scholarly journals Improving Bioavailability of Gallic Acid and Quercetin by Designing Polymeric Nanoparticle Formulation

2021 ◽  
Author(s):  
poournima shamrao Patil ◽  
Suresh Ganapati killedar
Keyword(s):  
Gallic Acid ◽  
Polymeric Nanoparticles ◽  
Fold Increase ◽  
Pharmacokinetic Parameters ◽  
Pomegranate Peel ◽  
Polymeric Nanoparticle ◽  
Pharmacokinetic Properties ◽  
Pomegranate Peel Extract ◽  
Pomegranate Fruit ◽  
Work Method

Abstract Objective The pharmacokinetic properties of encapsulated polyherbal nanoparticles (Gallic acid and quercetin nanoparticle) and polyherbal extract (Amla and pomegranate fruit peels) in normal and DMH-induced colorectal cancer in rats was examined in this work. Method Polyherbal nanoparticles such as Gallic acid isolated from amla fruit and quercetin from pomegranate peel extract formulated into polymeric nanoparticle by using probe sonicator and high pressure homogenization. Result In normal and DMH-induced rats, a pharmacokinetic study demonstrated that polyherbal nanoparticles had a typical sustained release profile with a 2-fold increase in bioavailability when compared to polyherbal extract. Based on serum–concentration profiles of polyherbal nanoparticles and polyherbal extract following oral administration, the pharmacokinetic parameters for polyherbal nanoparticles and polyherbal extract were established using a single compartmental approach. Conclusion This research suggests that encapsulating gallic acid and quercetin in polymeric nanoparticles improves oral bioavailability than polyherbal extract of amla and pomegranate peel. Polymeric nanoparticles could be a novel therapeutic possibility for carcinogenesis prevention.

scholarly journals In vitro anti-adenoviral activities of ethanol extract, fractions, and main phenolic compounds of pomegranate (Punica granatum L.) peel

2020 ◽  
Vol 28 ◽  
pp. 204020662091657
Author(s):  
Ali Karimi ◽  
Mohammad-Taghi Moradi ◽  
Mohammad Rabiei ◽  
Somayeh Alidadi
Keyword(s):  
Phenolic Compounds ◽  
Gallic Acid ◽  
Virus Replication ◽  
Ethanol Extract ◽  
Inhibitory Effect ◽  
Pomegranate Peel ◽  
Butanol Fraction ◽  
Pomegranate Peel Extract ◽  
Peel Extract

Background Adenovirus causes a number of diseases in human, and can cause serious infection in severely immunosuppressed individuals. Despite the seriousness of adenovirus infection, there is no definitely approved anti-adenoviral therapy. Many studies have shown that compounds derived from medicinal plants have antiviral activity. Therefore, this study evaluated in vitro anti-adenoviral activity of ethanol extract, fractions, and main phenolic compounds of pomegranate peel. Methods The ethanol extract of pomegranate peel was prepared with maceration method and fractionated by consecutive liquid/liquid partition. The cytotoxic and anti-adenovirus activities of the extract, fractions, and main phenolic compounds (ellagic acid, punicalagin and gallic acid) were evaluated on Hep-2 cell line using MTT assay. Inhibitory effect on adsorption and post-adsorption phases of the virus replication cycle was also evaluated. Results Pomegranate peel extract had a desirable effect against adenovirus with IC50 of 5.77 µg/mL and selectivity index of 49.9. Among the fractions and compounds, the n-butanol fraction and gallic acid had the highest anti-adenoviral activity with IC50 of 2.16 µg/mL and 4.67 µM and selectivity indices of 122.5 and 10.5, respectively. The crude extract, n-butanol fraction and gallic acid inhibited the virus replication in post-adsorption phase ( p <  0.01). Conclusion Pomegranate peel extract, especially its n-butanol fraction, could serve as a new promising anti-adenovirus agent due to high inhibitory effect against adenovirus replication. The effect of the n-butanol fraction may be related to the synergistic effect or other compounds of this fraction. Further understanding of the bioassay guided isolation of natural compounds of this fraction seems essential.

