Further Research in Polyphenols Formulations

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (30 September 2024) | Viewed by 3357

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Department of Drug Technology and Social Pharmacy, Lithuanian University of Health Sciences, Kaunas, Lithuania
Interests: cosmetology; cannabis sativa; herbal medicine; natural and non-natural non-opioid topical pain relievers; pharmaceutical technology
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Special Issue Information

Dear Colleagues,

The main flavonoid sources are fruits and vegetables, and they are also abundant in cocoa products (cocoa powder, chocolate), black and green tea and red wine. Among the fruits (berries, plums, cherries, and apples) are the richest in flavonoids, whereas tropical fruits are poor in flavonoids. Polyphenols are biologically active compounds found in a wide range of plant materials and are used in various pharmaceutical and cosmetic formulations. These compounds have various pharmacological effects, including antioxidant, anti-inflammatory, cognitive enhancement, anti-migraine and anti-cancer effects. Numerous studies have shown their strong positive activities in reducing inflammation, modulating immune response, and supporting and restoring the normal functions of cells.

It is important to find methods to isolate phenolic compounds and to use them to produce or improve innovative pharmaceutical forms. Traditional methods such as maceration, percolation, recolonization, etc., are used for the extraction of phenolic compounds. In this Special Issue, we expect to see not traditional, but innovative extraction methods for polyphenols.

It is also paramount to find methods to ensure the bioavailability and efficiency of phenolic compounds. This is usually ensured by various technological procedures. We therefore look forward to innovative technologies and possible new pharmacological effects of polyphenols for the future of pharmaceuticals.

Prof. Dr. Jurga Bernatoniene
Guest Editor

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Keywords

  • polyphenols
  • bioavailability
  • polyphenol activity
  • pharmaceuticals
  • cosmeceuticals
  • extraction
  • encapsulation
  • 3D printing
  • innovative drug formulations
  • targeted drug delivery

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Published Papers (3 papers)

