scholarly journals Development and Optimization of Epigallocatechin-3-Gallate (EGCG) Nano Phytosome Using Design of Experiment (DoE) and Their In Vivo Anti-Inflammatory Studies

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5453
Author(s):  
Mohammad H. Shariare ◽  
Kazi Afnan ◽  
Faria Iqbal ◽  
Mohammad A. Altamimi ◽  
Syed Rizwan Ahamad ◽  
...  

Inflammation is responsible for the development of many diseases that make up a significant cause of death. The purpose of the study was to develop a novel nanophytosomal preparation of epigallocatechin-3-gallate (EGCG) and egg phospholipid complex that has a lower particle size with higher drug loading capability, physical stability and anti-inflammatory activities. The impact of different factors and material characteristics on the average particle size was studied along with the drug loading of phytosome using design of experiment (DoE). The in vivo anti-inflammatory study was evaluated using a rat model to investigate the performance of EGCG nanophytosome. UHPLC results showed that 500 µg of EGCG were present in 1 mL of green tea extract. SEM data exhibited that phytosome (phospholipid-drug complex) was in the nanosize range, which was further evident from TEM data. Malvern Zetasizer data showed that the average particle size of the EGCG nanophytosome was in the range of 100–250 nm. High drug loading (up to 90%) was achieved with optimum addition rate, stirring temperature and phospholipid concentration. Stability study data suggest that no significant changes were observed in average particle size and drug loading of nanophytome. The in vivo anti-inflammatory study indicated a significant anti-inflammatory activity of green tea extract, pure EGCG and its phytosomal preparations (p ≤ 0.001) against acute paw edema.

2017 ◽  
Vol 6 (1) ◽  
pp. 32-38 ◽  
Author(s):  
Wara Dyah Pita Rengga ◽  
Arie Yufitasari ◽  
Wismoyo Adi

The synthesis of silver nanoparticles with micro size is highly required in antibacterial fields. The biorefinery material is highly potential as a bioreductor which is applied in the synthesis of nanoparticles. The bioreductor is made from green tea leaves extraction using aquadest to extract its active substance, the catechin which is derived from polyphenol. The polyphenol can reduce the synthesis of silver nanoparticles naturally. The result of FTIR analysis from green tea leaves extract containing polyphenol shown in the uptake functional groups is -OH group located in 3425 cm-1, C=O group located in 1635 cm-1, C=C group located in 1527, and 1442 cm-1 , and C-O group located in 1234 cm-1. The precursors of AgNO3 was used as the main synthetic material. The synthetic condition was resulted from the reaction between the extraction of green tea extract and AgNO3 as the precursors in the variation of synthetizing time. The heating process during synthesizing is done in 50 ?C along with stirring to foster the creation of silver nanoparticles. The analysis result of XRD shows that silver nanoparticles has the diffraction peaks in the angle of 2 theta that are 44.08, 64.40, and 77.51. The types of silver nanoparticles is Ag0 nanoparticles with face-centered cubic crystal structure. Based on TEM analysis, the size and particle size distribution can be determined using image J. The distribution shows that the longer synthesizing time, the bigger nanoparticles produced. With synthesizing times at 24 hours, 6 hours, 3 hours, and 2 hours produce average particle size of 26.4 nm; 9.2 nm; 8.4 nm; and 7.4 nm respectively.


Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 650
Author(s):  
Runqin Hao ◽  
Dong Li ◽  
Jie Zhang ◽  
Tifeng Jiao

Chromium (VI) is a ubiquitous groundwater contaminant and it is dangerous to both ecological and human health. Iron nanoparticles (nFe) have a large specific surface area and they are highly efficient in removing chromium (VI) from aqueous solution. However, since the traditional reductive synthesis of nFe is relatively expensive and often causes secondary pollution, it is necessary to develop a low-cost green synthetic method using plant extracts. Synthetic conditions are important for obtaining highly active chromium-removing nanomaterials. In this paper, a green tea extract was used to prepare nFe and the effects of synthetic conditions on subsequent remediation performance were investigated. The optimal conditions included a green tea extract/Fe2+ ratio of 1:2 (91.6%), a green tea extract temperature of 353 K (88.3%) and a synthetic temperature of 298 K (88.1%). Advanced material characterization techniques, including XPS, SEM-EDS, TEM, and Brunauer–Emmett–Teller (BET) confirmed that the average particle size was between 50–80 nm, with a specific surface area of 42.25 m2·g−1. Furthermore nFe had a core-shell structure, where Fe (0) constituted the core and a shell was composed of iron oxide. Finally, a mechanism for synthesizing nFe by green tea extract was proposed, providing a theoretical basis for optimized synthetic conditions for preparing nFe when using green tea extract.


2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.


