Characterisation of Preformulation Parameters to Design, Develop and Formulate Silymarin loaded PLGA Nanoparticles for Liver Targeted Drug Delivery

2021 ◽  
pp. 5508-5514
Author(s):  
Senthila S ◽  
Manojkumar P. ◽  
Venkatesan P.
Keyword(s):  
Water Solubility ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Chemical Properties ◽  
Water Soluble ◽  
Angle Of Repose ◽  
Effect Of Temperature ◽  
Pharmacokinetic Studies ◽  
Bioavailability Enhancement ◽  
Water Soluble Compound

Silymarin, a flavonolignan,derived from Silybum marianum, family Asteraceae has long been used as a hepatoprotective remedy. Silymarin has cytoprotective activities due to its antioxidant property and free radical scavenging activity. It inhibits the binding of hepatotoxins to receptor sites, protects hepatocyte membranes, enhances liver parenchyma regeneration and increases glutathione levels. The pharmacokinetic studies of past three decades revealed that Silymarin has poor absorption, rapid metabolism especially by Phase II metabolism and ultimately poor oral bioavailability. Typical oral adult dose of Silymarin is 240-800mg /day .It is a non-lipophilic and poorly water soluble compound with water solubility of 0.04mg/ml. Only 20-30% of oral Silymarin is absorbed from gastrointestinal tract where it undergoes extensive entero-hepatic circulation. The advanced type of formulation like polymeric nanoparticles (PNPs) can be successfully utilised for bioavailability enhancement and targeting the Silymarin to hepatocytes. A controlled release PNP of Silymarin was prepared by solvent evaporation method using Poly Lactic-co-Glycolic Acid (PLGA) as biodegradable polymer. Prior to the development of this novel dosage form, it is very important to identify fundamental physical and chemical properties of the drug molecule and other divided properties of the drug powder. This data helps in many of the subsequent events and approaches towards the development of a better formulation. Preformulation studies included determination of solubility, moisture content, partition coefficient, melting point , powder properties like tapped density, bulk density, compressibility index, flow properties like angle of repose, excipient compatibility, entrapment efficiency, release profile of nanoparticles like dissolution, stability studies like effect of temperature and humidity and analysis by scanning Electron Microscopy.

scholarly journals Curcumin-Functionalized Gelatin Films: Antioxidant Materials with Modulated Physico-Chemical Properties

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1824
Author(s):  
Katia Rubini ◽  
Elisa Boanini ◽  
Silvia Parmeggiani ◽  
Adriana Bigi
Keyword(s):  
Water Solubility ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Crosslinking Agent ◽  
Radical Scavenging ◽  
Chemical Properties ◽  
Mechanical Tests ◽  
Scanning Calorimetry ◽  
Gelatin Films ◽  
Physico Chemical

In this paper we used curcumin as a functionalizing agent of gelatin films with the aim to get antioxidant materials with modulated physico-chemical properties. To this aim, we prepared gelatin films at different contents of curcumin up to about 1.2 wt%. The as-prepared films, as well as glutaraldehyde crosslinked films, were submitted to several tests: swelling, water solubility, differential scanning calorimetry, X-ray diffraction, mechanical tests and curcumin release. The radical scavenging activity of the as-prepared films is similar to that of free curcumin, indicating remarkable antioxidant properties. All the other tested properties vary as a function of curcumin content and/or the presence of the crosslinking agent. In particular, the films exhibit sustained curcumin release in different solvents. Thanks to its biocompatibility, biodegradability and lack of antigenicity, gelatin uses span from food processing to packaging and biomaterials. It follows that the modulated properties exhibited by the functionalized materials developed in this work can be usefully employed in different application fields.

scholarly journals Purification, Characterization, Prebiotic Preparations and Antioxidant Activity of Oligosaccharides from Mulberries

Molecules ◽  
2019 ◽  
Vol 24 (12) ◽  
pp. 2329 ◽  
Author(s):  
Erna Li ◽  
Shiyuan Yang ◽  
Yuxiao Zou ◽  
Weiwei Cheng ◽  
Bing Li ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Average Molecular Weight ◽  
Radical Scavenging ◽  
Lactobacillus Rhamnosus ◽  
Gel Permeation Chromatography ◽  
Water Soluble ◽  
Gas Chromatography Mass Spectrometry ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Antioxidant Power