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Research

13 pages, 849 KiB  
Article
Enhancing Oral 5-ASA Effectiveness in Mild-to-Moderate Ulcerative Colitis through an H. erinaceus-Based Nutraceutical Add-on Multi-Compound: The “HERICIUM-UC” Two-Arm Multicentre Retrospective Study
by Antonio Tursi, Alessandro D’Avino, Giovanni Brandimarte, Giammarco Mocci, Raffaele Pellegrino, Edoardo Vincenzo Savarino, Antonietta Gerarda Gravina and the HERICIUM-UC Study Group
Pharmaceutics 2024, 16(9), 1133; https://doi.org/10.3390/pharmaceutics16091133 - 28 Aug 2024
Viewed by 776
Abstract
Mild-to-moderate ulcerative colitis (UC) management is centred on 5-aminosalicylic acid (5-ASA) derivatives. Whether supplementing 5-ASA with nutraceuticals can provide real advantages in UC-relevant outcomes is unclear. This retrospective multicentre study compared clinical remission, response rates, and faecal calprotectin levels in a two-arm design, [...] Read more.
Mild-to-moderate ulcerative colitis (UC) management is centred on 5-aminosalicylic acid (5-ASA) derivatives. Whether supplementing 5-ASA with nutraceuticals can provide real advantages in UC-relevant outcomes is unclear. This retrospective multicentre study compared clinical remission, response rates, and faecal calprotectin levels in a two-arm design, including patients treated with 5-ASA alone and those with additional H. erinaceus-based multi-compound supplementation. In the 5-ASA alone group, clinical response rates were 41% at three months (T1) and 60.2% at six months (T2), while corresponding clinical remission rates were 16.9% and 36.1%. In the nutraceutical supplementation group, clinical response rates were 49.6% (T1) and 70.4% (T2), with clinical remission rates of 30.4% (T1) and 50.9% (T2). No significant differences in clinical response rates between the groups at T1 (p = 0.231) and T2 (p = 0.143) emerged. Clinical remission rates differed significantly at both time points (p = 0.029 and p = 0.042, respectively). Faecal calprotectin levels decreased significantly in both groups during the retrospective follow-up (p < 0.05), and this was more pronounced in nutraceutical supplementation patients at both T1 (p = 0.005) and T2 (p = 0.01). No adverse events were reported. This multi-component nutraceutical supplementation offers real-world potential in controlling disease activity in patients with mild-to-moderate UC. Full article
(This article belongs to the Special Issue Further Research in Polyphenols Formulations)
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23 pages, 11650 KiB  
Article
Sweeteners Show a Plasticizing Effect on PVP K30—A Solution for the Hot-Melt Extrusion of Fixed-Dose Amorphous Curcumin-Hesperetin Solid Dispersions
by Kamil Wdowiak, Lidia Tajber, Andrzej Miklaszewski and Judyta Cielecka-Piontek
Pharmaceutics 2024, 16(5), 659; https://doi.org/10.3390/pharmaceutics16050659 - 15 May 2024
Cited by 2 | Viewed by 1136
Abstract
The co-administration of curcumin and hesperetin might be beneficial in terms of neuroprotective activity; therefore, in this study, we attempted to develop a fixed-dose formulation comprising these two compounds in an amorphous state. The aim of obtaining an amorphous state was to overcome [...] Read more.
The co-administration of curcumin and hesperetin might be beneficial in terms of neuroprotective activity; therefore, in this study, we attempted to develop a fixed-dose formulation comprising these two compounds in an amorphous state. The aim of obtaining an amorphous state was to overcome the limitations of the low solubility of the active compounds. First, we assessed the possibility of using popular sweeteners (erythritol, xylitol, and sorbitol) as plasticizers to reduce the glass transition temperature of PVP K30 to prepare the polymer–excipient blends, which allowed the preparation of amorphous solid dispersions via hot-melt extrusion at a temperature below the original glass transition of PVP K30. Erythritol proved to be the superior plasticizer. Then, we focused on the development of fixed-dose amorphous solid dispersions of curcumin and hesperetin. Powder X-ray diffraction and thermal analysis confirmed the amorphous character of dispersions, whereas infrared spectroscopy helped to assess the presence of intermolecular interactions. The amorphous state of the produced dispersions was maintained for 6 months, as shown in a stability study. Pharmaceutical parameters such as dissolution rate, solubility, and in vitro permeability through artificial membranes were evaluated. The best improvement in these features was noted for the dispersion, which contained 15% of the total content of the active compounds with erythritol used as the plasticizer. Full article
(This article belongs to the Special Issue Further Research in Polyphenols Formulations)
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21 pages, 2513 KiB  
Article
Impact of Polyvinylpyrrolidone-Vinyl Acetate Copolymer and Sodium Starch Glycolate Excipients on Phenolic Extraction from Red Clover: Enhancing Biological Activity and Antioxidant Potential
by Jurga Andreja Kazlauskaite, Mindaugas Marksa and Jurga Bernatoniene
Pharmaceutics 2024, 16(3), 399; https://doi.org/10.3390/pharmaceutics16030399 - 14 Mar 2024
Viewed by 984
Abstract
Adding certain excipients during the extraction process can enhance the concentration of target compounds, leading to potentially increased biological properties of the plant extract. This study explores the impact of PVP/VAC and SSG excipients on red clover bud extracts, aiming to enhance their [...] Read more.
Adding certain excipients during the extraction process can enhance the concentration of target compounds, leading to potentially increased biological properties of the plant extract. This study explores the impact of PVP/VAC and SSG excipients on red clover bud extracts, aiming to enhance their concentration of target compounds and, consequently, their biological properties. The antioxidative potential was evaluated using DPPH, ABTS, and FRAP methods, and the chemical profile was determined using mass spectrometry. Antibacterial activity against various strains was determined through the minimal inhibitory concentration (MIC) method. The results revealed that the excipient-enriched samples exhibited significantly elevated antioxidant activities as well as phenolic and flavonoid contents compared to control samples. Notably, sample V1E3 demonstrated the highest antioxidant potential, with 52.48 ± 0.24 mg GAE/g dw (phenolic content), 463 ± 6.46 μg TE/g dw (ABTS), 12.81 ± 0.05 μg TE/g dw (DPPH), and 29.04 ± 1.16 mg TE/g dw (post-column ABTS). The highest flavonoid content was found in the S1E3 sample—24.25 ± 0.17 mg RU/g dw. Despite the increased antioxidant potential, no significant variance in antimicrobial activity was noted between the test samples and controls. This implies that excipients may hold the potential to enhance the biological properties of red clover extracts for pharmaceutical applications. These findings contribute valuable insights into optimizing extraction processes for improved functionality and application of plant-derived compounds in therapeutic formulations. Full article
(This article belongs to the Special Issue Further Research in Polyphenols Formulations)
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