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Search Results (1,677)

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Keywords = in vitro absorption

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16 pages, 3423 KiB  
Article
Lepidium virginicum Water-Soluble Chlorophyll-Binding Protein with Chlorophyll A as a Novel Contrast Agent for Photoacoustic Imaging
by Victor T. C. Tsang, Hannah H. Kim, Bingxin Huang, Simon C. K. Chan and Terence T. W. Wong
Sensors 2025, 25(11), 3492; https://doi.org/10.3390/s25113492 (registering DOI) - 31 May 2025
Abstract
Photoacoustic (PA) imaging (PAI) holds great promise for non-invasive biomedical diagnostics. However, the efficacy of current contrast agents is often limited by photobleaching, toxicity, and complex synthesis processes. In this study, we introduce a novel, biocompatible PAI contrast agent: a recombinant water-soluble chlorophyll-binding [...] Read more.
Photoacoustic (PA) imaging (PAI) holds great promise for non-invasive biomedical diagnostics. However, the efficacy of current contrast agents is often limited by photobleaching, toxicity, and complex synthesis processes. In this study, we introduce a novel, biocompatible PAI contrast agent: a recombinant water-soluble chlorophyll-binding protein (WSCP) from Lepidium virginicum (LvP) reconstituted with chlorophyll a (LvP-chla). LvP-chla exhibits a strong and narrow absorption peak at 665 nm, with a molar extinction coefficient substantially higher than oxyhemoglobin and deoxyhemoglobin, enabling robust signal generation orthogonal to endogenous chromophores. Phantom studies confirmed a linear relationship between PA signal amplitude and LvP-chla concentration, demonstrating its stability and reliability. In vitro cytotoxicity testing using 4T1 cells showed high cell viability at 5 mg/mL, justifying its use for in vivo studies. In vivo experiments with a 4T1 tumor-bearing mouse model demonstrated successful tumor localization following intratumoral injection of LvP-chla, with clear visualization via spectroscopic differentiation from endogenous absorbers at 665 nm and 685 nm. Toxicity assessments, both in vitro and in vivo, revealed no adverse effects, and clearance studies confirmed minimal retention after 96 h. These findings show that LvP-chla is a promising contrast agent that enhances PAI capabilities through its straightforward synthesis, stability, and biocompatibility. Full article
(This article belongs to the Section Sensing and Imaging)
10 pages, 9927 KiB  
Communication
Silver Nanoparticles from Hermetia illucens Biomass Are Antibacterial Against Pseudomonas aeruginosa Infection in Caenorhabditis elegans
by Alinne Ayech, Gabriela Hollmann, Robson M. Marreiro Gomes, Belisa A. Rodrigues, Vanessa K. Engers, Rafael S. Gonçalves, Sandro Daniel Nornberg, Daniela F. Ramos, Karine Rigon Zimmer and José M. Monserrat
Microorganisms 2025, 13(6), 1277; https://doi.org/10.3390/microorganisms13061277 (registering DOI) - 30 May 2025
Viewed by 35
Abstract
Silver nanoparticles (AgNPs) are known for their antimicrobial properties, and can be synthesized through various routes. We used both chemical synthesis and green synthesis from the biomass of black soldier larvae (Hermetia illucens). To test the antimicrobial potential of these nanoparticles, [...] Read more.