scholarly journals Comparative Pharmacokinetics of Gallic Acid, Protocatechuic Acid, and Quercitrin in Normal and Pyelonephritis Rats after Oral Administration of a Polygonum capitatum Extract

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3873 ◽  
Author(s):  
Yong Huang ◽  
Zuying Zhou ◽  
Wu Yang ◽  
Zipeng Gong ◽  
Yueting Li ◽  
...  
Keyword(s):  
Gallic Acid ◽  
Protocatechuic Acid ◽  
Ultra Performance Liquid Chromatography ◽  
Pharmacokinetic Parameters ◽  
Bioactive Constituents ◽  
Time Points ◽  
Pharmacokinetic Properties ◽  
Liquid Chromatography Tandem Mass ◽  
Tract Infections ◽  
Pharmacokinetic Behavior

Polygonum capitatum Buch.-Ham. ex D. Don is traditionally used by Hmong for the treatment of urinary tract infections and pyelonephritis. Information regarding the pharmacokinetic behavior of the extract in the condition of pyelonephritis is lacking. In the present study, we aimed to compare the pharmacokinetic properties of gallic acid (GA), protocatechuic acid (PCA), and quercitrin (QR)—the main bioactive constituents in the herb—in normal and pyelonephritis rats. The plasma samples were collected at various time points after administration of a single dose of Polygonum capitatum extract. The plasma level of GA, PCA, and QR at the designed time points was determined by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) and drug concentration versus time plots were constructed to estimate the pharmacokinetic parameters. The AUC(0-t), AUC(0-∞), MRT(0-t), and CL of GA, PCA, and QR in pyelonephritis rats was significantly different from those of the normal rats. The results indicated that the three constituents have higher rate of uptake and slower rate of elimination in the rats with pyelonephritis, suggesting altered rate and extent of drug metabolism.

scholarly journals Gallic Acid Content and Antioxidant Activity of Pomegranate Peel Ethanol Extract

2020 ◽  
Vol 52 (4) ◽  
Author(s):  
Diah Dhianawaty ◽  
Latifah Rahman Nurfazriah ◽  
Andri Rezano
Keyword(s):  
Cell Proliferation ◽  
Antioxidant Activity ◽  
Gallic Acid ◽  
Acid Content ◽  
High Performance ◽  
Ethanol Extract ◽  
Antitumor Effects ◽  
Pomegranate Peel ◽  
Chromatography Method ◽  
Pomegranate Peel Extract

Ethanol extract of Pomegranate peel is proven to have the ability to inhibit the proliferation of cervical cancer HeLa cells. It was reported that this extract contains ellagic acid, gallic acid, and punicalagin which are identified as major effectors of antitumor activity. Gallic acid has been demonstrated to have an antioxidant activity that can influence cancer cell proliferation. The aim of the study was to identify the gallic acid content in pomegranate peel ethanol extract and to measure its antioxidant. This study was an experimental study performed at the Biochemistry and Molecular Biology Laboratory and Central Laboratory of Universitas Padjadjaran Bandung, Indonesia during September-December 2019. Gallic acid concentration was measured by using a high-performance liquid chromatography method (HPLC) and the antioxidant activity was measured by using 1,1-diphenyl-2-picrylhydrazyl (DPPH). The extract contained 616.97 mg/kg of gallic acid with an antioxidant activity of IC50 6.1 µg/mL. In conclusion, gallic acid has cytotoxic and antitumor effects from its ability to modulate antioxidant/pro-oxidant balance and inhibit reactive oxygen species (ROS). Therefore, both gallic acid content and antioxidant activity parameters can be used as markers in pomegranate peel extract which shows activities that inhibit HeLa cell proliferation.