A water-soluble oligosaccharide termed EMOS-1a was prepared by enzymatic hydrolysis of polysaccharides purified from mulberries by column chromatography. The chemical structure of the purified fraction was investigated by ultraviolet spectroscopy, Fourier-transform infrared spectroscopy, and gas chromatography–mass spectrometry, which indicated that galactose was the main constituent of EMOS-1a. Chemical analyses showed that the uronic acid and sulfate content of EMOS-1a were 5.6% and 8.35%, respectively, while gel permeation chromatography showed that EMOS-1a had an average molecular weight of 987 Da. The antioxidant activities of EMOS-1a were next investigated, and EMOS-1a exhibited concentration-dependent 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, Trolox equivalent antioxidant capacity, and ferric reducing antioxidant power. The level of proliferation of Lactobacillus rhamnosus reached 1420 ± 16% when 4% (w/v) EMOS-1a was added, where the number of colonies in MRS (de Man, Rogosa, and Sharpe) medium with no added oligosaccharide was defined as 100% proliferation. These results indicate that the oligosaccharide EMOS-1a could be used as a natural antioxidant in prebiotic preparations.

scholarly journals Changes in Metabolisms of Antioxidant and Cell Wall in Three Pummelo Cultivars during Postharvest Storage

Biomolecules ◽  
2019 ◽  
Vol 9 (8) ◽  
pp. 319 ◽  
Author(s):  
Liu ◽  
Liang ◽  
Jiang ◽  
Chen
Keyword(s):  
Cell Wall ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Pectate Lyase ◽  
Water Soluble ◽  
Scavenging Activity ◽  
Total Phenols ◽  
Postharvest Storage ◽  
Total Antioxidant ◽  
Juice Sacs

The juice sacs of pummelo fruit is susceptible to softening during storage at 25 °C, which causes quality deterioration and flavor loss during postharvest pummelo storage. This study investigated the changes in metabolisms of antioxidant and cell wall in juice sacs of three pummelo cultivars—Hongroumiyou (HR), Bairoumiyou (BR) and Huangroumiyou (HuR)—during postharvest storage. The results revealed that, with the extension of storage, the juice sacs of three pummelo cultivars exhibited a decrease in total antioxidant capacity (TAC), DPPH and ABTS radical scavenging activity; a decline in total phenols (TP) content and an increase firstly then a decrease in total ascorbic acid (TAA) content; and a decrease in lipoxygenase (LOX) activity and a rise initially, but a decline in activities of ascorbate peroxidase (APX) and glutathione peroxidase (GPX). Additionally, increased water-soluble pectin (WSP), but declined propectin, ionic-soluble pectin (ISP) and chelator-soluble pectin (CSP); as well as an increase from 0 d to 60 d then followed by a decline in activities of pectinesterase (PE), polygalacturonase (PG) and pectate lyase (PL) were observed. These results suggested that the metabolisms of antioxidant and cell wall could result in softening and senescence of pummelo fruit.

scholarly journals Chitooligosaccharides from squid pen prepared using different enzymes: characteristics and the effect on quality of surimi gel during refrigerated storage

2019 ◽  
Vol 1 (1) ◽  
Author(s):  
Avtar Singh ◽  
Soottawat Benjakul ◽  
Thummanoon Prodpran
Keyword(s):  
Microbial Growth ◽  
Water Solubility ◽  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Radical Scavenging Activity ◽  
Average Molecular Weight ◽  
Radical Scavenging ◽  
Refrigerated Storage ◽  
Surimi Gel

Abstract Chitooligosaccharides (COS) from squid pen produced using amylase, lipase and pepsin were characterized. COS produced by 8% (w/w) lipase (COS-L) showed the maximum FRAP and ABTS radical scavenging activity than those prepared using other two enzymes. COS-L had the average molecular weight (MW) of 79 kDa, intrinsic viscosity of 0.41 dL/g and water solubility of 49%. DPPH, ABTS radical scavenging activities, FRAP and ORAC of COS-L were 5.68, 322.68, 5.66 and 42.20 μmol TE/g sample, respectively. Metal chelating activity was 2.58 μmol EE/g sample. For antibacterial activity, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of COS-L against the targeted bacteria were in the range of 0.31–4.91 mg/mL and 0.62–4.91 mg/mL, respectively. Sardine surimi gel added with 1% (w/w) COS-L showed the lower PV, TBARS and microbial growth during 10 days of storage at 4 °C. COS-L from squid pen could inhibit lipid oxidation and extend the shelf-life of refrigerated sardine surimi gel. Graphical abstract

