scholarly journals Synthesis, Characterization, and Evaluation of Radical Scavenging Ability of Ellagic Acid-Loaded Nanogels

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Gautam Behl ◽  
Monal Sharma ◽  
Saurabh Dahiya ◽  
Aruna Chhikara ◽  
Madhu Chopra
Keyword(s):  
Ellagic Acid ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Radical Scavenging ◽  
Aqueous Solubility ◽  
Loading Level ◽  
Human Cervical Cancer Cell ◽  
Poly Ethylene ◽  
Radical Scavenging Ability ◽  
Acid Loading

Ellagic acid (EA), a potential antioxidant phytochemical has low aqueous solubility and bioavailability. In this paper, encapsulation of ellagic acid has been carried out into the biodegradable disulfide crosslinked poly (ethylene glycol) PEO-based nanogels synthesized via AGET (activator generated electron transfer) ATRP (atom transfer radical polymerization), and their radical scavenging ability was evaluated. The encapsulation of the EA was carried out at two drug loading percentages, that is, 10 and 20 wt.% of the nanogels. 1,1-Diphenyl-2-picryldrazyl (DPPH) assay was utilized in order to assess the radical scavenging ability of the ellagic acid-loaded nanogels. A drug-loading level of about 2.5 wt.% was achieved with encapsulation efficiency of about 25% at 10 wt.% of the EA w.r.t nanogels, which was found to increase to about 4.7 wt.% with decreased encapsulation efficiency of 23.5% as EA content was increased to 20wt.% of the nanogels. Ellagic acid loading was found to be accompanied with increase in the size of the nanogels from144.6±39.52 nm for neat nanogels to217.8±105.5and633±160.1 nm at 2.5 and 4.7 wt.% drug loading level. The nanogels were found to be capable of scavenging radicals and biocompatible on human cervical cancer cell lines (HeLa cells) at appropriate concentrations.

scholarly journals Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1688 ◽  
Author(s):  
Vieri Piazzini ◽  
Mario D’Ambrosio ◽  
Cristina Luceri ◽  
Lorenzo Cinci ◽  
Elisa Landucci ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Oral Absorption ◽  
Drug Loading ◽  
Antioxidant Properties ◽  
Aqueous Solubility ◽  
Average Diameter ◽  
Critical Micellar Concentration ◽  
Polydispersity Index ◽  
Vitamin E Tpgs

Two novel nanomicellar formulations were developed to improve the poor aqueous solubility and the oral absorption of silymarin. Polymeric nanomicelles made of Soluplus and mixed nanomicelles combining Soluplus with d-α-tocopherol polyethylene glycol 1000 succinate (vitamin E TPGS) were prepared using the thin film method. Physicochemical parameters were investigated, in particular the average diameter, the homogeneity (expressed as polydispersity index), the zeta potential, the morphology, the encapsulation efficiency, the drug loading, the critical micellar concentration and the cloud point. The sizes of ~60 nm, the narrow size distribution (polydispersity index ≤0.1) and the encapsulation efficiency >92% indicated the high affinity between silymarin and the core of the nanomicelles. Solubility studies demonstrated that the solubility of silymarin increased by ~6-fold when loaded into nanomicelles. Furthermore, the physical and chemical parameters of SLM-loaded formulations stored at room temperature and in refrigerated conditions (4 °C) were monitored over three months. In vitro stability and release studies in media miming the physiological conditions were also performed. In addition, both formulations did not alter the antioxidant properties of silymarin as evidenced by the 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH) assay. The potential of the nanomicelles to increase the intestinal absorption of silymarin was firstly investigated by the parallel artificial membrane permeability assay. Subsequently, transport studies employing Caco-2 cell line demonstrated that mixed nanomicelles statistically enhanced the permeability of silymarin compared to polymeric nanomicelles and unformulated extract. Finally, the uptake studies indicated that both nanomicellar formulations entered into Caco-2 cells via energy-dependent mechanisms.

