dependent release of curcumin pre-encapsulated in nanogels, with significant retention of curcumin in gastric condition compared to curcumin encapsulated in nanogels or alginate beads alone. Hydrogel beads prepared with low viscous alginate and Ca2+ showed limited swelling property and more sustained release of curcumin in simulated gastrointestinal conditions, compared to the beads prepared with high viscous alginate and Fe3+. Gradual dissociation of nanogels from the beads during incubation in simulated intestinal fluid was studied with transmission electron microscope. Our study demonstrated the promising potential of alginate beads as a carrier to protect LDL-based nanogels from destabilization in gastric condition, thus expanding their applications as oral delivery system.


Assuntos
Alginatos/química , Curcumina/química , Sistemas de Liberação de Medicamentos , Polietilenoglicóis/química , Polietilenoimina/química , Administração Oral , Alginatos/uso terapêutico , Curcumina/síntese química , Curcumina/uso terapêutico , Gema de Ovo/química , Humanos , Hidrogel de Polietilenoglicol-Dimetacrilato/química , Hidrogel de Polietilenoglicol-Dimetacrilato/uso terapêutico , Concentração de Íons de Hidrogênio , Lipoproteínas LDL/química , Microscopia Eletrônica de Varredura , Nanogéis , Pectinas/química , Pectinas/uso terapêutico , Polietilenoglicóis/uso terapêutico , Polietilenoimina/uso terapêutico , Espectroscopia de Infravermelho com Transformada de Fourier
16.
Food Chem ; 239: 840-847, 2018 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-28873642

RESUMO

Egg yolk low density lipoprotein (LDL)/polysaccharide nanogels are newly explored as oral delivery systems with promising encapsulation potentials. Nonetheless, the stability of nanogels against aggregation in gastrointestinal tract remains a challenge. Therefore, chemical crosslinking by 1-ethyl-3-(3-dimethylaminopropyl) and carbodiimide/N-hydroxysuccinimide (EDC/NHS) was adopted to improve the gastrointestinal stability of nanogels. Compared to original uncrosslinked nanogels, crosslinking did not change particle size, polydispersity index (PDI) and morphology, but it reduced surface charge of nanogels. The nano spray dried LDL/CMC/EDC nanogels had relatively poor surface structure with agglomerations. The FT-IR spectra confirmed the formation of new peptide bonds, which significantly improved stability of nanogels under simulated gastrointestinal conditions. Fluorescence spectra evidenced that non-polar microenvironment for curcumin embedded in nanogels was strengthened, which therefore enhanced encapsulation efficiency. Moreover, curcumin exhibited sustained release profile from crosslinked nanogels in simulated gastrointestinal fluids. Overall, our study provided a promising strategy to enhance the stability of LDL-based nanogels in digestive conditions.


Assuntos
Gema de Ovo , Nanogéis , Polietilenoglicóis , Polietilenoimina , Polissacarídeos , Espectroscopia de Infravermelho com Transformada de Fourier
17.
Int J Pharm ; 531(1): 59-66, 2017 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-28802794

RESUMO

In this work, a new and novel organic solvent-free and synthetic surfactant-free method was reported to fabricate stable solid lipid nanoparticles (SLNs) from stearic acid, sodium caseinate (NaCas) and pectin, as well as water. Melted stearic acid was directly emulsified into an aqueous phase containing NaCas and pectin, followed by pH adjustment and thermal treatment to induce the formation of a compact and dense polymeric coating which stabilized SLNs. The preparation procedures and formulations were comprehensively optimized. The inter- and intra-molecular interactions among three ingredients were characterized by fluorescence and Fourier transform infrared spectroscopies. The stability of as-prepared SLNs was evaluated under simulated gastrointestinal conditions, and compared with traditional SLNs prepared with organic solvents. Our results revealed that the SLNs prepared from this organic solvent-free method had superior physicochemical properties over the traditional SLNs, including smaller size and better stability. Furthermore, redispersible SLNs powders were obtained by nano spray drying, but only the SLNs prepared by organic solvent-free method had sub-micron scale, uniform and spherical morphology. The organic solvent-free preparation method was proved to be a promising approach to prepare stable and uniform SLNs for potential oral delivery applications.


Assuntos
Biopolímeros/química , Portadores de Fármacos/química , Emulsificantes/química , Lipídeos/química , Nanopartículas/química , Caseínas , Química Farmacêutica , Tamanho da Partícula , Pectinas , Solventes , Ácidos Esteáricos
18.
J Colloid Interface Sci ; 507: 119-130, 2017 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-28780331

