Low Molecular Weight Kappa-Carrageenan Based Microspheres for Enhancing Stability and Bioavailability of Tea Polyphenols

Tea polyphenols (TP) are a widely acknowledged bioactive natural product, however, low stability and bioavailability have restricted their application in many fields. To enhance the stability and bioavailability of TP under certain moderate conditions, encapsulation technique was applied. Kappa–Carrageenan (KCG) was initially degraded to a lower molecular weight KCG (LKCG) by H2O2, and was selected as wall material to coat TP. The obtained LKCG (Mn = 13,009.5) revealed narrow dispersed fragments (DPI = 1.14). FTIR and NMR results demonstrated that the main chemical structure of KCG remained unchanged after degradation. Subsequently, LK-CG and TP were mixed and homogenized to form LK-CG-TP microspheres. SEM images of the microspheres revealed a regular spherical shape and smooth surface with a mean diameter of 5–10 μM. TG and DSC analysis indicated that LK-CG-TP microspheres exhibited better thermal stability as compared to free TP. The release profile of LK-CG-TP in simulated gastric fluid (SGF) showed a slowly release capacity during the tested 180 min with the final release rate of 88.1% after digestion. Furthermore, in vitro DPPH radical scavenging experiments revealed that LK-CG-TP had an enhanced DPPH scavenging rate as compared to equal concentration of free TP. These results indicated that LK-CG-TP microspheres were feasible for protection and delivery of TP and might have extensive potential applications in other bioactive components.

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Green Technology Enabled Graphene Oxide Reduction Using Justichia wynaadensis Extract and Assessment of In Vitro Antioxidant and Antibacterial Activity

Advanced Science Letters ◽

10.1166/asl.2018.12186 ◽

2018 ◽

Vol 24 (8) ◽

pp. 5726-5730 ◽

Cited By ~ 2

Author(s):

P Shubha ◽

K Namratha ◽

K. C Mithali ◽

V Divya ◽

M. S Thakur ◽

...

Keyword(s):

Antibacterial Activity ◽

Graphene Oxide ◽

Aqueous Extract ◽

Biological Activities ◽

Radical Scavenging ◽

Green Technology ◽

Oxide Reduction ◽

Efficient Removal ◽

Sem Images

Graphene oxide (GO) was reduced using Justichia wynaadensis aqueous extract. GO was mixed with extract and refluxed at 100 °C for 10 h to obtain reduced GO. PXRD of rGO showed broad peak at 2 = 25° and disappearance of 2 = 9.75° after refluxing which indicates efficient removal of oxygen containing groups. SEM images of rGO showed flaky structures typical of retainment of GO structure with folded curtains like appearance of rGO. UV-vis spectra demonstrated absorption band ~300 nm and shoulder at 400 nm corresponding to π–π* transitions and C ═ O bonds respectively indicating that rGO is red shifted due to decrease in oxygen functional groups. rGO showed potent antibacterial activity against Staphylococcus aureus, upon testing against S. aureus and P. aeruginosa. It showed 67% radical scavenging against DPPH at 500 μg/mL concentration. In conclusion, J. wynaadensis aqueous extract efficiently removed oxygen functionalities from GO surface with significant biological activities.

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Fabrication and Characterization of Zein Composite Particles Coated by Caseinate-Pectin Electrostatic Complexes with Improved Structural Stability in Acidic Aqueous Environments

Molecules ◽

10.3390/molecules24142535 ◽

2019 ◽

Vol 24 (14) ◽

pp. 2535 ◽

Cited By ~ 2

Author(s):

Yaqiong Zhang ◽

Bo Wang ◽

Yan Wu ◽

Boyan Gao ◽

Liangli (Lucy) Yu

Keyword(s):