In Vitro Antioxidant Activities of Polysaccharides from Auricularia auriada

2011 ◽  
Vol 183-185 ◽  
pp. 104-109
Author(s):  
Ning Zhang ◽  
Zhen Yu Wang ◽  
Hua Zhang ◽  
Jian Ren ◽  
Xiu Mei Hao
Keyword(s):  
Hydrogen Peroxide ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Water Soluble ◽  
Peroxide Radical ◽  
Scavenging Effect ◽  
Radical Scavenging Effect ◽  
Chelating Ability

This study aims to evaluate the antioxidative activities of water and alkaline solution pH=8, 50% ethanolic (APP1 or SAPP1), 75% ethanolic (APP2 or SAPP2) and 100% ethanolic (APP3 or SAPP3) extracts of A. auricular. The antioxidant activities, including the ABTS, superoxide anion radical-scavenging effect, hydrogen peroxide radical-scavenging effect and chelating ability on ferrous ions were studied in vitro. A comparison of the 50% effective concentration (EC50) values of different antioxidative reactions revealed that SAPP3 was more effective in scavenging ABTS, hydrogen peroxide and chelating ability on ferrous ions.SAPP2 showed a higher superoxide radical-scavenging activity. The alkali-soluble polysaccharides extracts showed higher radical-scavenging effect than water-soluble polysaccharides.

scholarly journals Degradation kinetics during storage of vitamins and antioxidants in coconut powder

DYNA ◽  
2020 ◽  
Vol 87 (213) ◽  
pp. 61-68
Author(s):  
Juan Carlos Lucas Aguirre ◽  
German Antonio Giraldo Giraldo ◽  
Misael Cortés Rodríguez
Keyword(s):  
Antioxidant Activity ◽  
Storage Temperature ◽  
Degradation Kinetics ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Storage Conditions ◽  
Treatment Temperature ◽  
Effect Of Temperature ◽  
Order Kinetic ◽  
Degradation Kinetic

Degradation kinetic parameters in vitamins and antioxidants in coconut powder fortified with functionally active compounds (CP+FAC) during storage represents a valuable tool to predict the product’s shelf life. The aim of this research was to evaluate the degradation kinetics during storage of vitamins (C, D3, and E), total phenols, and properties associated to antioxidant activity. Vitamins were quantified via high-resolution liquid chromatography and the antioxidant activity through DPPH and ABTS free radical scavenging activity. An experimental design was used with two-factor factorial design: 1) storage time (tS) and 2) treatment: temperature (TA) - type of packaging (N2 and atmospheric air), where the dependent variables were adjusted to zero-, first-, and second-order kinetic models. In general, losses of FAC were significant with respect to the factors evaluated and their interactions, with minor changes at lower TA and packaged with N2, indicating that the degradation kinetics of the FAC is slower under these storage conditions. Increased storage temperature reduced FACstability, where the Arrhenius equation was able to quantify the effect of temperature of the rate of deterioration reactions of the FAC.

scholarly journals The changes of chemical quality of ginger during postharvest storage at chilling temperature

Food Research ◽  
2020 ◽  
Vol 4 (5) ◽  
pp. 1653-1662
Author(s):  
N.I.A. Shukor ◽  
A. Misran ◽  
S.H. Ahmad ◽  
Y.T. Xue ◽  
T.M.M. Mahmud ◽  
...  
Keyword(s):  
Storage Temperature ◽  
Radical Scavenging Activity ◽  
Chilling Injury ◽  
Radical Scavenging ◽  
Chemical Properties ◽  
Temperature Management ◽  
Total Phenolic ◽  
Scavenging Activity ◽  
Fresh Weight ◽  
And Storage

Zingiber officinale is a tropical produce which is susceptible to chilling injury due to improper storage temperature management. Therefore, the objective of the study was to investigate the development of chilling injury (CI) in ‘Bentong’ ginger rhizome. Fresh ‘Bentong’ ginger rhizomes were harvested at 9-10 months and were stored at 5, 15 and 25°C for 0, 8, 16, and 24 days. The treatments were evaluated for the effects of storage temperatures and storage durations on postharvest chemical qualities of ginger rhizomes. The experiment showed significant interaction effects between storage temperature and storage durations for total flavonoid contents (TFC), total phenolic contents (TPC), 6- gingerol, 6-shogaol, and DPPH radical scavenging activity of the treated rhizome. Ginger stored at 15°C showed the highest TPC at 16 days of storage and then reduced throughout the storage as compared to the ginger stored at 5°C and 25°C. The 6-gingerol content increased from day 0 to day 16 and resulted in an optimum content at 66.7 mg/g fresh weight when it was stored at 15°C. 6-shogaol was identified in smaller quantities within the range of 1.52 to 3.11 mg/100 g of fresh weight. A similar trend was also observed in 6 -shogoal after 24 days of the storage. DPPH scavenging activity showed that storage at 5 and 25°C resulted in a decrease of DPPH inhibition along with storage durations. Therefore, it was suggested that the ginger was best kept at 15°C up to 16 days of storage in order to maintain the postharvest qualities and chemical properties of ginger.