RESUMO

Exploitation of lipid nanoparticles for oral delivery of nutrients and drugs is limited by their poor stability under gastrointestinal tract and low loading capacity, unless a high concentration of synthetic surfactants is formulated. The main objective of present study is to design a series of new formulations for solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) that are suitable for potential oral delivery applications, using natural biopolymers, i.e. sodium caseinate (NaCas) as emulsifier and pectin as coating, with minimal addition of a synthetic surfactant, Tween 80. Effects of pectin coating, concentration of Tween 80, thermal treatment (80°C for 30min), as well as two chemical cross-linkers on the particulate characteristics, stability, encapsulation efficiency, controlled release and drying feasibility were comprehensively investigated. The intermolecular interactions and cross-linking reactions were studied using Fourier transform infrared spectroscopy. Tween 80 at 0.15% (w/v) together with 0.15% (w/v) NaCas was proved effective to obtain stable cross-linked pectin-coated SLN (PSLN) under 200nm with high loading capacity for curcumin, while NLC prepared under the same condition failed to pass storage stability test. The 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide/N-hydroxysuccinimide (EDC/NHS) cross-linked PSLN exhibited superior characteristics than glutaradehyde (GA) cross-linked PSLN, especially for the stability and controlled release under simulated gastrointestinal conditions, with curcumin studied as a model compound. The feasibility of both nano spray drying and freeze-drying technologies were both investigated to transform of colloidal lipid nanoparticles into dry powders. Our results demonstrated a novel strategy to prepare small and homogenous SLN with exceptional GI stability and high loading capacity as a potential oral delivery system.


Assuntos
Portadores de Fármacos/química , Lipídeos/química , Nanopartículas/química , Caseínas/química , Reagentes de Ligações Cruzadas/química , Curcumina/administração & dosagem , Curcumina/química , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Emulsificantes/química , Excipientes/química , Liofilização , Absorção Gastrointestinal , Humanos , Cinética , Tamanho da Partícula , Pectinas/química , Succinimidas/química , Propriedades de Superfície , Tensoativos/química
19.
Int J Biol Macromol ; 104(Pt A): 117-124, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28579466

RESUMO

In this study, pectin was used as coating material to form zein/caseinate/pectin complex nanoparticles through pH adjustment and heating treatment for potential oral delivery applications. The preparation conditions were studied by applying heating treatment at different pHs, either the isoelectric point of zein (pH 6.2) or caseinate (pH 4.6), or consecutively at both pHs. The particulate characteristics, including particle size, polydispersity index, and zeta potential were monitored for complex nanoparticles formed under different preparation conditions. The complex nanoparticles generally exhibited particle size smaller than 200nm with narrow distribution, spherical shape, and strong negative charge. Fourier transform infrared and fluorescence spectroscopy revealed that hydrophobic interactions and hydrogen bonds were involved in the formation of complex nanoparticles, in addition to electrostatic interactions. Fresh colloidal dispersion and freeze-dried powders varied in their morphology, depending on their preparation conditions. Our results suggested that heating pH and sequence significantly affected the morphology of complex nanoparticles, and pectin coating exerted stabilization effect under simulated gastrointestinal conditions. The present study provides insight into the formation of protein/polysaccharide complex nanoparticles under different preparation conditions.


Assuntos
Caseínas/química , Nanopartículas/química , Pectinas/química , Zeína/química , Liofilização , Trato Gastrointestinal/metabolismo , Tamanho da Partícula
20.
Sci Rep ; 7(1): 2750, 2017 06 05.
Artigo em Inglês | MEDLINE | ID: mdl-28584240

RESUMO

The toxicity associated with concentrated synthetic surfactants and the poor stability at gastrointestinal condition are two major constraints for practical applications of solid lipid nanoparticles (SLN) as oral delivery vehicles. In this study, a synthetic surfactant-free and cross-linker-free method was developed to fabricate effective, safe, and ultra-stable lipid-polymer hybrid nanoparticles (LPN). Bovine serum albumin (BSA) and dextran varying in molecular weights were first conjugated through Maillard reaction and the conjugates were exploited to emulsify solid lipid by a solvent diffusion and sonication method. The multilayer structure was formed by self-assembly of BSA-dextran micelles to envelope solid lipid via a pH- and heating-induced facile process with simultaneous surface deposition of pectin. The efficiency of different BSA-dextran conjugates was systematically studied to prepare LPN with the smallest size, the most homogeneous distribution and the greatest stability. The molecular interactions were characterized by Fourier transform infrared and fluorescence spectroscopies. Both nano spray drying and freeze-drying methods were tested to produce spherical and uniform pectin-coated LPN powders that were able to re-assemble nanoscale structure when redispersed in water. The results demonstrated the promise of a synthetic surfactant- and cross-linker-free technique to prepare highly stable pectin-coated LPN from all natural biomaterials as potential oral delivery vehicles.


Assuntos
Portadores de Fármacos/química , Lipídeos/química , Nanopartículas/química , Polímeros/química , Administração Oral , Adsorção , Reagentes de Ligações Cruzadas/química , Dextranos , Portadores de Fármacos/síntese química , Sistemas de Liberação de Medicamentos , Reação de Maillard , Pectinas , Polímeros/síntese química , Soroalbumina Bovina , Espectroscopia de Infravermelho com Transformada de Fourier , Tensoativos/química
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