Silver nanoparticles (AgNPs) are known for their antimicrobial properties, and can be synthesized through various routes. We used both chemical synthesis and green synthesis from the biomass of black soldier larvae (Hermetia illucens). To test the antimicrobial potential of these nanoparticles, we employed an in vitro test, with CFU counting, and also used the worm Caenorhabditis elegans as an in vivo model. C. elegans were infected with Pseudomonas aeruginosa and treated with AgNPs from both syntheses. These AgNPs exhibited absorption spectrum peaks around 400 nm and sizes of 8 ± 3.5 (chemical) and 11 ± 4.7 nm (green). P. aeruginosa-infected worms, without treatment with AgNPs, achieved 100% mortality within 3 days, while AgNPs-treated worms survived until the end of the experiment, with no statistical differences compared to the non-infected worms of the control group. The results demonstrate that nanoparticles produced from H. illucens biomass have antimicrobial capacity, reducing bacterial growth in vitro and being able to protect C. elegans from infection by P. aeruginosa, similar to those produced by chemical synthesis. However, AgNPs from green synthesis are less harmful to the environment while maintaining their antimicrobial potential. Full article
(This article belongs to the Special Issue Antimicrobial Properties of Nanoparticles)
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24 pages, 2199 KiB  
Article
Design, Synthesis, Anti-Tumor Activity and Molecular Docking Studies of Novel Triphenylphosphine-Containing Formononetin Derivatives
by Hongjuan Cui, Yan Zhao, Wei Li, Huanjie Cui, Jiahong Han and Enbo Cai
Int. J. Mol. Sci. 2025, 26(11), 5280; https://doi.org/10.3390/ijms26115280 (registering DOI) - 30 May 2025
Viewed by 31
Abstract
Formononetin is widely used in anti-tumor research, but its poor water solubility leads to low absorption and poor utilization efficiency in vivo, limiting further development. The triphenylphosphine cation was partially attached to the 7-position hydroxyl group of formononetin to specifically target it into [...] Read more.
Formononetin is widely used in anti-tumor research, but its poor water solubility leads to low absorption and poor utilization efficiency in vivo, limiting further development. The triphenylphosphine cation was partially attached to the 7-position hydroxyl group of formononetin to specifically target it into the mitochondria of tumor cells to enhance the anti-tumor effect. Detailed structural characterization via 1H-NMR and 13C-NMR analysis confirmed the physical properties and chemical structures of 21 newly synthesized derivatives. The effects of these derivatives on tumor cells were assessed by in vitro and computational methods. MTT results from four tumor cell lines showed that formononetin derivatives containing triphenylphosphine had stronger anti-tumor activity than formononetin and exhibited more cytotoxic effects in cancer cells than in normal cells. In particular, the final product 2c (IC50 = 12.19 ± 1.52 μM) showed more potent anti-tumor activity against A549 cells. It was also superior to formononetin and 5-FU. To identify the potential biological targets, the core-expressed gene SHMT2 in lung cancer mitochondria was screened using network pharmacology technology, and molecular docking analysis confirmed the stable binding of the end products to the amino acid residues of the core genes through the formation of hydrogen bonds and via other interactions. In addition, molecular docking simulations further confirmed that the end product exhibited excellent stability when bound to SHMT2. These results suggest that triphenylphosphine-containing formononetin derivatives are worthy of further exploration in the search for novel drug candidates for the treatment of cancer. Full article
15 pages, 1047 KiB  
Article
Bioactive Peptides from Sodium Caseinate Hydrolysate with High Oral Absorption Regulate Blood Glucose in Type 2 Diabetic Mice via Inhibition of DPP-IV and Stimulation of GLP-1
by Pei-Yu Wu, Cheng-Hong Hsieh, Ali Iqbal, Yu-Shun Lin, Ming-Wei Cheng, Ling-Hsuan Chang, Shang-Ming Huang and Kuo-Chiang Hsu
Foods 2025, 14(11), 1953; https://doi.org/10.3390/foods14111953 - 30 May 2025
Viewed by 68
Abstract
Type 2 diabetes mellitus remains a critical global health challenge, driving the pursuit of novel therapeutic strategies. This study investigated the anti-diabetic efficacy of the peptide 1CBR, derived from sodium caseinate hydrolysate, administered orally at 25 mg/kg/day to db/db mice over a 4-week [...] Read more.