Poly(lactide-co-glycolide)-Methoxy-Poly(ethylene glycol) Nanoparticles: Drug Loading and Release Properties

2006 ◽  
Vol 6 (9) ◽  
pp. 3080-3086 ◽  
Author(s):  
Georgia Katsikogianni ◽  
Konstantinos Avgoustakis
Keyword(s):  
Drug Loading ◽  
Double Emulsion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Molar Ratio ◽  
Nanoparticle Preparation ◽  
Physical Entrapment ◽  
Poly Ethylene ◽  
Phosphate Buffered Saline

In this work, the drug loading and in vitro release properties of PLGA-mPEG nanoparticles were studied. Three methyl-xanthine derivatives differing significantly in aqueous solubility, i.e., caffeine, theophylline, and theobromine, were employed as model drugs. Two different PLGA-mPEG copolymer compositions, namely PLGA(40)mPEG(5) and PLGA(136)mPEG(5), were included in the study. The nanoparticles were prepared by a double emulsion technique. The drug release properties of the nanoparticles in phosphate buffered saline (PBS) and in human plasma were determined. An increase of the drug proportion in the feed led to increased drug loading. The composition of the PLGA-mPEG copolymer (PLGA/mPEG molar ratio) did not appear to affect drug loading and encapsulation. Caffeine exhibited higher loading in the nanoparticles than theobromine and this exhibited a little higher loading than theophylline. Solid-state solubility of the drug in PLGA-mPEG did not affect drug loading. Drug loading and encapsulation in the PLGA-mPEG nanoparticles appeared to be governed by the partition coefficient of the drug between the organic phase and the external aqueous phase employed in nanoparticle preparation. Relatively low loading and encapsulation values were obtained, suggesting that the physical entrapment of drugs in PLGA-mPEG nanoparticles could only be an option in the development of formulations of potent drugs. Only the release of the least water-soluble theobromine was efficiently sustained by its entrapment in the nanoparticles, indicating that the physical entrapment of drugs provides the means for the development of controlled-release PLGA-mPEG nanoparticulate formulations only in the case of drugs with low aqueous solubility.

scholarly journals Preparation of Silymarin–quercetin Loaded Nanoparticles by Spontaneous Emulsification Solvent Diffusion Method Using D-alpha-tocopheryl Poly (Ethylene Glycol) 1000 Succinate

2021 ◽  
pp. 84-94
Author(s):  
S. Senthila ◽  
P. Manoj Kumar ◽  
P. Venkatesan
Keyword(s):  
Electron Microscopy ◽  
Drug Release ◽  
Ethylene Glycol ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Release Profile ◽  
Poly Ethylene Glycol ◽  
Drug Release Profile ◽  
Spontaneous Emulsification ◽  
Poly Ethylene

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. 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. Quercetin, a flavonoid present in edible vegetables and fruits, It is a potent antioxidant and shows a wide range of biological functions. Quercetin improves blood levels and efficacy of number of drugs since it is P-Glycoprotein inhibitor and also inhibits drug metabolizing enzymes. Both silymarin and quercetin were, poorly soluble in the water shows low bioavailability. The advanced type of formulation like polymeric nanoparticles (PNPs) can be successfully utilised for bioavailability enhancement and targeting the Silymarin-quercetin to hepatocytes. A controlled release PNPs of silymarin-quercetin were prepared by spontaneous emulsification solvent diffusion (SESD) method using Poly Lactic-co-Glycolic Acid (PLGA) as biodegradable polymer, D-alpha-tocopheryl poly (ethylene glycol) 1000 succinate (TPGS) used as a solubilizer, as an emulsifier. TPGS as an emulsifier and further as a matrix material blended with PLGA was used to enhance the encapsulation efficiency and improve the drug release profile of nanoparticles. Different formulations with various drug: polymer ratios and volume and concentration of surfactant, centrifugation time were evaluated. The effect of formulation parameters such as drug/polymer ratio, volume and surfactant content were evaluated. The surface morphology and size of the nanoparticles were studied by scanning electron microscopy (SEM) Transmission electron microscopy (TEM). Drug encapsulation efficiency and in vitro drug release profiles of nanoparticles were determined using UV spectrophotometry. The nanoparticles prepared with combination of both the drugs in this study were spherical with size range of 100–200 nm. It was shown that TPGS was a good emulsifier for producing nanoparticles of hydrophobic drugs and improving the encapsulation efficiency and drug loading and drug release profile of nanoparticles. Although the amount of the TPGS used had a significant effect on the nanoparticle size and morphology, the drug loading and release profile of nanoparticles

Encapsulation of Ellagic Acid in Di-Block Copolymeric Micelle for Non-Small Cell Lung Cancer Therapy

2021 ◽  
Vol 13 (1) ◽  
pp. 66-72
Author(s):  
Serag Eldin I. Elbehairi ◽  
Mohammad Y. Alfaifi ◽  
Ali A. Shati ◽  
Usama A. Fahmy ◽  
Bapi Gorain ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Ellagic Acid ◽  
Polymeric Micelles ◽  
A549 Cells ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Polymeric Micelle ◽  
Lung Adenocarcinoma Cell Line ◽  
Lung Cancer Therapy ◽  
Poly Ethylene