2017 ◽  
Vol 6 (6) ◽  
pp. 517-526 ◽  
Author(s):  
Permender Rathee ◽  
Anjoo Kamboj ◽  
Shabir Sidhu

AbstractBackground:Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes. The study was undertaken to assess the influence of piperine on the pharmacokinetics and pharmacodynamics of nisoldipine nanoparticles in rats.Methods:Optimization studies of nanoparticles were performed using Taguchi L9 orthogonal array, and the nanoparticles were formulated by the precipitation method. The influence of piperine and nanoparticles was evaluated by means of in vivo kinetic and dynamic studies by oral administration in rats.Results:The entrapment efficiency, drug loading, ζ potential, and average particle size of optimized nisoldipine-piperine nanoparticles was 89.77±1.06%, 13.6±0.56%, −26.5 mV, and 132±7.21 nm, respectively. The in vitro release in 0.1 n HCl and 6.8 pH phosphate buffer was 96.9±0.48% and 98.3±0.26%, respectively. Pharmacokinetic studies showed a 4.9-fold increase in oral bioavailability and a >28.376±1.32% reduction in systemic blood pressure by using nanoparticles as compared to control (nisoldipine suspension) in Wistar rats.Conclusion:The results revealed that piperine being an inhibitor of cytochrome P4503A4 enzymes enhanced the bioavailability of nisoldipine by 4.9-fold in nanoparticles.


2013 ◽  
Vol 49 (2) ◽  
pp. 341-349 ◽  
Author(s):  
Tariq Mahmood ◽  
Naveed Akhtar ◽  
Barkat Ali Khan ◽  
Akhtar Rasul ◽  
Haji M. Shoaib Khan

Complex multiple emulsions have an excellent ability to fill large volumes of functional cosmetic agents. This study was aimed to encapsulate large volume of green tea in classical multiple emulsion and to compare its stability with a multiple emulsion without green tea extract. Multiple emulsions were developed using Cetyl dimethicone copolyol as lipophilic emulsifier and classic polysorbate-80 as hydrophilic emulsifier. Multiple emulsions were evaluated for various physicochemical aspects like conductivity, pH, microscopic analysis, rheology and these characteristics were followed for a period of 30 days in different storage conditions. In vitro and in vivo skin protection tests were also performed for both kinds of multiple emulsions i.e. with active (MeA) and without active (MeB). Both formulations showed comparable characteristics regarding various physicochemical characteristics in different storage conditions. Rheological analysis showed that formulations showed pseudo plastic behavior upon continuous shear stress. Results of in vitro and in vivo skin protection data have revealed that the active formulation has comparable skin protection effects to that of control formulation. It was presumed that stable multiple emulsions could be a promising choice for topical application of green tea but multiple emulsions presented in this study need improvement in the formula, concluded on the basis of pH, conductivity and apparent viscosity data.


Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.


2021 ◽  
Vol 13 (9) ◽  
pp. 1691-1698
Author(s):  
Hongzhe Liu ◽  
Kai Tong ◽  
Ziyi Zhong ◽  
Gang Wang

To explore the effect of hydrogen sulfide (H2S) drug-loaded nanoparticles (H2S-NPs) on the mTOR/STAT3 signaling pathway in rats and its mechanism on repair of spinal cord injury (SCI), a new H2S-NP (G16MPG-ADT) was prepared and synthesized. The rats were selected as the research objects to explore the mechanism of SCI repair. The G16MPG-ADT NPs were evaluated by average particle size (APS), dispersion coefficient (DC), drug loading content (DLC), drug loading efficacy (DLE), in vitro release (IV-R), and acute toxicity (AT). It was found that G16MPG-ADT nanoparticles had a uniform particle size distribution with a unimodal distribution, with an average particle size of 186.5 nm and a dispersion coefficient of 0.129; within the concentration range of 8~56 μg/L, there was a good linear relationship with the peak area; and the release rate of the nanoparticles within 16 h~32 h was higher than 50%. G16MPG-ADT NP injection treatment was performed on rats with SCI. Western blotting (WB) and immunofluorescence staining were adopted to analyze the expression levels of mammalian target of rapamycin (mTOR) and signal transducers and activators of transcription (STAT3) protein and the growth of neurites. It was found that G16MPG-ADT can increase mTOR and STAT3 protein levels and promote nerve growth after SCI. Finally, the Basso, Beattie and Bresnahan locomotor rating (BBB) score was to evaluate the recovery effect of rats after treatment. It was found that the recovery effect was excellent after G16MPG-ADT treatment. In summary, G16MPG-ADT has a good effect on SCI repair in rats and can be promoted in the clinic.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 589 ◽  
Author(s):  
Chang-baek Lim ◽  
Sharif Md Abuzar ◽  
Pankaj Ranjan Karn ◽  
Wonkyung Cho ◽  
Hee Jun Park ◽  
...  