Type 2 diabetes mellitus remains a critical global health challenge, driving the pursuit of novel therapeutic strategies. This study investigated the anti-diabetic efficacy of the peptide 1CBR, derived from sodium caseinate hydrolysate, administered orally at 25 mg/kg/day to db/db mice over a 4-week period. Glucose tolerance was evaluated via oral glucose tolerance tests (OGTT), while plasma dipeptidyl peptidase-IV (DPP-IV) activity, glucagon-like peptide-1 (GLP-1), and insulin concentrations were quantified using enzyme-linked immunosorbent assays (ELISA). Two bioactive peptides, GPFPLPD and APDSGNFR, were isolated and characterized, exhibiting half-maximal inhibitory concentrations (IC50) of 99.12 µM and 73.07 µM for DPP-IV inhibition, respectively, and both significantly stimulated GLP-1 secretion in enteroendocrine cells in vitro. Pharmacokinetic analysis in Sprague–Dawley rats demonstrated oral bioavailability of 11.28% and 19.12% for these peptides, surpassing typical expectations for peptide-based agents. Collectively, these results provide compelling evidence that 1CBR-derived peptides exert glucose-lowering effects through the dual mechanisms of DPP-IV inhibition and GLP-1 stimulation, combined with favorable oral absorption profiles. These findings underscore the potential of 1CBR peptides as promising candidates for development into nutraceuticals or pharmaceutical agents for diabetes management. Full article
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14 pages, 475 KiB  
Systematic Review
Can Clear Aligners Release Microplastics That Impact the Patient’s Overall Health? A Systematic Review
by Adriana Assunta De Stefano, Martina Horodynski and Gabriella Galluccio
Materials 2025, 18(11), 2564; https://doi.org/10.3390/ma18112564 - 30 May 2025
Viewed by 127
Abstract
This systematic review aims to further current knowledge on the effects of microplastics from orthodontic clear aligners, identifying potential implications for human health and providing a basis for further research and development of alternative materials. A literature search to find all peer-reviewed citations [...] Read more.
This systematic review aims to further current knowledge on the effects of microplastics from orthodontic clear aligners, identifying potential implications for human health and providing a basis for further research and development of alternative materials. A literature search to find all peer-reviewed citations relevant to the review topic was conducted in the following databases: PubMed, Scopus, Web of Science, and Cochrane Library on 31 December 2024. A manual search of grey literature was also performed. There were 62 citations retrieved by the search query, and 11 were selected for inclusion in the review. Four selected studies were in vitro, while seven were in vitro following intraoral material aging studies. Ten studies evaluated the surface morphology of the material after aging, among the mechanical characteristics assessed, while only one article evaluated the chemical characteristics and size of the microplastic particles released from the aligners after simulated in vitro use. Discussion: From the evaluation of the studies included in this review, it is possible to state that there is a gradual increase over time in the surface roughness of the material, and modifications occurred in the morphology and surface topography of the aligners. Furthermore, it emerged that dispersion of microplastics occurs during the use of different types of aligners, with microplastic particle sizes ranging from 5 to 20 μm The findings suggest that clear aligners may cause microplastic dispersion in saliva during therapy, and this could cause a problem for the general health of patients, due to the absorption or ingestion of these released molecules. Further research is needed to fully understand the extent of microplastics released from aligners and to find alternative materials that can reduce this occurrence. Full article
(This article belongs to the Special Issue Orthodontic Materials: Properties and Effectiveness of Use)
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30 pages, 4063 KiB  
Article
Ferrocene-Based Hybrid Drugs as Potential Anticancer and Antibacterial Therapeutic Agents for Incorporation into Nanocarriers: In Silico, In Vitro, Molecular Docking Evaluations
by Sijongesonke Peter, Eric Morifi, Mutshinyalo Nwamadi, Samson Olaitan Oselusi, Asongwe Lioniel Tantoh, Thierry Youmbi Fonkui, Derek Tantoh Ndinteh and Blessing Atim Aderibigbe
Pharmaceutics 2025, 17(6), 722; https://doi.org/10.3390/pharmaceutics17060722 - 30 May 2025
Viewed by 71
Abstract
Background/Objectives: Cancer and bacterial cases are increasing. Hence, new drugs to treat these diseases are paramount. Ferrocene-based hybrid compounds were synthesizedas potential cancer and bacteria therapeutics. Methods: The synthesized compounds were characterized via FTIR, NMR, and LC-MS and evaluated against different cancer cells [...] Read more.