Ellagic acid (EA) is an anticancer agent as evidenced in numerous pre-clinical studies. The clinical application of EA is limited because of its poor aqueous solubility and bioavailability. The present study was designed to formulate polymeric micelles of the drug using poly(L-lactide-co-glycolide)-poly (ethylene glycol) (PLGA-PEG) di-block copolymer. The particle size and entrapment efficiency of EA by the polymeric micelle were found to be dependent on the concentration of polymer. Consequently, optimized micellar formulations with 82 ± 7.1 nm size and 45.32 ± 5.43% drug entrapment were further evaluated for cytotoxicity, cell cycle arrest, and apoptotic potential in the human lung adenocarcinoma cell line, A549. EA was toxic to A549 cells, and this cytotoxicity was significantly increased when EA was delivered using a micellar formulation. Flow cytometry analysis revealed a superior G1 phase arresting potential of the optimized EA-loaded PLGA-PEG micelles (PLGA-PEG-EA-F3), with a concomitant increased apoptotic potential. Further investigation of the mechanism of apoptosis showed a significant overexpression of caspase-3 in A549 cells when treated with PLGA-PEG-EA-F3 compared to free EA. Thus, it can be concluded that the PLGA-PEG polymeric micellar platform for EA could be a potential tool to treat lung cancer.

scholarly journals Antioxidant capacity and antioxidants of strawberry, blackberry, and raspberry leaves

2011 ◽  
Vol 29 (No. 2) ◽  
pp. 181-189 ◽  
Author(s):  
L. Buřičová ◽  
M. Andjelkovic ◽  
A. Čermáková ◽  
Z. Réblová ◽  
O. Jurček ◽  
...  
Keyword(s):  
Antioxidant Capacity ◽  
Ellagic Acid ◽  
Radical Scavenging ◽  
Water Extract ◽  
Rubus Idaeus ◽  
Total Phenolic ◽  
Water Extracts ◽  
Antioxidant Capacities ◽  
Dpph Method ◽  
Radical Scavenging Ability

The total phenolic content (Folin-Ciocalteu method), free radical scavenging ability expressed as DPPH value, ferric reducing antioxidant capacity (FRAP), and oxygen radical absorbance capacity (ORAC) were determined in water extracts of leaves from Rosaceae family plants (Fragaria vesca L., Rubus fructicosus L., and Rubus idaeus L.). The antioxidant capacities of the extracts (in the order of the above mentioned methods) were 73.6–88.9%, 60.1–71.4%, 49.7–78.0% respectively, and 45.3–66.5% of that of green tea water extract. Further, the presence of 15 compounds (gallic acid, rutin, ellagic acid, caffeic acid, p-coumaric acid, quercetin, kaempferol, myricetin, quercetin-3-d-glucoside, ascorbic acid, (+)-catechin, (–)-epicatechin, epicatechingallate, epigallocatechin, procyanidin B1) was studied by HPLC-ECD and their antioxidant capacities were compared to the antioxidant capacity of the extracts. Out of the compounds studied, mostly (+)-catechin, ellagic acid, and (–)-epicatechin participated in the antioxidant capacities of the studied plant leaves water extracts. The antioxidant capacity of leaves infusions (determined by DPPH method) was lower than those of red wines and tea infusions, but comparable to the antioxidant capacities of white wines and fruit beverages.

PHARMACOGNOSTIC, ANTIOXIDANT AND ACUTE TOXICITY STUDY OF Ficus sycomorus (Linn) (Moraceae) ROOT AND STEM BARK

2020 ◽  
Vol 4 (2) ◽  
pp. 605-614
Author(s):  
Murtala M. Namadina ◽  
H. Haruna ◽  
U. Sanusi
Keyword(s):  
Acute Toxicity ◽  
Radical Scavenging ◽  
Stem Bark ◽  
The Body ◽  
Toxicity Study ◽  
Bark Extract ◽  
Root Extract ◽  
Acute Toxicity Study ◽  
Radical Scavenging Ability ◽  
Phytochemical Components

