Stability and Bioaccessibility of Fucoxanthin in Nanoemulsions Prepared from Pinolenic Acid-contained Structured Lipid

Abstract: Fucoxanthin intake has been correlated with the functions of anti-obesity and anti-oxidation, but applications of it in functional food or dietary supplements are still challenging due to its poor water-solubility, chemical instability, and low bioavailability. In this work, to study physicochemical and biological properties of fucoxanthin nanoemulsions, we investigated the influence of emulsion particle diameter on the stability of fucoxanthin during storage time and bioaccessibility in-vitro digestion. The structured lipid that enriched pinolenic acid at sn-2 position was chosen as the oil phase and the fucoxanthin oil-in-water nanoemulsions with droplet diameters of 344, 173, and 98 nm were prepared through a high-pressure microfluidizer. Then fucoxanthin emulsions were stored for 28 days at 4, 37, and 55 °C. Results showed that the physical stabilities of droplets were decreased with increases in the initial size and storage temperature, while the change of fucoxanthin retention indicated that fucoxanthin chemical stability was improved with increasing emulsion particle size. The augmentation of lipolysis and the value of free fatty acids (FFA) released in vitro digestion proved that digestion stability of fucoxanthin emulsion reduced with decreasing initial particle diameter, which was probably attributed to the increased surface area interacting with pancreatic lipase with decreasing droplet size. In addition, the concentrations of fucoxanthin in micelle phase were appreciable increased as droplet size decreased. Therefore, the bioaccessibility of fucoxanthin was improved. These results may benefit the optimization of an emulsion-based delivery system for fucoxanthin in food applications.

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DEVELOPMENT OF MICROEMULSION FORMULATION FOR ORAL DELIVERY OF ROSUVASTATIN CALCIUM

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2020.120106 ◽

2020 ◽

pp. 35-39

Author(s):

Himanshu Paliwal ◽

Ram Singh Solanki ◽

Chetan Singh Chauhan

Keyword(s):

Zeta Potential ◽

Droplet Size ◽

Oral Delivery ◽

Water Solubility ◽

Tween 80 ◽

In Vitro Dissolution ◽

Microemulsion Formulation ◽

Polyethylene Glycol 400 ◽

Rosuvastatin Calcium

The purpose of conducting this study was to prepare an oral microemulsion formulation of Rosuvastatin calcium (RC) to improve its water solubility. Oil in water microemulsion was formulated using Oleic acid, Tween 80 and Polyethylene Glycol-400(PEG-400) as oil, surfactant and co-surfactant, respectively. The ideal proportion of surfactant: co-surfactant (Smix) was chosen by constructing pseudoternary diagrams. The microemulsion formulations which proved to be stable after thermodynamic stability testing were further evaluated for physical characteristics. Selected formulations were evaluated for droplet size, zeta potential, polydispersity index, viscosity and % drug content. The results were suggestive that optimized microemulsion formulation (F2) was thermodynamically stable and clear having a droplet size of 74.29 nm and zeta potential of -18.44. In vitro dissolution study for optimized microemulsion was performed using a dialysis bag method and cumulative % drug release was determined. The result from the release study was indicative of improved solubility of Rosuvastatin calcium which may serve to boost up the oral bioavailability of drug.

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Characterization of Andean Blueberry in Bioactive Compounds, Evaluation of Biological Properties and in vitro Bioaccessibility

10.20944/preprints202009.0055.v1 ◽

2020 ◽

Author(s):

Nieves Baenas ◽

Jenny Ruales ◽

Diego A. Moreno ◽

Daniel Alejandro Barrio ◽

Carla M. Stinco ◽

...

Keyword(s):

Antioxidant Capacity ◽

Bioactive Compounds ◽

Biological Activities ◽

In Vitro Digestion ◽

Biological Properties ◽

Wide Range ◽

Zebrafish Embryogenesis

Andean blueberries are wild berries grown and consumed in Ecuador which contain high values of bioactive compounds, mainly anthocyanins, with powerful antioxidant activity. The aim of this study was to evaluate the profile and contents of (poly)phenols and carotenoids in Andean blueberry by HPLC-DAD-MSn and determine a wide range of its biological activities. The antioxidant capacity of this fruit was evaluated in vitro by three different methods and in vivo using the zebrafish animal model, also the toxicity effect was determined by the zebrafish embryogenesis test. Besides, the antimicrobial activity and the capacity of Andean blueberry to produce hemagglutination in blood cells were evaluated. Finally, the bioaccessibility of (poly)phenols and related antioxidant capacity were determined in the different phases of an in vitro digestion. The global results indicated no toxicity of Andean blueberry, weakly bacteriostatic activity, and high contents of anthocyanins and antioxidant capacity, which were partially bioaccesible in vitro (~ 50 % at the final intestinal step), contributing to the knowledge of its health benefits for consumers and its potential use in the food and pharmaceutical industry as functional ingredient.