Background/Objectives: Cancer and bacterial cases are increasing. Hence, new drugs to treat these diseases are paramount. Ferrocene-based hybrid compounds were synthesizedas potential cancer and bacteria therapeutics. Methods: The synthesized compounds were characterized via FTIR, NMR, and LC-MS and evaluated against different cancer cells and bacterial strains. Moreover, computational studies of these compounds were conducted using several silico tools. Results: Among the synthesized compounds, hybrid 10 was the most promising compound, displaying promising anticancer activity with IC50 values between 42.42 and 45.37 and 50.64 and 73.37 µg/mL against HeLa and CHO cancer cells, respectively, with a selective index greater than one on HeLa cancer cells. Compounds 2226 displayed promising antibacterial activity with a MIC value of 7.8125 µg/mL against most bacterial strains in vitro. The in silico results revealed that this compound has strong binding affinities for 4qtb, 3eqm, and 2w3l cervical cancer proteins, exhibiting binding energies of −7.3, −8.7, and 7.4 kcal/mol, respectively. Furthermore, hybrid 10 showed promising pharmacokinetics and drug-like properties, including high GI absorption, moderate water solubility, favoring the oral administration route, nontoxicity, and is a P-gp substrate. Conclusions: The findings obtained in this study illustrate that hybrid compounds are potential therapeutics that need to be explored. The compounds also contained functionalities relevant for incorporating into nanocarriers to improve their biological activities further. Therefore, further studies are recommended for the most effective compounds to reinforce these findings. Full article
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22 pages, 4409 KiB  
Article
Newly Synthesized CoFe2−yPryO4 (y = 0; 0.01; 0.03; 0.05; 0.1; 0.15; 0.2) Nanoparticles Reveal Promising Selective Anticancer Activity Against Melanoma (A375), Breast Cancer (MCF-7), and Colon Cancer (HT-29) Cells
by Slaviţa Rotunjanu, Roxana Racoviceanu, Armand Gogulescu, Alexandra Mioc, Andreea Milan, Narcisa Laura Marangoci, Andrei-Ioan Dascălu, Marius Mioc, Roxana Negrea-Ghiulai, Cristina Trandafirescu and Codruţa Șoica
Nanomaterials 2025, 15(11), 829; https://doi.org/10.3390/nano15110829 - 30 May 2025
Viewed by 148
Abstract
In this study, praseodymium-doped cobalt ferrite nanoparticles (CoFe2−yPryO4, y = 0–0.2) were synthesized via sol-gel auto-combustion and systematically characterized to assess their structural, morphological, magnetic, and biological properties. X-ray diffraction (XRD) confirmed single-phase cubic cobalt ferrite formation [...] Read more.
In this study, praseodymium-doped cobalt ferrite nanoparticles (CoFe2−yPryO4, y = 0–0.2) were synthesized via sol-gel auto-combustion and systematically characterized to assess their structural, morphological, magnetic, and biological properties. X-ray diffraction (XRD) confirmed single-phase cubic cobalt ferrite formation for samples with y ≤ 0.05 and the emergence of a secondary orthorhombic PrFeO3 phase at higher dopant concentrations. FTIR spectroscopy identified characteristic metal–oxygen vibrations and revealed a progressive shift of absorption bands with increasing praseodymium (Pr) content. Vibrating sample magnetometry (VSM) demonstrated a gradual decline in saturation (Ms) and remanent (Mr) magnetization with Pr doping, an effect further intensified by cyclodextrin surface coating. TEM analyses revealed a particle size increase correlated with dopant level, while SEM images displayed a porous morphology typical of combustion-synthesized ferrites. In vitro cell viability assays showed minimal toxicity in normal human keratinocytes (HaCaT), while significant antiproliferative activity was observed against human cancer cell lines A375 (melanoma), MCF-7 (breast adenocarcinoma), and HT-29 (colorectal adenocarcinoma), particularly in Pr 6-CD and Pr 7-CD samples. These findings suggest that Pr substitution and cyclodextrin coating can effectively modulate the physicochemical and anticancer properties of cobalt ferrite nanoparticles, making them promising candidates for future biomedical applications. Full article
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17 pages, 2310 KiB  
Article
Enhancing Oral Absorption of Quercetin Through Multifactorial Synergies in Crystal Dispersion Systems
by Yao Liu, Qiuli Yan and Chunhui Hu
Molecules 2025, 30(11), 2390; https://doi.org/10.3390/molecules30112390 - 30 May 2025
Viewed by 97
Abstract
This study aims to enhance the dissolution rate and oral absorption of quercetin (QUR) by formulating quercetin crystalline solid dispersion (QUR-CSD). Quercetin, as a natural antioxidant, can effectively neutralize free radicals, reduce inflammatory responses, help lower the risk of cardiovascular diseases and certain [...] Read more.