Most of biochemical reactions in the body generates Reactive Oxygen Species (ROS), which are involved in the pathogenesis of oxidative stress-related disorders like diabetes, nephrotoxicity, cancer, cardiovascular disorders, inflammation and neurological disorders when they attack biochemical molecules like proteins, lipids and nucleic acid. Antioxidants are used to protect the cells or tissues against potential attack by ROS. Most medicinal plants possess a rich source of antioxidants such as flavonoids, phenols, tannins, alkaloids among others. These phytochemicals are currently pursued as an alternative and complimentary drug. In this study, phytochemical components, antioxidant and acute toxicity study of the methanol extract of stem bark and root of F. sycomorus were carried out using standard methods. Findings from this study revealed the presence of some diagnostic microscopical features such as calcium oxalate, starch, gum/mucilage, lignin, Aleurone grain, suberized/Cuticular cell wall and inulin but calcium carbonate was absent in stem bark but present in the powdered root. Quantitative physical constants include moisture contents (6.40% and 7.82%), ash value (7.20% and 9.30 %) in stem bark and root respectively. Carbohydrates, alkaloid, flavonoids, saponins, tannins, glycoside, steroid, triterpenes and phenols were present in all the extracts. They were found to exhibit potent 1,1,-diphenyl 2-picryl hydrazyl (DPPH) free scavenging activity. The DPPH radical scavenging ability of the extracts showed the following trend Ascorbic acid < stem bark extract˃ root extract. The LD50 of the methanolic stem bark and root extracts were found to be greater than 5000 mg /kg and is considered safe for use. Nonetheless, further

scholarly journals Preparation of Antioxidant and Antibacterial Chitosan Film from Periplaneta americana

Insects ◽  
2021 ◽  
Vol 12 (1) ◽  
pp. 53
Author(s):  
Sicong Chen ◽  
Xunfan Wei ◽  
Zhuoxiao Sui ◽  
Mengyuan Guo ◽  
Jin Geng ◽  
...  
Keyword(s):  
Food Packaging ◽  
Periplaneta Americana ◽  
Uv Light ◽  
Radical Scavenging ◽  
Chitosan Film ◽  
American Cockroach ◽  
Raw Material ◽  
Potential Resource ◽  
Radical Scavenging Ability ◽  
Dpph Radical Scavenging

Among different insects, the American cockroach (Periplaneta americana) has been bred in industrial scale successfully as a potential resource of protein, lipid, and antibacterial peptide. However, the application of its chitosan has not been studied widely, which has hindered the sufficient utilization of P. americana. In this paper, the chitosan from P. americana was separated, characterized, and processed into film (PaCSF) to examine its potential of being applied in food packaging. As the results of different characterizations showed, PaCSF was similar to shrimp chitosan film (SCSF). However, concerning the performances relating to food packaging, the two chitosan films were different. PaCSF contained more water (42.82%) than SCSF did, resulting in its larger thickness (0.08 mm). PaCSF could resist UV light more effectively than SCSF did. Concerning antioxidant activity, the DPPH radical scavenging ability of PaCSF increased linearly with time passing, reaching 72.46% after 8 h, which was better than that of SCSF. The antibacterial activity assay exhibited that PaCSF resisted the growth of Serratia marcescens and Escherichia coli more effectively than SCSF did. The results implied that P. americana chitosan could be a potential raw material for food packaging, providing a new way to develop P. americana.

scholarly journals Tailoring Atomoxetine Release Rate from DLP 3D-Printed Tablets Using Artificial Neural Networks: Influence of Tablet Thickness and Drug Loading

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 111
Author(s):  
Gordana Stanojević ◽  
Djordje Medarević ◽  
Ivana Adamov ◽  
Nikola Pešić ◽  
Jovana Kovačević ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Release Rate ◽  
Drug Loading ◽  
Prolonged Release ◽  
Cylindrical Shape ◽  
Poly Ethylene Glycol ◽  
Scanning Calorimetry ◽  
3D Printed ◽  
Artificial Neural ◽  
Poly Ethylene

Various three-dimensional printing (3DP) technologies have been investigated so far in relation to their potential to produce customizable medicines and medical devices. The aim of this study was to examine the possibility of tailoring drug release rates from immediate to prolonged release by varying the tablet thickness and the drug loading, as well as to develop artificial neural network (ANN) predictive models for atomoxetine (ATH) release rate from DLP 3D-printed tablets. Photoreactive mixtures were comprised of poly(ethylene glycol) diacrylate (PEGDA) and poly(ethylene glycol) 400 in a constant ratio of 3:1, water, photoinitiator and ATH as a model drug whose content was varied from 5% to 20% (w/w). Designed 3D models of cylindrical shape tablets were of constant diameter, but different thickness. A series of tablets with doses ranging from 2.06 mg to 37.48 mg, exhibiting immediate- and modified-release profiles were successfully fabricated, confirming the potential of this technology in manufacturing dosage forms on demand, with the possibility to adjust the dose and release behavior by varying drug loading and dimensions of tablets. DSC (differential scanning calorimetry), XRPD (X-ray powder diffraction) and microscopic analysis showed that ATH remained in a crystalline form in tablets, while FTIR spectroscopy confirmed that no interactions occurred between ATH and polymers.

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