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Polyphenols and their Nanoformulations: Challenges and Opportunities

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A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (15 February 2023) | Viewed by 15503

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Dr. Carolina Sánchez-Rodríguez

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Guest Editor

Center for Research in Health and Life Sciences, European University of Madrid, 28670 Villaviciosa de Odon, Madrid, Spain
Interests: polyphenols; age-related hearing loss (ARHL); aging; oxidative stress; apoptosis; nanomedicine; head and neck cancer

Special Issue Information

Dear Colleagues,

I am Guest Editing a Special Issue for the journal Pharmaceuticals on “Polyphenols and their Nanoformulations: Challenges and Opportunities”.

Polyphenols are food constituents rich in a number of phenolic units. Polyphenols are commonly used in maintaining good health and in disease prevention. Among different possible experimental approaches, the study of the effect of several polyphenols has been active in the last decade due to i) a wide range of biological actions including their anti-oxidant, anti-inflammatory, anti-cancer, and anti-microbial properties; and ii) their great abundance in the diet and their role in the prevention of various diseases. In fact, a continuous and optimal intake of polyphenols has been associated with a lower incidence of cancer, inflammation, obesity, diabetes, cardiovascular disease (CVD), cognitive disorders, and aging. The mechanisms of action of polyphenols may be direct or indirect. However, the use of polyphenols in humans is limited by many factors, such as poor permeability, instability, low solubility, low bioavailability, and rapid release. In order to overcome these limitations, polyphenols can be loaded into carriers to enhance their bioavailability. Nanocarriers, as excellent drug delivery systems, can overcome these limitations and maximize the pharmacological effects of polyphenols. In recent years, many nanoparticles have been developed for the delivery of polyphenolic compounds, including liposomes, phospholipid complexes, niosomes, protein-based nanoparticles, micelles, emulsions and metal nanoparticles.

This Special Issue aims to highlight the following topics: (a) benefits and safety of polyphenols; (b) protective effects of polyphenols in acute and chronic diseases, including obesity, neurodegenerative diseases, type 2 diabetes, cardiovascular diseases, cancer, and others; (c) potential application of polyphenol nanoparticles in food and medicine; (d) potential harmful effects of some polyphenols; (e) implications of food processing on the bioavailability of polyphenols, the health claims and marketing of polyphenols as a functional food; and (f) the need for increased regulation and guidelines for polyphenol consumption and supplementation.

Dr. Carolina Sánchez-Rodríguez
Guest Editor

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Keywords

polyphenols
oxidative stress
dietary antioxidants
aging
prevention
adverse effects/drug interactions of polyphenols
polyphenols nanoformulations
nanoparticles

Published Papers (7 papers)

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Research

17 pages, 5071 KiB

Open AccessArticle

Can Resveratrol Influence the Activity of 11β-Hydroxysteroid Dehydrogenase Type 1? A Combined In Silico and In Vivo Study

by Jurica Novak, Vadim E. Tseilikman, Olga B. Tseilikman, Svetlana S. Lazuko, Lyudmila E. Belyeva, Azam Rahmani and Julia Fedotova

Pharmaceuticals 2023, 16(2), 251; https://doi.org/10.3390/ph16020251 - 07 Feb 2023

Cited by 2 | Viewed by 1459

Abstract

The enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) is an NADPH-dependent reductase, responsible for the activation of cortisol by reducing cortisone. Resveratrol (RES), a type of natural polyphenol, is reported to be able to slow the progression of cancer and cardiovascular disease and improve the health of mice on a high-calorie diet. In this article, we applied molecular docking and molecular dynamics simulations to investigate the possibility of binding RES to 11β-HSD-1. The 11β-HSD-1:RES complex is stable on the μs time scale, and backbone RMSD-based clustering identified three conformations. Special attention was paid to the interaction pattern between the ligand and the target molecule, revealing hydrogen bonds between the hydroxyl group of RES and Thr124, as well as hydrophobic interactions responsible for the binding. In vivo studies demonstrated the ability of resveratrol at a dose of 40 mg/kg to reduce 11β-HSD-1 activity in the liver of rats under conditions of experimental post-traumatic stress disorder (PTSD), as well as in non-stressed animals. In both cases, the resveratrol-induced reduction in 11β-HSD-1 activity was accompanied by an increase in plasma corticosterone levels and a decrease in anxiety levels in the plus maze test. Full article