This study aims to enhance the dissolution rate and oral absorption of quercetin (QUR) by formulating quercetin crystalline solid dispersion (QUR-CSD). Quercetin, as a natural antioxidant, can effectively neutralize free radicals, reduce inflammatory responses, help lower the risk of cardiovascular diseases and certain cancers, and support the function of the immune system. CSDs underwent characterization through powder X-ray diffraction and scanning electron microscopy, and dissolution rates were evaluated in vitro. Oral absorption assessment was conducted using SD rats, while Caco-2 monolayer cell transmembrane (CMCT) and single pass intestinal perfusion (SPIP) were performed to assess the permeability of CSDs. QUR within the CSDs exhibited hydrogen bond interactions with P188 and PEG, displaying stronger interaction parameters (χ) of –4.0 and –6.1, respectively. The crystalline domain of QUR within Poloxamer 188 (P188) was smaller than within polyethylene glycol 8000 (PEG8000). CSDs improved the dissolution rate of QUR, with the P188-CSD slightly outperforming the PEG8000-CSD due to P188’s ability to enhance drug wettability and solubility and to maintain supersaturation. Pharmacokinetic results revealed a 3.5-fold and 25-fold increase in oral absorption for P188-CSD and PEG8000-CSD, respectively, compared to QUR. CMCT and SPIP indicated superior permeability for PEG8000-CSD, potentially attributed to caveolin-mediated PEG transmembrane transport. QUR-CSD significantly enhanced oral absorption, with PEG8000-CSD demonstrating superior efficacy. This improvement was attributed to various factors, including crystalline size reduction, drug wettability enhancement, maintenance of supersaturation by polymers, and caveolin-mediated transmembrane transport. Full article
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20 pages, 4221 KiB  
Article
Preparation and Evaluation of an Oral Administration System of Albendazole-Metal-Organic Framework Based on Dual Response to pH and Enzymes
by Weiqi Liu, Zhimei Guo, Yong Zhang, Yufei Guo, Ting Wang, Dahuan Liu and Chunhui Hu
Pharmaceuticals 2025, 18(6), 819; https://doi.org/10.3390/ph18060819 - 29 May 2025
Viewed by 78
Abstract
Objective: This study aims to develop a metal–organic framework (ABZ-MOFs)-based oral drug delivery system for albendazole (ABZ) to enhance its dissolution rate and oral bioavailability. Methods: ABZ@MOF-802, ABZ@UiO-66-NH2, and ABZ@MIL-125-NH2 were synthesized using a solvothermal method, and their physicochemical properties [...] Read more.
Objective: This study aims to develop a metal–organic framework (ABZ-MOFs)-based oral drug delivery system for albendazole (ABZ) to enhance its dissolution rate and oral bioavailability. Methods: ABZ@MOF-802, ABZ@UiO-66-NH2, and ABZ@MIL-125-NH2 were synthesized using a solvothermal method, and their physicochemical properties were characterized. The in vitro drug release was investigated under pH- and enzyme-responsive conditions, followed by transmembrane transport studies in Caco-2 cells. Finally, the oral bioavailability of ABZ@MOFs was evaluated in rats. Results: The particle sizes of ABZ@MOF-802, ABZ@UiO-66-NH2, and ABZ@MIL-125-NH2 were (1062.6 ± 94.8), (228.3 ± 12.3), and (502.3 ± 16.2) nm, with drug loading efficiencies of (1.71 ± 0.08%), (12.13 ± 0.04%), and (26.17 ± 0.10%), respectively. The ABZ@MOFs demonstrated structural stability in acidic environments and released ABZ under weakly acidic and neutral conditions, exhibiting distinct release profiles in the presence of different enzymes. Cellular experiments confirmed that ABZ@MOFs significantly improved transmembrane drug absorption. Pharmacokinetic analysis revealed that the bioavailability of ABZ@UiO-66-NH2 and ABZ@MIL-125-NH2 was 10.3-fold and 1.8-fold higher, respectively, compared to ABZ. Conclusions: The ABZ@MOFs systems effectively improved ABZ dissolution and oral bioavailability, with ABZ@UiO-66-NH2 showing a dual response mechanism to pH and enzymes. Full article
(This article belongs to the Section Biopharmaceuticals)
11 pages, 1830 KiB  
Article
Lactoferrin Solution as a New Natural Photosensitizer in Photodynamic Therapy Against Oral Candida spp. Multidrug-Resistant Isolates: A Preliminary In Vitro Study
by Cinzia Casu, Andrea Butera, Alice Piga, Andrea Scribante, Sara Fais and Germano Orrù
Microorganisms 2025, 13(6), 1255; https://doi.org/10.3390/microorganisms13061255 - 29 May 2025
Viewed by 181
Abstract
Serious oral infections are frequently caused by Candida species, which have lately demonstrated resistance to antifungal medications. As a result, new therapeutic strategies, like photodynamic therapy (PDT), are desperately needed. Lactoferrin (LF), a salivary enzyme, is a natural protein that binds iron and [...] Read more.