Hydrophobic Interactions ◽

In Vitro Release ◽

Radical Scavenging ◽

Spherical Shape ◽

Average Diameter ◽

Composite Particles ◽

Aqueous Environment ◽

Electrostatic Deposition ◽

Long Term Storage

Zein composite particles coated with caseinate-pectin electrostatic complexes (zein-caseinate-pectin particles) were fabricated using an electrostatic deposition and liquid-liquid dispersion method without heating treatment. Compared to zein particles coated only with caseinate, the acidic stability of zein-caseinate-pectin particles was greatly improved, and the particle aggregation was suppressed at pH 3–6, especially at pH values near the isoelectric point of caseinate (pH 4–5). Besides, desirable long-term storage stability and re-dispersibility were observed. Under different zein to curcumin (Cur) feeding ratios (10:1, 20:1, 30:1 and 40:1, w/w), the Cur-loaded zein-caseinate-pectin particles had a spherical shape with an average diameter ranging from 358.37 to 369.20 nm, a narrow size distribution (polydispersity index < 0.2) and a negative surface charge ranging from −18.87 to −19.53 mV. The relatively high encapsulation efficiencies of Cur (81.27% to 94.00%) and desirable re-dispersibility were also achieved. Fluorescence spectroscopy indicated that the encapsulated Cur interacted with carrier materials mainly through hydrophobic interactions. The in-vitro release profile showed a sustained release of Cur from zein-caseinate-pectin particles in acidic aqueous environment (pH 4) up to 24 h, without any burst effect. In addition, the encapsulation retained more ABTS•+ radical scavenging capacity of Cur during 4 weeks of storage. These results suggest that zein-caseinate-pectin particles may be used as a potential delivery system for lipophilic nutrients in acidic beverages.

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The role of hemolysate in the facilitation of oxyhemoglobin-induced contraction in rabbit basilar arteries

Journal of Neurosurgery ◽

10.3171/jns.1994.81.2.0261 ◽

1994 ◽

Vol 81 (2) ◽

pp. 261-266 ◽

Cited By ~ 35

Author(s):

Toshiki Aoki ◽

Katsunobu Takenaka ◽

Satoshi Suzuki ◽

Neal F. Kassell ◽

Oren Sagher ◽

...

Keyword(s):

Molecular Weight ◽

Contractile Response ◽

Weight Fraction ◽

Low Molecular Weight ◽

Equal Concentration ◽

Content Type ◽

Basilar Arteries ◽

Fine Print

✓ The importance of factors within hemolysate in modulating oxyhemoglobin (oxyHb)-induced contraction was examined in an in vitro model of rabbit basilar arteries. When the basilar arteries were exposed to purified oxyHb alone, the contractile response observed was significantly weaker than that seen in arteries exposed to hemolysate containing an equal concentration of oxyHb. In order to delineate the nature of the factors within hemolysate that facilitate contraction, hemolysate was fractionated, and various components were tested individually for their ability to elicit this effect. A low-molecular-weight fraction of hemolysate, ranging from 0.5 to 2.0 kD, elicited only a mild contraction. However, when this fraction was combined with purified oxyHb, the contractile response was comparable in magnitude to that of unfractionated hemolysate. These studies confirm that purified oxyHb is capable of inducing contraction in vitro. The data also demonstrate that oxyHb elicits a significantly weaker contraction than does hemolysate. In addition, the results suggest that low-molecular-weight components in hemolysate (in the 0.5- to 2.0-kD range), while incapable of inducing a potent contraction alone, may act in concert with oxyHb to elicit the vasoconstriction seen following subarachnoid hemorrhage.

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In-Vitro Characterization of Nanoparticles and Antiagregation Tests on Brown Seaweed Extracts (Sargassum polycystum) Types of Sellulase Enzyme Hydrolysis

JURNAL ILMU KEFARMASIAN INDONESIA ◽

10.35814/jifi.v17i2.720 ◽

2019 ◽

Vol 17 (2) ◽

pp. 164

Author(s):

Kartiningsih Kartiningsih ◽

Syamsudin Abdillah ◽

Partomuan Simanjuntak ◽

Cyntia Cyntia ◽

Haryo Haryo

Keyword(s):