(This article belongs to the Special Issue Polyphenols and their Nanoformulations: Challenges and Opportunities)

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24 pages, 29011 KiB

Open AccessArticle

The Physicochemical and Antimicrobial Properties of Silver/Gold Nanoparticles Obtained by “Green Synthesis” from Willow Bark and Their Formulations as Potential Innovative Pharmaceutical Substances

by Roxana Colette Sandulovici, Mihailescu Carmen-Marinela, Alexandru Grigoroiu, Carmen Aura Moldovan, Mihaela Savin, Viorel Ordeanu, Sorina Nicoleta Voicu, Daniel Cord, Gabriela Mariana Costache, Mona Luciana Galatanu, Mariana Popescu, Iulian Sarbu, Erand Mati, Lucia Elena Ionescu, Răzvan Neagu, Vasilica Ţucureanu, Rîmbu Mirela Claudia, Iuliana Mihalache, Cosmin Romanitan, Alice Piperea-Sianu, Adina Boldeiu, Oana Brincoveanu, Carmen Elisabeta Manea, Bogdan Firtat, George Stelian Muscalu and David Dragomir Show full author list Hide full author list

Pharmaceuticals 2023, 16(1), 48; https://doi.org/10.3390/ph16010048 - 29 Dec 2022

Cited by 5 | Viewed by 2679

Abstract

Green chemistry is a pharmaceutical industry tool, which, when implemented correctly, can lead to a minimization in resource consumption and waste. An aqueous extract of Salix alba L. was employed for the efficient and rapid synthesis of silver/gold particle nanostructures via an inexpensive, nontoxic and eco-friendly procedure. The nanoparticles were physicochemically characterized using ultraviolet–visible spectroscopy (UV–Vis), Fourier transform infrared spectroscopy (FT-IR), dynamic light scattering (DLS), X-ray diffraction (XRD) and scanning electron microscopy (SEM), with the best stability of up to one year in the solution obtained for silver nanoparticles without any chemical additives. A comparison of the antimicrobial effect of silver/gold nanoparticles and their formulations (hydrogels, ointments, aqueous solutions) showed that both metallic nanoparticles have antibacterial and antibiofilm effects, with silver-based hydrogels having particularly high antibiofilm efficiency. The highest antibacterial and antibiofilm efficacies were obtained against Pseudomonas aeruginosa when using silver nanoparticle hydrogels, with antibiofilm efficacies of over 75% registered. The hydrogels incorporating green nanoparticles displayed a 200% increased bacterial efficiency when compared to the controls and their components. All silver nanoparticle formulations were ecologically obtained by “green synthesis” and were shown to have an antimicrobial effect or potential as keratinocyte-acting pharmaceutical substances for ameliorating infectious psoriasis wounds. Full article

(This article belongs to the Special Issue Polyphenols and their Nanoformulations: Challenges and Opportunities)

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24 pages, 5245 KiB

Open AccessArticle

Protective Effects of Naringin–Dextrin Nanoformula against Chemically Induced Hepatocellular Carcinoma in Wistar Rats: Roles of Oxidative Stress, Inflammation, Cell Apoptosis, and Proliferation

by Eman E. Mohamed, Osama M. Ahmed, Adel Abdel-Moneim, Khairy M. A. Zoheir, Basem H. Elesawy, Ahmad Al Askary, Ahmed Hassaballa and Ahmed A. G. El-Shahawy

Pharmaceuticals 2022, 15(12), 1558; https://doi.org/10.3390/ph15121558 - 14 Dec 2022