Serious oral infections are frequently caused by Candida species, which have lately demonstrated resistance to antifungal medications. As a result, new therapeutic strategies, like photodynamic therapy (PDT), are desperately needed. Lactoferrin (LF), a salivary enzyme, is a natural protein that binds iron and has antifungal properties. Given its chemical structure and light absorption at 310–350 nm, LF appears to be a good photosensitizer in a PDT process for treating oral candidiasis. The purpose of this work was to assess the effectiveness of lactoferrin (LF) as a photosensitizer (PS) in photodynamic treatment (PDT) against oral multidrug-resistant (MDR) isolates of Candida spp. using an in vitro investigation. For this in vitro investigation, oral MDR isolates of Candida albicans, Candida kruseii, and Candida glabrata were employed. Using a Kirby–Bauer test (Eucast protocol), a solution of 20 mg of bovine lactoferrin dissolved in 1 mL of Sabouraud’s broth was tested in four different experimental combinations: (i) the solution as it is; (ii) the solution activated with 3% H2O2; (iii) the solution activated by light at 310–350 nm; and (iv) the solution activated with both 3% H2O2 and light at 310–350 nm. A control group and one with only H2O2 were also tested. After that, the Petri plates were incubated for 48 h at 37 °C. With inhibitory halos ranging from 30 to 40 mm for all Candida spp. MDR analyzed, group (iv) displayed the greatest results. H2O2 + lactoferrin-based solutions are thought to be potential PS in PDT for MDR Candida spp. eradication. Full article
(This article belongs to the Special Issue Oral Microbes and Human Health, Second Edition)
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28 pages, 1959 KiB  
Article
Okra Flower Polysaccharide–Pea Protein Conjugates Stabilized Pickering Emulsion Enhances Apigenin Stability, Bioaccessibility, and Intestinal Absorption In Vitro
by Nuo Zhang, Jiale You, Xiaoli Yan, Hongchen Ji, Wenxuan Ji, Zhengyu Liu, Min Zhang, Peng Liu, Panpan Yue, Zain Ullah, Ting Zhao and Liuqing Yang
Foods 2025, 14(11), 1923; https://doi.org/10.3390/foods14111923 - 28 May 2025
Viewed by 156
Abstract
The covalent interactions of polysaccharides and protein can improve the emulsification and stability of Pickering emulsions, which are promising systems for the delivery of active substances. Okra flowers, which commonly represent agricultural waste, have high-viscosity polysaccharides that can be used for the development [...] Read more.