Molecular Weight ◽

Brown Seaweed ◽

Spherical Shape ◽

Enzyme Hydrolysis ◽

Seaweed Extract ◽

Small Molecular Weight ◽

Quality Requirements ◽

Physical Quality ◽

Before And After

Brown seaweed contains fucoidan, a large molecular weight sulfate polysaccharide (about 100,000 Da) which has platelet antiagregation activity. This activity is achieved if the fucoidan has a small molecular weight (3900-7600 Da) so this activity can increase by hydrolized with sellulase Enzym. The purpose of this study was to obtain extract nanoparticles that meet physical quality requirements and have a higher platelet antiagregation activity than brown seaweed extract both before and after hydrolysis. Extraction was using kinetic maseration method using 80% ethanol after that using 2% calcium chloride solution. The results were dried and hydrolyzed with cellulase enzyme and nanoparticles were made by ionic gelation method. Nanoparticle characterization results in particle size of 552.8, polydispersity index of 0.569, potential zeta of +53.5 mV, and spherical shape. In-vitro testing results for platelet antiagregation activity showed the percentage of platelet aggregation inhibition of brown seaweed extract with a concentration 500µg / mL is 22.19% and extracts after hydrolysis was 57.94% and nanoparticles extract after hydrolysis was 72.93%. Extract nanoparticles meet physical quality requirements and extracted nanoparticles after hydrolysis have the highest platelet antiagregation activity compared to brown seaweed extract both before and after hydrolysis.

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STUDY ON THE INFLAMMATORY RESPONSE OF PMMA/POLYSTYRENE/SILICA NANOCOMPOSITE MEMBRANES FOR DRUG DELIVERY AND DENTAL APPLICATIONS

10.1101/499160 ◽

2018 ◽

Author(s):

Shanmuga Sundar Saravanabhavan ◽

KANNAN NATARAJAN ◽

Sundaravadivel Elumalai ◽

Sarang Zsolt ◽

Mukunthan K SELVAM ◽

...

Keyword(s):

Inflammatory Response ◽

Sol Gel ◽

Research Work ◽

Polymeric Materials ◽

Composite Membranes ◽

In Vitro Cytotoxicity ◽

Sem Images ◽

Equal Concentration ◽

Cytotoxicity Studies

Background The application of polymeric materials in medical industry has grown drastically in the last two decades due to their various advantages compared to existing materials. The present research work emphases on the sol-gel technique to formulate the polymethyl methyl acrylate/polystyrene/silica composite membrane. Methods The characteristic of the composite was investigated through modern state art of instrumentation. Results The functional groups attached to the polymer was absorbed by FTIR. The FTIR spectrum confirm that the blend was mixed thoroughly and the formation of unite intimately between the polymers. The membranes were observed by SEM for its surface homogeneity which depends upon the composition of the two blending polymers. The captured SEM images showed the formation of microcracks on the surface, which was evidently controlled by varying the constituent polymer ratios. The prepared blend membranes with 2:1 ratio of PMMA/PS/Si displayed higher water uptake compared to other blended membranes. The composite membranes had good hydroxyl apatite growth in SBF solution. Furthermore, the in vitro cytotoxicity studies carried out by MTT method, using RAW macrophage cells showed that all the samples exhibited excellent cell viability. Conclusion The inflammatory response of composite with equal concentration of PMMA-PS were performed and observed no inflammation in comparison with control and other tested concentrations.

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Physicochemical Properties and Biological Activities of Silver Carp Scale Peptide and Its Nanofiltration Fractions

Frontiers in Nutrition ◽

10.3389/fnut.2021.812443 ◽

2022 ◽

Vol 8 ◽

Author(s):

Xiao-yan Zu ◽

Ya-jing Zhao ◽

Shi-ming Fu ◽

Tao Liao ◽

Hai-lan Li ◽

...