Polymeric Nanoparticles for Brain Drug Delivery - A Review

2020 ◽  
Vol 21 (9) ◽  
pp. 649-660
Author(s):  
Subashini Raman ◽  
Syed Mahmood ◽  
Ayah R. Hilles ◽  
Md Noushad Javed ◽  
Motia Azmana ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Surface Modification ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Preparation Methods ◽  
Brain Drug Delivery ◽  
Polymeric Nanoparticle ◽  
Relationship Of ◽  
The Relationship ◽  
The Brain

Background: Blood-brain barrier (BBB) plays a most hindering role in drug delivery to the brain. Recent research comes out with the nanoparticles approach, is continuously working towards improving the delivery to the brain. Currently, polymeric nanoparticle is extensively involved in many therapies for spatial and temporal targeted areas delivery. Methods: We did a non-systematic review, and the literature was searched in Google, Science Direct and PubMed. An overview is provided for the formulation of polymeric nanoparticles using different methods, effect of surface modification on the nanoparticle properties with types of polymeric nanoparticles and preparation methods. An account of different nanomedicine employed with therapeutic agent to cross the BBB alone with biodistribution of the drugs. Results: We found that various types of polymeric nanoparticle systems are available and they prosper in delivering the therapeutic amount of the drug to the targeted area. The effect of physicochemical properties on nanoformulation includes change in their size, shape, elasticity, surface charge and hydrophobicity. Surface modification of polymers or nanocarriers is also vital in the formulation of nanoparticles to enhance targeting efficiency to the brain. Conclusion: More standardized methods for the preparation of nanoparticles and to assess the relationship of surface modification on drug delivery. While the preparation and its output like drug loading, particle size, and charge, permeation is always conflicted, so it requires more attention for the acceptance of nanoparticles for brain delivery.

Preparation and Biochemical Evaluation of Functionalized Multi-Walled Carbon Nanotubes with Punica granatum Extract

2019 ◽  
Vol 15 (1) ◽  
pp. 138-144 ◽  
Author(s):  
Ahmed A. Haroun ◽  
Abdel-Tawab H. Mossa ◽  
Samia M.M. Mohafrash
Keyword(s):  
Liver Enzymes ◽  
Histopathological Analysis ◽  
Pomegranate Peel ◽  
Liver And Kidney ◽  
Multi Walled Carbon Nanotubes ◽  
Pomegranate Peel Extract ◽  
Walled Carbon Nanotubes ◽  
Functionalized Mwcnts ◽  
Peel Extract

Background: Funcionalized multi-walled carbon nanotubes (ox-MWCNTs) were used for the preparation of therapeutic nanoparticles for delivery of some bioactive compounds. Consequently, this work deals with the preparation of grafted MWCNTs with n-vinyl caprolactam in the presence of pomegranate peel extract (P. granatum), titanium dioxide (TiO2) and/or silver nanoparticeles and their toxic effects on male mice using in vivo biological examination (liver and kidney dysfunction biomarkers) and the histopathological analysis. Methods: P. granatum extract was immobilized onto functionalized MWCNTs using simple adsorption technique. Moreover, The prepared materials were analyzed by Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM). In vivo examination using liver and kidney dysfunction biomarkers was investigated. In addition, the histopathological study was carried out. Results: The ox-MWCNTs induced significant elevation in the liver enzymes including AST, ALT and ALP relative to the control group. While, the treatment with P. granatum extract only did not induce any change in the liver and kidney biomarkers. In other words, P. granatum extract loaded onto functionalized MWCNTs showed low effects on liver enzymes and kidney function biomarkers in the treated mice in comparison with ox-MWCNTs and extract separately. Moreover, histopathological analysis revealed that the P. granatum extract functionalized MWCNTs exhibited normal renal tissue with no histopathological alteration. Conclusion: The grafted MWCNTs with n-vinyl caprolactam in the presence of pomegranate peel extract (P. granatum), titanium dioxide (TiO2) and/or silver nanoparticeles were successfully prepared. SEM-micrographs showed complete coating of MWCNTs fiber with the extract. The prepared materials resulted in no toxic effects and the histopathological findings were confirmed by inflammation of the liver and kidney tissues.