scholarly journals Synthesis of a novel green carbon dots as a bioimaging agent and a drug delivery system for enhanced antioxidant and antibacterial efficacy

2020 ◽  
Author(s):  
Neeraj Tejwan ◽  
Mousumi Kundu ◽  
Anirudh Sharma ◽  
Joydeep Das ◽  
Parames C Sil
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Carbon Dots ◽  
Radical Scavenging Activity ◽  
Drug Loading ◽  
Radical Scavenging ◽  
Water Soluble ◽  
Root Extract ◽  
Scavenging Activity

Abstract Background Now-a-days, synthesis of carbon dots (CDs) from renewable sources has attracted considerable attention due to their wide spread availability, lower cost, higher aqueous solubility and more biocompatibility. Here, we have synthesized water soluble CDs from the root extract of red Korean ginseng via simple microwave irradiation. The CDs were further loaded with a natural flavonoid, rutin, to check its efficacy as a drug delivery system. Result The CDs showed a size distribution between 1–4 nm and excitation-dependent fluorescence emission, and could be used as a bio-imaging agent.The CDs showed a drug loading content of 14% and a sustained drug release behavior at physiological conditions. CDs showed excellent free radical scavenging activity both in cell free systems and intra-cellular conditions. Besides, loading with the drug further improved the intra-cellular radical scavenging activity. The CDs and the nanohybrids also showed very little toxicity upto the concentration of 100 µg/mL in normal kidney epithelial cells. The CDs and the nanohybrids also showed a dose-dependent antibacterial effect against both gram negative as well as gram positive bacteria. Conclusion Our synthesized green CDs can be considered as a promising candidate for the biomedical applications due to its facile synthesis, low cytotoxicity, excellent fluorescent properties and potential as drug delivery systems.

scholarly journals Bioactive chemical constituents, acute toxicity and 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity of Polyalthia longifolia root

2021 ◽  
Vol 14 (1) ◽  
pp. 018-026
Author(s):  
Charles Akhadelor Unuigbe ◽  
Chinem Fumi Unula ◽  
Anthony Aiwonegbe ◽  
Jeremiah Ogboma Uadia ◽  
Isaac Akhigbe ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Ethyl Acetate ◽  
Methanol Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Water Soluble ◽  
Total Phenolic ◽  
Scavenging Activity ◽  
Polyalthia Longifolia ◽  
Crude Methanol Extract

Polyalthia longifolia (masquerade tree) is a plant which is believed to possess varied pharmacological and therapeutic values among different populations. The present report investigated the phytochemical composition, proximate, acute toxicity and antioxidant potential of P. longfolia root. All analyses were carried out using established methods; the antioxidant activity of the crude methanol extract and its fractions (n-hexane and ethyl acetate) were examined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay while the total phenolic and flavonoid contents were assessed using the Folin-Ciocalteu and the aluminum chloride calibration methods respectively. The phytochemical analysis revealed the presence of alkaloids, carbohydrate, reducing sugars, tannins, saponins, flavonoids, phenolic compounds and protein in aqueous extract. The proximate analysis showed moisture content, total ash, alcohol extractive value, water extractive value, acid insoluble ash and water soluble ash at 8.80, 9.35, 3.28, 3.29, 2.27 and 7.29% respectively. The ethyl acetate fraction showed the highest antioxidant property compared to the n-hexane fraction and crude methanol extract in all assays conducted. Also, the methanol fraction was found to have the highest flavonoids and phenolic content among the extract and fractions. Oral administration of crude methanol extract of P. longifolia to Swiss mice was relatively non-toxic at a maximum dose of 5000 mg/kg. The root extract and fractions of P. longifolia indicated moderately high level of some phytochemicals with outstanding radical scavenging activity, and therefore substantiate its use as a conventional and comparatively non-toxic plant antioxidant.

Sign in / Sign up

Export Citation Format

Share Document