Keyword(s):

Amino Acids ◽

Molecular Weight ◽

Physicochemical Properties ◽

Biological Activities ◽

Silver Carp ◽

Radical Scavenging ◽

Hydrophobic Amino Acids ◽

Radical Scavenging Ability ◽

Molecular Weight Fractions

To explore the physicochemical properties and biological functions of silver carp scale peptide (SCSP), its molecular-weight fractions SCSP-I, II, and III obtained by nanofiltration were assessed for their solubility, emulsibility, free radical scavenging ability, effect on the proliferation of mouse B16 cells. The results showed that the solubility of each fraction of SCSP was higher than 90%, SCSP-II and III were higher than 95%. The antioxidant powers on ⦁OH, O2-⦁ and Fe3+ were ranked as SCSP-III > SCSP-II > SCSP-I > SCSP. All fractions of SCSP had no toxic or side effects in mouse B16 melanoma cells experiments in vitro. At a concentration of 0.01 mg/mL, the tyrosinase activity of B16 cells in the SCSP-II fraction was significantly lower than that of the α-arbutin (P < 0.05), at 65.37%. The molecular weight distribution of SCSP was 399–1404 Dalton and 13 peptide sequences were detected. Among them, SCSP-II contained many hydrophobic amino acids, and SCSP-III stood out for combining arginine with hydrophobic amino acids. This may be the reason why the low molecular-weight SCSPs show the strong antioxidant activity and strong tyrosinase inhibition. The work provides a data base for the development of SCSP and increases the possibility of its application.

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Polyphenols and Alkaloids in Byproducts of Longan Fruits (Dimocarpus Longan Lour.) and Their Bioactivities

Molecules ◽

10.3390/molecules24061186 ◽

2019 ◽

Vol 24 (6) ◽

pp. 1186 ◽

Cited By ~ 8

Author(s):

Ya-Yuan Tang ◽

Xue-Mei He ◽

Jian Sun ◽

Chang-Bao Li ◽

Li Li ◽

...

Keyword(s):

High Performance ◽

Antioxidant Activities ◽

Radical Scavenging Activity ◽

Research Result ◽

Radical Scavenging ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Total Phenolic ◽

Functional Components

The longan industry produces a large amount of byproducts such as pericarp and seed, resulting in environmental pollution and resource wastage. The present study was performed to systematically evaluate functional components, i.e., polyphenols (phenolics and flavonoids) and alkaloids, in longan byproducts and their bioactivities, including antioxidant activities, nitrite scavenging activities in simulated gastric fluid and anti-hyperglycemic activities in vitro. Total phenolic and total flavonoid contents in pericarp were slightly higher than those in seeds, but seeds possessed higher alkaloid content than pericarp. Four polyphenolic substances, i.e., gallic acid, ethyl gallate, corilagin and ellagic acid, were identified and quantified using high-performance liquid chromatography. Among these polyphenolic components, corilagin was the major one in both pericarp and seed. Alkaloid extract in seed showed the highest DPPH radical scavenging activity and oxygen radical absorbance capacity. Nitrite scavenging activities were improved with extract concentration and reaction time increasing. Flavonoids in seed and alkaloids in pericarp had potential to be developed as anti-hyperglycemic agents. The research result was a good reference for exploring longan byproducts into various valuable health-care products.

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Taste Masking of Nizatidine Using Ion-Exchange Resins

Processes ◽

10.3390/pr7110779 ◽

2019 ◽

Vol 7 (11) ◽

pp. 779 ◽

Cited By ~ 2

Author(s):

Pattaraporn Panraksa ◽

Kasidech Boonsermsukcharoen ◽

Kyu-Mok Hwang ◽

Eun-Seok Park ◽

Pensak Jantrawut

Keyword(s):

Drug Release ◽

Bitter Taste ◽

Drug Loading ◽

Electronic Tongue ◽

Spherical Shape ◽

Batch Process ◽

Taste Masking ◽

Simulated Gastric Fluid ◽

Exchange Resins

The purpose of this study was to mask the bitter taste of nizatidine (NZD) using cation-exchange resins. Amberlite IRP-69 and Dowex-50 containing cross-linked polystyrene backbones were used. The drug resin complexes were prepared by batch process using drug: resin ratios of 1:1, 1:3, and 1:5. The optimum drug: resin ratio and the time required for maximum percentage drug loading into the complexes were determined. The selected drug-resin complexes were evaluated for morphology, drug release, and taste. The NZD-Dowex complex was obtained at a drug: resin ratio of 1:5 using a stirring time of 1 h in order to get 100% loading of NZD. The NZD-Dowex complex had a spherical shape and smooth texture similar to Dowex resin. The NZD-Dowex complex with a ratio of 1:5 showed that in vitro drug release of 4.27% at 5 min in simulated salivary fluid of pH 6.8 and 99.67% at 1 h in simulated gastric fluid of pH 1.2. NZD’s bitter taste was effectively masked when it formed a complex with Dowex at a ratio of 1:5. This was proved by an electronic tongue and human test panel.