Revealing changes in curcumin bioavailability using vitamin C as an enhancer by HPLC-MS/MS

2019 ◽  
Vol 16 ◽  
Author(s):  
Xufen Dai ◽  
Jiaxue Hao ◽  
Ying Feng ◽  
Jing Wang ◽  
Qiannan Li ◽  
...  
Keyword(s):  
Vitamin C ◽  
High Performance ◽  
Internal Standard ◽  
Fold Increase ◽  
Rat Plasma ◽  
Pharmacokinetic Parameters ◽  
Solution Ph ◽  
Esi Ms ◽  
Simple Strategy ◽  
Isolated Compound

Background: Curcumin (CUR), a natural isolated compound from turmeric, has been the promising star in fighting many diseases but the broad application of curcumin has been limited ascribed to low bioavailability. Objective: The aim of this study is to pursue the enhancement of curcumin bioavailability through co-administration of vitamin C. Methods: Such purpose was achieved through the analysis of curcumin pharmacokinetics by high performance liquid chromatography coupled with electrospray ionization - tandem mass spectrometry (HPLC - ESI - MS/MS). The plasma was separated on a C18 reverse phase column using acetonitrile and ammonium formate solution (pH 6.5; 2.0 mM) at 0.8 mL/min. MS/MS detection was carried out in negative mode using mass patterns of m/z 367.0 > 216.7 for curcumin and m/z 265.2 > 223.9 for internal standard (honokiol). Results: Successful application of the proposed method in the pharmacokinetic study presented clear changes in key pharmacokinetic parameters including the growth of AUC (0-t) up to 2.4 times, 2.2-fold increase of Cmax, 2.2-fold loss of CL, and 1.5-fold diminishment of t1/2. Conclusion: We developed an HPLC-ESI-MS/MS method for determination of curcumin in rat plasma and validated the improvement of bioavailability of curcumin through co-administration of vitamin C. We reasoned these changes to the inhibition of lipid peroxidation induced by the use of vitamin C. Such a simple strategy is possible to become an alternative for enhancing curcumin efficiency in practice.

Novel Applications of Nanotechnology in Controlling HIV and HSV Infections

2020 ◽  
Vol 12 ◽  
Author(s):  
Sai Akilesh M ◽  
Ashish Wadhwani
Keyword(s):  
Drug Delivery ◽  
Viral Infections ◽  
Polymeric Nanoparticles ◽  
Volume Ratio ◽  
Fold Increase ◽  
Multi Drug Resistance ◽  
Health Crisis ◽  
Pharmaceutical Properties ◽  
Simplex Virus ◽  
The Impact

: Infectious diseases have been prevalent since many decades and viral pathogens have caused global health crisis and economic meltdown on a devastating scale. High occurrence of newer viral infections in the recent years, in spite of the progress achieved in the field of pharmaceutical sciences defines the critical need for newer and more effective antiviral therapies and diagnostics. The incidence of multi-drug resistance and adverse effects due to the prolonged use of anti-viral therapy is also a major concern. Nanotechnology offers a cutting edge platform for the development of novel compounds and formulations for biomedical applications. The unique properties of nano-based materials can be attributed to the multi-fold increase in the surface to volume ratio at the nano-scale, tunable surface properties of charge and chemical moieties. Idealistic pharmaceutical properties such as increased bioavailability and retention times, lower toxicity profiles, sustained release formulations, lower dosage forms and most importantly, targeted drug delivery can be achieved through the approach of nanotechnology. The extensively researched nano-based materials are metal and polymeric nanoparticles, dendrimers and micelles, nano-drug delivery vesicles, liposomes and lipid based nanoparticles. In this review article, the impact of nanotechnology on the treatment of Human Immunodeficiency Virus (HIV) and Herpes Simplex Virus (HSV) viral infections during the last decade are outlined.

Sargassum fusiforme together with turmeric extract and pomegranate peel extract alleviates obesity in high fat-fed C57BL/6J mice

2021 ◽  
Author(s):  
Sainan Zhou ◽  
Qing Zhang ◽  
Yuan Gao ◽  
Fang Liu ◽  
Wanxiu Cao ◽  
...  
Keyword(s):  
Intestinal Flora ◽  
Obese Mice ◽  
High Fat ◽  
Pomegranate Peel ◽  
Fat Accumulation ◽  
Sargassum Fusiforme ◽  
Turmeric Extract ◽  
Pomegranate Peel Extract ◽  
Peel Extract

Sargassum fusiforme together with the turmeric extract and pomegranate peel extract may effectively reduce fat accumulation and improve the disorder of intestinal flora in obese mice.

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