Cited by 4 | Viewed by 1870

Abstract

Nanotechnology holds great promise for the development of treatments for deadly human diseases, such as hepatocellular carcinoma (HCC). In the current study, we compared the hepatoprotective effects of naringin–dextrin nanoparticles (NDNPs) against HCC in male Wistar rats with those of pure naringin and investigated the underlying cellular and molecular mechanisms. HCC was induced by intraperitoneal injection of diethylnitrosamine (DEN, 150 mg/kg body weight (b.w.) per week) for two weeks, followed by oral administration of 2-acetylaminofluorene (2AAF, 20 mg/kg b.w.) four times per week for three weeks. DEN/2AAF-administered rats were divided into three groups that respectively received 1% carboxymethyl cellulose (as vehicle), 10 mg/kg b.w. naringin, or 10 mg/kg b.w. NDNP every other day by oral gavage for 24 weeks. Both naringin and NDNP significantly attenuated the harmful effects of DEN on liver function. Both compounds also suppressed tumorigenesis as indicated by the reduced serum concentrations of liver tumor markers, and this antitumor effect was confirmed by histopathological evaluation. Additionally, naringin and NDNP prevented DEN-induced changes in hepatic oxidative stress and antioxidant activities. In addition, naringin and NDNP suppressed inflammation induced by DEN. Moreover, naringin and NDNP significantly reduced the hepatic expression of Bcl-2 and increased Bax, p53, and PDCD5 expressions. Naringin and NDNP also reduced expression of IQGAP1, IQGAP3, Ras signaling, and Ki-67 while increasing expression of IQGAP2. Notably, NDNP more effectively mitigated oxidative stress and inflammatory signaling than free naringin and demonstrated improved antitumor efficacy, suggesting that this nanoformulation improves bioavailability within nascent tumor sites. Full article

(This article belongs to the Special Issue Polyphenols and their Nanoformulations: Challenges and Opportunities)

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16 pages, 5362 KiB

Open AccessArticle

Comparative Cytotoxic Evaluation of Zygophyllum album Root and Aerial Parts of Different Extracts and Their Biosynthesized Silver Nanoparticles on Lung A549 and Prostate PC-3 Cancer Cell Lines

by Reda F. A. Abdelhameed, Mohamed S. Nafie, Dina M. Hal, Ali M. Nasr, Shady A. Swidan, Maged S. Abdel-Kader, Amany K. Ibrahim, Safwat A. Ahmed, Jihan M. Badr and Enas E. Eltamany

Pharmaceuticals 2022, 15(11), 1334; https://doi.org/10.3390/ph15111334 - 28 Oct 2022

Cited by 4 | Viewed by 1693

Abstract

The current work demonstrates a comparative study between aerial and root parts of Zygophyllum album L. The total phenolic (TPC) and flavonoid content (TFC), in addition to the antioxidant activity, of the crude extracts were investigated, where the aerial parts revealed a higher value overall. By means of UV–VIS and HPLC, rutin and caffeic acid were detected and then quantified as 5.91 and 0.97 mg/g of the plant extract, respectively. Moreover, the biosynthesis of AgNPs utilizing the crude extract of the arial parts and root of Z. album L. and the phenolic extracts was achieved in an attempt to enhance the cytotoxicity of the different plant extracts. The prepared AgNPs formulations were characterized by TEM and zeta potential measurements, which revealed that all of the formulated AgNPs were of a small particle diameter and were highly stable. The mean hydrodynamic particle size ranged from 67.11 to 80.04 nm, while the zeta potential ranged from 29.1 to 38.6 mV. Upon biosynthesis of the AgNPs using the extracts, the cytotoxicity of the tested samples was improved, so the polyphenolics AgNPs of the aerial parts exhibited a potent cytotoxicity against lung A549 and prostate PC-3 cancer cells with IC₅₀ values of 6.1 and 4.36 µg/mL, respectively, compared with Doxorubicin (IC₅₀ values of 6.19 and 5.13 µg/mL, respectively). Regarding the apoptotic activity, polyphenolics AgNPs of the aerial parts induced apoptotic cell death by 4.2-fold in PC-3 and 4.7-fold in A549 cells compared with the untreated control. The mechanism of apoptosis in both cancerous cells appeared to be via the upregulation proapoptotic genes; p53, Bax, caspase 3, 8, and 9, and the downregulation of antiapoptotic gene, Bcl-2. Hence, this formula may serve as a good source for anticancer agents against PC-3 and A549 cells. Full article