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DEVELOPMENT AND CHARACTERIZATION OF A NANOCARRIER FOR QUERCETIN

International Journal of Nanoscience ◽

10.1142/s0219581x09005979 ◽

2009 ◽

Vol 08 (01n02) ◽

pp. 175-179 ◽

Cited By ~ 1

Author(s):

MAN-YI WONG ◽

GIGI N. C. CHIU

Keyword(s):

Breast Cancer Cells ◽

Water Solubility ◽

Storage Temperature ◽

In Vitro Cytotoxicity ◽

Cytotoxic Compound ◽

Naturally Occurring ◽

Quercetin Concentration ◽

Fold Stability

Quercetin is a naturally occurring cytotoxic compound where clinical use has been limited by its low water solubility. Therefore, liposomes were explored for solubilizing quercetin. Liposomes composed of DPPC (1,2 dipalmitoyl-sn-glycerol-3-phosphocholine)/DSPE-PEG2000 (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)2000])/quercetin (90:5:5 mole ratio) incorporated quercetin efficiently at 100.9 ± 4.6% and increased quercetin concentration in water 11.2-fold. Stability studies at storage temperature of 4°C showed that the liposomes were stable for up to 16 weeks, without any significant changes in diameters. Liposomal quercetin showed a delayed release profile and reduced quercetin degradation. In vitro cytotoxicity tests also showed that the ED50 of liposomal quercetin was 17.6 times lower than free quercetin in MDA-MB-231 breast cancer cells. In conclusion, the DPPC/DSPE-PEG-based liposomes were stable and were capable of solubilizing quercetin, preventing quercetin degradation, and increasing quercetin in vitro cytotoxicity. Hence, liposomes are a suitable nanocarrier for quercetin.

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Supersaturation and Solubilization upon In Vitro Digestion of Fenofibrate Type I Lipid Formulations: Effect of Droplet Size, Surfactant Concentration and Lipid Type

Pharmaceutics ◽

10.3390/pharmaceutics13081287 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1287

Author(s):

Vladimir Katev ◽

Sonya Tsibranska-Gyoreva ◽

Zahari Vinarov ◽

Slavka Tcholakova

Keyword(s):

Droplet Size ◽

Surfactant Concentration ◽

Drop Size ◽

Prediction Models ◽

In Vitro Digestion ◽

Oral Drug ◽

Type I ◽

Concentration Effects ◽

Drug Solubilization

Lipid-based formulations (LBF) enhance oral drug absorption by promoting drug solubilization and supersaturation. The aim of the study was to determine the effect of the lipid carrier type, drop size and surfactant concentration on the rate of fenofibrate release in a bicarbonate-based in vitro digestion model. The effect of the lipid carrier was studied by preparing type I LBF with drop size ≈ 2 µm, based on medium-chain triglycerides (MCT), sunflower oil (SFO), coconut oil (CNO) and cocoa butter (CB). The drop size and surfactant concentration effects were assessed by studying MCT and SFO-based formulations with a drop size between 400 nm and 14 µm and surfactant concentrations of 1 or 10%. A filtration through a 200 nm filter followed by HPLC analysis was used to determine the aqueous fenofibrate, whereas lipid digestion was followed by gas chromatography. Shorter-chain triglycerides were key in promoting a faster drug release. The fenofibrate release from long-chain triglyceride formulations (SFO, CNO and CB) was governed by solubilization and was enhanced at a smaller droplet size and higher surfactant concentration. In contrast, supersaturation was observed after the digestion of MCT emulsions. In this case, a smaller drop size and higher surfactant had negative effects: lower peak fenofibrate concentrations and a faster onset of precipitation were observed. The study provides new mechanistic insights on drug solubilization and supersaturation after LBF digestion, and may support the development of new in silico prediction models.

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Influence of Dairy Emulsifier Type and Lipid Droplet Size on Gastrointestinal Fate of Model Emulsions: In Vitro Digestion Study

Journal of Agricultural and Food Chemistry ◽

10.1021/acs.jafc.8b02959 ◽

2018 ◽

Vol 66 (37) ◽

pp. 9761-9769 ◽

Cited By ~ 10

Author(s):

Li Liang ◽

Xiaoyun Zhang ◽

Xingguo Wang ◽

Qingzhe Jin ◽

David Julian McClements

Keyword(s):

Droplet Size ◽

Lipid Droplet ◽

In Vitro Digestion ◽

Lipid Droplet Size

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Comparison of Different Protein Emulsifiers on Physicochemical Properties of β-Carotene-Loaded Nanoemulsion: Effect on Formation, Stability, and In Vitro Digestion

Nanomaterials ◽

10.3390/nano11010167 ◽

2021 ◽

Vol 11 (1) ◽

pp. 167

Author(s):

Yanlong Liu ◽

Chang Liu ◽

Shenyi Zhang ◽

Jishu Li ◽

Huanyu Zheng ◽

...