The covalent interactions of polysaccharides and protein can improve the emulsification and stability of Pickering emulsions, which are promising systems for the delivery of active substances. Okra flowers, which commonly represent agricultural waste, have high-viscosity polysaccharides that can be used for the development of protein–polysaccharide-based emulsifiers. In this study, the Maillard reaction was performed under optimized conditions (70 °C, pH 10, and 12 h) with a 1:1 mass ratio to generate pea protein isolate (PPI) –okra flower polysaccharide (OP) conjugate with the highest grafting degree of 22.80 ± 0.26%. The covalent binding of OP facilitated variations in the secondary and tertiary structures of PPI, decreasing its particle size (from 535.70 to 212.05 nm) and zeta-potential (from −30.37 to −44.39 mV). The emulsifying stability of the emulsion stabilized by OP-PPI conjugates was significantly improved due to the formation of a stable interfacial layer, showing an 80.39% increase compared to that of free PPI. Simultaneously, the emulsions prepared with the conjugates demonstrated excellent stability across diverse environmental conditions by enhancing the interaction between the lipid and protein. Moreover, the conjugate-stabilized emulsion not only exhibited a higher encapsulation efficiency of 91.52 ± 0.75% and superior protective efficacy but also controlled the release of apigenin (API) during gastrointestinal digestion, achieving the highest API bioaccessibility (74.58 ± 1.19%). Furthermore, it also contributed to the absorption and transmembrane transport efficiency of API in Caco-2 cells, improving its bioavailability. These results confirmed that covalent conjugation with OP is a valuable strategy for enhancing the emulsifying features of PPI. The PPI–OP emulsion delivery system holds great potential for nutrient delivery. Full article
(This article belongs to the Section Food Physics and (Bio)Chemistry)
17 pages, 3142 KiB  
Article
Evaluation of the In Vitro Permeation Parameters of Topical Diclofenac Sodium from Transdermal Pentravan® Products and Hydrogel Celugel Through Human Skin
by Urszula Adamiak-Giera, Michał Gackowski, Joanna Szostak, Tomasz Osmałek, Damian Malinowski, Anna Nowak, Anna Machoy-Mokrzyńska, Maciej Miernik, Mirosław Halczak, Maciej Romanowski, Anna Czerkawska and Monika Białecka
Pharmaceuticals 2025, 18(6), 810; https://doi.org/10.3390/ph18060810 - 28 May 2025
Viewed by 62
Abstract
Background: Diclofenac is a phenylacetic acid derivative classified as a non-selective COX inhibitor. Similar to other NSAIDs, it is characterized by anti-inflammatory, antipyretic, and analgesic effects. Long-term therapy with diclofenac might also lead to severe gastrointestinal, renal, or cardiovascular systems disorders. Aim of [...] Read more.
Background: Diclofenac is a phenylacetic acid derivative classified as a non-selective COX inhibitor. Similar to other NSAIDs, it is characterized by anti-inflammatory, antipyretic, and analgesic effects. Long-term therapy with diclofenac might also lead to severe gastrointestinal, renal, or cardiovascular systems disorders. Aim of the study was to compare own formulation prepared from pharmaceutical raw materials with ready-to-use diclofenac product. Methods: In the in vitro permeation experiments, human skin was excised from the abdomen of living patients as a result of plastic surgery. The transdermal semi-solid formulations were compounded using Pentravan®, a ready-to-use transdermal base and hydrophilic gel base (Celugel). In vitro Penetration Studies, HPLC analysis, optical microscopy imaging, and a spreadability test were conducted. Rheological analysis provided insights into flow behavior, structure, and thixotropy. Results: Combination of Celugel with diclofenac sodium and the addition of substances acting as absorption enhancers, e.g., menthol, may provide an interesting alternative for enteral drugs, especially in patients with multimorbidity and polypharmacy. Conclusions: Topical diclofenac sodium with of addition of permeation enhancers like menthol might provide higher drug concentrations in the surrounding tissues and better analgesic and anti-inflammatory effects in compare to commercially available product and may provide optimum effectiveness with minimal risk of adverse effects, particularly in elderly and polymedicated patients. Full article
(This article belongs to the Section Pharmaceutical Technology)
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23 pages, 2553 KiB  
Article
A Green Integrated Approach to Multifunctional Silver Nanoparticles Derived from Aronia melanocarpa
by Andreia Corciova, Cornelia Mircea, Adrian Fifere, Ioana-Andreea Turin Moleavin, Ana Flavia Burlec, Bianca Ivanescu, Ana-Maria Vlase, Monica Hancianu and Irina Macovei
Pharmaceutics 2025, 17(5), 669; https://doi.org/10.3390/pharmaceutics17050669 - 20 May 2025
Viewed by 293
Abstract
Background/Objectives: This study reports the green synthesis, optimization, characterization, and multifunctional evaluation of silver nanoparticles (AgNPs) using an ethanolic Aronia melanocarpa berry extract. The objective was to establish optimal synthesis conditions; assess the in vitro stability; and evaluate the antioxidant, photocatalytic, and photoprotective [...] Read more.