(This article belongs to the Special Issue Polyphenols and their Nanoformulations: Challenges and Opportunities)

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28 pages, 8086 KiB

Open AccessArticle

Nanoparticulate System for the Transdermal Delivery of Catechin as an Antihypercholesterol: In Vitro and In Vivo Evaluations

by Soraya Ratnawulan Mita, Marline Abdassah, Unang Supratman, Yoshihito Shiono, Driyanti Rahayu, Iyan Sopyan and Gofarana Wilar

Pharmaceuticals 2022, 15(9), 1142; https://doi.org/10.3390/ph15091142 - 13 Sep 2022

Cited by 6 | Viewed by 1923

Abstract

Gambir (Uncaria gambir, Roxb.) contains catechins that is often empirically used to treat various diseases. Catechins can reduce cholesterol levels by inhibiting coenzyme HMG-CoA reductase that plays a role in cholesterol metabolism. Research has been carried out covering the optimization of transethosomal catechins, the formulation of Transethosomal Catechin Gel (TCG) and Non-Transethosomal Catechin Gel (NTCG), which were then tested for catechin permeation from these gel preparations in vitro using Franz’s diffusion cell with PTFE membranes. The anti-hypercholesterol activity test was carried out with Simvastatin orally as a positive control using 25 male Wistar rats (Rattus norvegicus). The catechin transetosomes have a size of 176.1 ± 5.8 nm, Zeta potential −11.6 ± 5.28, and Entrapment Efficacy of 96.77% ± 0.05. The result of cumulative catechins that permeated from TCG and NTCG were and 172.454 ± 5.287 and 112.741 ± 2.241 μg respectively. Permeation test graphs showed similar permeation and flux profiles. TCG can reduce total cholesterol and LDL (Low Density Lipoprotein) values in rats by 39.77% and 51.52% respectively during 14 days of use. Full article

(This article belongs to the Special Issue Polyphenols and their Nanoformulations: Challenges and Opportunities)

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18 pages, 3228 KiB

Open AccessArticle

Targeting Acne Bacteria and Wound Healing In Vitro Using Plectranthus aliciae, Rosmarinic Acid, and Tetracycline Gold Nanoparticles

by Isa A. Lambrechts, Velaphi C. Thipe, Kattesh V. Katti, Vusani Mandiwana, Michel Lonji Kalombo, Suprakas Sinha Ray, Rirhandzu Rikhotso, Arno Janse van Vuuren, Tenille Esmear and Namrita Lall

Pharmaceuticals 2022, 15(8), 933; https://doi.org/10.3390/ph15080933 - 28 Jul 2022