Keyword(s):

Droplet Size ◽

Corn Oil ◽

Emulsion Stability ◽

Soy Protein Isolate ◽

Oxidation Stability ◽

In Vitro Digestion ◽

Protein Isolate ◽

Oxidation Rates ◽

Β Carotene

In this study, β-carotene-loaded nanoemulsions are emulsified using four biomacromolecular proteins—peanut protein isolate (PPI), soy protein isolate (SPI), rice bran protein isolate (RBPI), and whey protein isolate (WPI)—in order to explore their emulsion stability and in vitro digestion characteristics. All four nanoemulsions attained high encapsulation levels (over 90%). During the three-stage in vitro digestion model (including oral, gastric, and small intestine digestion phases), the PPI-emulsified nanoemulsion showed the highest lipolysis rates (117.39%) and bioaccessibility (37.39%) among the four nanoemulsions. Moreover, the PPI-emulsified nanoemulsion (with the smallest droplet size) also demonstrated the highest stability during storage and centrifugation, while those for the RBPI-emulsified nanoemulsion (with the largest droplet size) were the lowest. In addition, all four nanoemulsions showed superior oxidation stability when compared with the blank control of corn oil. The oxidation rates of the PPI- and WPI-stabilized groups were slower than the other two groups.

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Recent Advances on Nanoparticle Based Strategies for Improving Carotenoid Stability and Biological Activity

Antioxidants ◽

10.3390/antiox10050713 ◽

2021 ◽

Vol 10 (5) ◽

pp. 713

Author(s):

Kandi Sridhar ◽

Baskaran Stephen Inbaraj ◽

Bing-Huei Chen

Keyword(s):

Water Solubility ◽

Metal Oxide Nanoparticles ◽

Physical Stability ◽

Aqueous Solubility ◽

In Vitro Digestion ◽

Storage Conditions ◽

Lipid Nanoparticles ◽

Research Review ◽

Metal Metal

Carotenoids are natural pigments widely used in food industries due to their health-promoting properties. However, the presence of long-chain conjugated double bonds are responsible for chemical instability, poor water solubility, low bioavailability and high susceptibility to oxidation. The application of a nanoencapsulation technique has thus become a vital means to enhance stability of carotenoids under physiological conditions due to their small particle size, high aqueous solubility and improved bioavailability. This review intends to overview the advances in preparation, characterization, biocompatibility and application of nanocarotenoids reported in research/review papers published in peer-reviewed journals over the last five years. More specifically, nanocarotenoids were prepared from both carotenoid extracts and standards by employing various preparation techniques to yield different nanostructures including nanoemulsions, nanoliposomes, polymeric/biopolymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid nanoparticles, supercritical fluid-based nanoparticles and metal/metal oxide nanoparticles. Stability studies involved evaluation of physical stability and/or chemical stability under different storage conditions and heating temperatures for varied lengths of time, while the release behavior and bioaccessibility were determined by various in vitro digestion and absorption models as well as bioavailability through elucidating pharmacokinetics in an animal model. Moreover, application of nanocarotenoids for various biological applications including antioxidant, anticancer, antibacterial, antiaging, cosmetics, diabetic wound healing and hepatic steatosis were summarized.

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BETULIN DERIVATIVES. BIOLOGICAL ACTIVITY AND SOLUBILITY IMPROVEMENT

chemistry of plant raw material ◽

10.14258/jcprm.2019045419 ◽

2019 ◽

pp. 407-430

Author(s):

Ol'ga Aleksandrovna Vorobyeva ◽

Darina Sergeyevna Malygina ◽

Elizaveta Vladimirovna Grubova ◽

Nina Borisovna Melnikova

Keyword(s):