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Preparation and Comparative Bioavailability Studies of Indomethacin-Loaded Cetyl Alcohol Microspheres

Journal of Pharmaceutics ◽

10.1155/2013/109837 ◽

2013 ◽

Vol 2013 ◽

pp. 1-9 ◽

Cited By ~ 1

Author(s):

N. Vishal Gupta ◽

D. V. Gowda ◽

V. Balamuralidhara ◽

M. S. Khan

Keyword(s):

Size Range ◽

Spherical Shape ◽

Cetyl Alcohol ◽

Pharmacokinetic Parameters ◽

Healthy Male ◽

Sem Images ◽

Comparative Bioavailability ◽

Extent Of Absorption

The purpose of the present study was to compare the in vitro release and to find out whether the bioavailability of a 75 mg indomethacin capsule (Microcid SR) was equivalent to optimized formulation (indomethacin-loaded cetyl alcohol microspheres). Indomethacin-loaded cetyl alcohol microspheres were prepared by meltable emulsified cooling-induced technique. Surface morphology of microspheres has been evaluated using scanning electron microscopy. A single dose, randomized, complete cross over study of IM microspheres was carried out on 10 healthy male and female Albino sheep’s under fasting conditions. The plasma was separated and the concentrations of the drug were determined by HPLC-UV method. Plasma indomethacin concentrations and other pharmacokinetic parameters obtained were statistically analyzed. The SEM images revealed the spherical shape of fat microspheres, and more than 98.0% of the isolated microspheres were in the size range 12–32 μm. DSC, FTIR spectroscopy and stability studies indicated that the drug after encapsulation with fat microspheres was stable and compatible. Both formulations were found to be bioequivalent as evidenced by in vivo studies. Based on this study, it can be concluded that cetyl alcohol microspheres and Microcid SR capsule are bioequivalent in terms of the rate and extent of absorption.

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Preparation, Characterization, and In Vitro Sustained Release Profile of Resveratrol-Loaded Silica Aerogel

Molecules ◽

10.3390/molecules25122752 ◽

2020 ◽

Vol 25 (12) ◽

pp. 2752 ◽

Cited By ~ 2

Author(s):

Lili Qin ◽

Yiwei He ◽

Xinyu Zhao ◽

Ting Zhang ◽

Yao Qin ◽

...

Keyword(s):

Silica Aerogel ◽

Low Cost ◽

Drug Carrier ◽

Sol Gel ◽

Gastric Fluid ◽

Ethanol Solution ◽

Simulated Gastric Fluid ◽

In Vitro Toxicity ◽

Sem Images

Silica aerogel, a kind of nanoporous material, is regarded as a desired drug carrier for its low toxicity, high specific surface area, and excellent biocompatibility. Using silica aerogel in a drug carrier may be an appropriate method to improve the performance of pure resveratrol. In this study, resveratrol-loaded silica aerogel (RSA) as a drug delivery system was prepared by the sol-gel method. Before gelling, resveratrol was added into the hydrolyzed tetraethyl orthosilicate (TEOS) ethanol solution then dispersed by stir and ultrasound. The results showed that RSA has a high loading rate of 19% with low cost and excellent biocompatibility. The SEM images showed that silica aerogel wraps up outside the resveratrol. Sustained releasing effect could be observed in RSA after 1 h, while pure resveratrol did not display this. The release of RSA lasted for over 6 h, and the release amount reached over 90% and 80% in either simulated gastric fluid (pH = 2.0) or phosphate-buffered saline (pH = 7.4) at 37 °C. Preliminary in vitro toxicity test revealed RSA to be biocompatible and stable; and when coupled with the anti-inflammatory effects of resveratrol, showed good potential for osteoarthritis treatment.

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