Cited by 7 | Viewed by 2564

Abstract

Gold nanoparticles from plant extracts and their bioactive compounds to treat various maladies have become an area of interest to many researchers. Acne vulgaris is an inflammatory disease of the pilosebaceous unit caused by the opportunistic bacteria Cutibacterium acnes and Staphylococcus epidermis. These bacteria are not only associated with inflammatory acne but also with prosthetic-implant-associated infections and wounds. Studies have hypothesised that these bacteria have a mutualistic relationship and act as a multispecies system. It is believed that these bacteria form a multispecies biofilm under various conditions and that these biofilms contribute to increased antibiotic resistance compared to single-species biofilms. This study aimed to investigate the antibacterial and wound healing potential of synthesised gold nanoparticles (AuNP_s) from an endemic South African plant, Plectranthus aliciae (AuNP_PAE), its major compound rosmarinic acid (AuNP_RA) and a widely used antibiotic, tetracycline (AuNP_TET). Synthesised gold nanoparticles were successfully formed and characterised using ultraviolet–visible spectroscopy (UV–vis), dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), zeta potential (ζ-potential), high-resolution transmission electron microscopy (HRTEM), and selected area electron diffraction (SAED), and they were investigated for stability under various biological conditions. Stable nanoparticles were formed with ζ-potentials of −18.07 ± 0.95 mV (AuNP_PAE), −21.5 ± 2.66 mV (AuNP_RA), and −39.83 ± 1.6 mV (AuNP_TET). The average diameter of the AuNP_s was 71.26 ± 0.44 nm, 29.88 ± 3.30 nm, and 132.6 ± 99.5 nm for AuNP_PAE, AuNP_RA, and AuNP_TET, respectively. In vitro, biological studies confirmed that although no antibacterial activity or biofilm inhibition was observed for the nanoparticles tested on the multispecies C. acnes and S. epidermis systems, these samples had potential wound closure activity. Gold nanoparticles formed with rosmarinic acid significantly increased wound closure by 21.4% at 25% v/v (≈29.2 µg/mL) compared to the negative cell control and the rosmarinic acid compound at the highest concentration tested of 500 µg/mL. This study concluded that green synthesised gold nanoparticles of rosmarinic acid could potentially be used for treating wounds. Full article

(This article belongs to the Special Issue Polyphenols and their Nanoformulations: Challenges and Opportunities)

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12 pages, 1918 KiB

Open AccessArticle

Design, Characterization, and Antimicrobial Evaluation of Copper Nanoparticles Utilizing Tamarixinin a Ellagitannin from Galls of Tamarix aphylla

by Mohamed A. A. Orabi, Mounir M. Salem-Bekhit, Ehab I. Taha, El-Shaymaa Abdel-Sattar, Omaish Salman Alqahtani, Fakhria A. Al-Joufi, Basel A. Abdel-Wahab, Ali Mohamed Alshabi, Hamad S. Alyami, Javed Ahmad and Tsutomu Hatano

Pharmaceuticals 2022, 15(2), 216; https://doi.org/10.3390/ph15020216 - 11 Feb 2022

Cited by 4 | Viewed by 2274

Abstract

The application of plant extracts or plant-derived compounds in the green synthesis of metal nanoparticles (NPs) was researched. Determining the exact metabolite implicated in the formation of NPs would necessitate comprehensive investigations. Copper nanoparticles (CuNPs) are gaining a lot of attention because of their unique properties and effectiveness against a wide range of bacteria and fungi, as well as their potential for usage in catalytic, optical, electrical, and microelectronics applications. In the course of this study, we aimed to formulate CuNPs utilizing pure tamarixinin A (TA) ellagitannin isolated from Tamarix aphylla galls. The main particle size of the formed CuNPs was 44 ± 1.7 nm with zeta potential equal to −23.7 mV, which emphasize the stability of the CuNPs. The X-ray diffraction spectroscopy showed a typical centered cubic crystalline structure phase of copper. Scanning electron microscopy images were found to be relatively spherical and homogeneous in shape. The antimicrobial properties of TA, as well as its mediated CuNPs, have been evaluated through well diffusion assays against four bacterial, Bacillus subtilis NCTC 10400, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Pseudomonas aeruginosa ATCC 27853, and two fungal, Candida albicans and Aspergillus flavus, strains. The distinctive antimicrobial activities were noted against the fungal strains and the Gram-negative bacterial strains P. aeruginosa ATCC 27853, and E. coli ATCC 25922. In conclusion, CuNPs mediated by TA can be applied for combating a wide range of bacterial and fungal species especially C. albicans, Asp. flavus, and P. aeruginosa in a variety of fields. Full article

(This article belongs to the Special Issue Polyphenols and their Nanoformulations: Challenges and Opportunities)

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