Here, we aimed to prepare and optimize liposomal amphotericin B (AmB) while using the supercritical fluid of carbon dioxide (SCF-CO2) method and investigate the characteristics and pharmacokinetics of the SCF-CO2-processed liposomal AmB. Liposomes containing phospholipids, ascorbic acid (vit C), and cholesterol were prepared by the SCF-CO2 method at an optimized pressure and temperature; conventional liposomes were also prepared using the thin film hydration method and then compared with the SCF-CO2-processed-liposomes. The optimized formulation was evaluated by in vitro hemolysis tests on rat erythrocytes and in vivo pharmacokinetics after intravenous administration to Sprague-Dawley rats and compared with a marketed AmB micellar formulation, Fungizone®, and a liposomal formulation, AmBisome®. The results of the characterization studies demonstrated that the SCF-CO2-processed-liposomes were spherical particles with an average particle size of 137 nm (after homogenization) and drug encapsulation efficiency (EE) was about 90%. After freeze-drying, mean particle size, EE, and zeta potential were not significantly changed. The stability study of the liposomes showed that liposomal AmB that was prepared by the SCF method was stable over time. In vivo pharmacokinetics revealed that the SCF-CO2-processed-liposomes were bioequivalent to AmBisome®; the hemolytic test depicted less hematotoxicity than Fungizone®. Therefore, this method could serve as a potential alternative for preparing liposomal AmB for industrial applications.


2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
F. Piran ◽  
Z. Khoshkhoo ◽  
S. E. Hosseini ◽  
M. H. Azizi

Applying bioactive ingredients in the formulation of foods instead of artificial preservatives is problematic because bioactive ingredients are unstable and sensitive to environmental conditions. The present study aimed to control the antioxidant activity of green tea extract (GT) through encapsulating in chitosan nanoparticles (CS-NP). The synthesized nanoparticles were analyzed by using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), and X-ray diffraction (XRD). The encapsulation efficiency (EE), particle size, zeta potential, and polydispersity index (PDI) of GT-loaded CS-nanoparticles (CS-NP-GT) were assessed. Based on the results, the particle size and zeta potential related to the ratio of CS to GT of 1 : 0.5 were obtained as 135.43 ± 2.52 nm and 40.40 ± 0.2 mV, respectively. Furthermore, the results of FT-IR and XRD confirmed the validity of encapsulating GT in CS-NP. In addition, the antioxidant activity of GT increased after nanoencapsulation since the IC50 value of CS-NP-GT decreased to 6.13 ± 0.12 μg/ml. Finally, applying these particles for delivering GT polyphenols in foods is regarded as promising.


2017 ◽  
Vol 22 (2) ◽  
pp. 73
Author(s):  
Nining Sugihartini ◽  
Ratih Saridewi ◽  
Ulfa Ramdhani M ◽  
Fitri Rahmawanti ◽  
Sapto Yuliani ◽  
...  

Green tea extract cream contains epigallocatechin gallate (EGCG) as the active ingredient for anti-inflammatory. Epigallocatechin gallate is easyly oxidized and able to reduce its effectivity as an anti-inflammatory. Therefore, an addition of antioxidants in order to increase its stability is required. The purpose of this study was to determine the effect of adding the antioxidant Vitamin C on the effectivity of green tea extract as an anti-inflammatory. This study uses 6 groups of male mice strain BALB/C which were given treatment as follows: normal control, negative control, base cream, green tea extract (0.2%), Vitamin C cream (1%) and green tea extract cream with addition of Vitamin C. The anti-inflammatory activity was evaluated based on the expression of COX-2, inflammatory cells and the thickness of the epidermis in the skin tissue of mice after given crotton oil (0.1%) on the back for the induction of inflammation. After treatment cream for 3 days, mice were sacrificed for histopathological tissue preparations made with hematoxylin eosin staining and immunohistochemistry COX-2. Data were analyzed statistically with one way Anova followed by t-test to determine differences between groups at a significance level of 0.05. The test results indicate that cream of green tea extract is higher in decreasing inflammatory parameters in comparison with cream of Vitamin C, except in the thickness of epidermal parameter. Green tea extract cream with the addition of Vitamin C is higher in reducing inflammatory parameters than cream of green tea extract or cream of Vitamin C. The decline percentage of cells that express COX-2, inflammatory cells and the thickness of the epidermis in the each of groups were cream of green tea extract:57.95%;53.75%;34.83%, cream of Vitamin C:48.76%;34.96%;34.27%, cream of green tea extract and Vitamin C:61,89%;65,54%;46.30%, respectively. Based on the results of this study, it can be concluded that anti-inflammatory activity of green tea extract cream increased due to the addition of 1% vitamin C as an antioxidant.


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