Betulinic Acid ◽

Water Solubility ◽

Ex Vivo ◽

Mechanical Action ◽

Biological Properties ◽

Birch Bark ◽

Solubility Improvement ◽

Betulin Derivatives

In the review the biological properties (antitumor, antiviral, hypolipidemic, anti-inflammatory, etc.) and bioavailability of betulin and betulinic acid derivatives were discussed. These compounds are isolated from various natural sources, including birch bark (Betula, Betulaceae). The structure-activity correlation was considered for well-known betulinic acid derivatives. The perspectivity of this compounds as active pharmaceutical ingredients was demonstrated by in vitro, in vivo, and ex vivo experiments. The type of antitumor actions, generally, depends on substituents at the C-3 and C-28 carbon atoms of the lupane skeleton. It is very important that the carboxyl group of betulinic acid in the C-28 position was present. In this case, the cytotoxicity of C-3 modified derivatives is extremely high for all tested cell lines. The use of these compounds in the medical practice is complicated because they have low bioavailability and poor water solubility (from 1 to 100 µg*l-1). The main chemical syntheses for solubility improvement of betulin derivatives by grafting of hydrophilic groups were discussed. Moreover, the colloid-chemical approaches for the bioavailability improving of triterpenoids include: 1) including of these compounds in liposomes, vesicles and other nanoparticles; 2) obtaining of micelles with high-molecular compounds; 3) colloid-chemical dissolution due to physico-mechanical action; 4) inclusion complexes formation; 5) using of polymers for triterpenoids grafting. Chemical modification of betulin and betulinic acid by polar groups, such as phosphate/phosphonate, sulfate, amino acids, etc. has been shown for bioavailability improving.

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Changes in Physicochemical and Biological Properties of Polyphenolic-Protein-Polysaccharide Ternary Complexes from Hovenia dulcis after In Vitro Simulated Saliva-Gastrointestinal Digestion

Foods ◽

10.3390/foods10102322 ◽

2021 ◽

Vol 10 (10) ◽

pp. 2322

Author(s):

Ding-Tao Wu ◽

Yuan He ◽

Meng-Xi Fu ◽

Ren-You Gan ◽

Yi-Chen Hu ◽

...

Keyword(s):

Molecular Weight ◽

Biological Activities ◽

In Vitro Digestion ◽

Biological Properties ◽

Inhibitory Effects ◽

Gastrointestinal Digestion ◽

Sugar Release ◽

Physicochemical And Biological Properties ◽

Hovenia Dulcis

The present study aimed to explore the impacts of in vitro simulated saliva-gastrointestinal digestion on physicochemical and biological properties of the polyphenolic-protein-polysaccharide ternary complex (PPP) extracted from Hovenia dulcis. The results revealed that the in vitro digestion did remarkably affect physicochemical properties of PPP, such as content of reducing sugar release, content of bound polyphenolics, and molecular weight distribution, as well as ratios of compositional monosaccharides and amino acids. In particular, the content of bound polyphenolics notably decreased from 281.93 ± 2.36 to 54.89 ± 0.42 mg GAE/g, which might be the major reason for the reduction of bioactivities of PPP after in vitro digestion. Molecular weight of PPP also remarkably reduced, which might be attributed to the destruction of glycosidic linkages and the disruption of aggregates. Moreover, although biological activities of PPP obviously decreased after in vitro digestion, the digested PPP (PPP-I) also exhibited remarkable in vitro antioxidant and antiglycation activities, as well as in vitro inhibitory effects against α-glucosidase. These findings can help to well understand the digestive behavior of PPP extracted from H. dulcis, and provide valuable and scientific supports for the development of PPP in the industrial fields of functional food and medicine.

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Effective and Sustained Control of Soil-Borne Plant Diseases by Biodegradable Polyhydroxybutyrate Mulch Films Embedded with Fungicide of Prothioconazole

Molecules ◽

10.3390/molecules26030762 ◽

2021 ◽

Vol 26 (3) ◽

pp. 762

Author(s):

Ge Chen ◽

Lidong Cao ◽

Chong Cao ◽

Pengyue Zhao ◽

Fengmin Li ◽

...

Keyword(s):

Environmental Sustainability ◽

Water Solubility ◽

Composite Films ◽

Sclerotium Rolfsii ◽

Pathogenic Fungi ◽

Biological Properties ◽

Plant Diseases ◽

Soil System ◽

Mulch Films

Soil-borne diseases and plant rhizosphere nematode have caused many crop yield losses. Increased environmental awareness is leading to more restrictions on the use of certain fumigants and root irrigation methods due to their impact on human health and soil system. Therefore, it is necessary to find alternative treatments to maintain crop economic yields and environmental sustainability. In the present work, biodegradable antifungal mulches were prepared by blending poly(3-hydroxybutyrate-co-4-hydroxybutyrate) (PHB) with fungicide of prothioconazole (PRO), which were used for effective and sustained control of soil-borne plant diseases. To reveal the application prospect of the PHB/PRO composite films in the management of soilborne plant diseases, some physical and biological properties were evaluated. The proper mulch film of PHB/PRO was assessed based on its mechanical and optical properties, while water solubility and the film micromorphology was further characterized. The release patterns of composite films under different pH levels were investigated. Moreover, the in vitro antifungal bioassay and pot experiment showed satisfactory bioactivity of the PHB/PRO films against Sclerotium rolfsii Sacc., a soil-borne disease in peanut fields. This study demonstrated that the biodegradable mulch films containing PRO fungicide are capable of inhibiting soil-borne plant pathogenic fungi effectively, and this facile but powerful strategy may find wide applicability in sustainable plant and horticulture protection.

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