Background/Objectives: This study reports the green synthesis, optimization, characterization, and multifunctional evaluation of silver nanoparticles (AgNPs) using an ethanolic Aronia melanocarpa berry extract. The objective was to establish optimal synthesis conditions; assess the in vitro stability; and evaluate the antioxidant, photocatalytic, and photoprotective activities. Methods: The cytogenotoxic effects of the AgNPs were evaluated on Triticum aestivum roots. The AgNPs were synthesized via bioreduction using an ethanolic extract of A. melanocarpa under varied pH, AgNO3 concentration, extract/AgNO3 ratio, temperature, and stirring time, with optimization guided by UV–Vis spectral analysis. The AgNPs were further characterized by FTIR, DLS, TEM, and EDX. In vitro stability was evaluated over six months in different dispersion media (ultrapure water; 5% NaCl; and PBS at pH 6, 7, and 8). Biological assessments included antioxidant assays (lipoxygenase inhibition, DPPH radical scavenging, metal chelation, and hydroxyl radical scavenging), photocatalytic dye degradation, and SPF determination. Results: Optimal synthesis was achieved at pH 8, 3 mM AgNO3, extract/AgNO3 ratio of 1:9, 40 °C, and 240 min stirring. The AgNPs were spherical (TEM), well dispersed (PDI = 0.32), and highly stable (zeta potential = −40.71 mV). PBS pH 6 and 7 ensured the best long-term colloidal stability. The AgNPs displayed strong dose-dependent antioxidant activity, with superior lipoxygenase inhibition (EC50 = 18.29 µg/mL) and the effective photocatalytic degradation of dyes under sunlight. Photoprotective properties were confirmed through UV absorption analysis. The AgNPs showed a strong antimitotic effect on wheat root cells. Conclusions: The study demonstrates that A. melanocarpa-mediated AgNPs are stable, biologically active, and suitable for potential biomedical, cosmetic, and environmental applications, reinforcing the relevance of plant-based nanotechnology. Full article
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17 pages, 4964 KiB  
Article
Adverse Effect of Polystyrene Nanoplastics in Impairing Glucose Metabolism in Liver Injury
by Raden Joko Kuncoroningrat Susilo, Manikya Pramudya, Firli Rahmah Primula Dewi, Windy Seftiarini, Dewi Hidayati, Aunurohim Aunurohim, Vuanghao Lim, Mochammad Aqilah Herdiansyah and Alfiah Hayati
Int. J. Mol. Sci. 2025, 26(10), 4870; https://doi.org/10.3390/ijms26104870 - 19 May 2025
Viewed by 230
Abstract
Polystyrene nanoplastics (PS-NPs) are result from the degradation of plastic and have diameters ranging from 1 nm to 100 nm. The objective of this study is to provide information on the adverse effects of PS-NPs with in vitro and in vivo analyses of [...] Read more.
Polystyrene nanoplastics (PS-NPs) are result from the degradation of plastic and have diameters ranging from 1 nm to 100 nm. The objective of this study is to provide information on the adverse effects of PS-NPs with in vitro and in vivo analyses of liver injury. An in vitro study was conducted using confocal microscopy, flow cytometry, and MTT test analysis. An in vivo study was conducted to determine apoptosis levels, glucose metabolism gene expressions, liver enzymes, and liver histology. Data were analyzed using GraphPad Prism software 10.2.1. The in vitro study showed the absorption of PS-NPs in the cell cytoplasm, the percentage of apoptosis, 3t3, and the WiDr cell lines’ viability. The in vivo analysis showed that PS-NPs can stimulate liver injuries, such as inducing the elevation of liver enzymes, necrosis, edema, inflammation, and the dilatation of the portal vein diameter. High levels of caspase-3, caspase-9, and Bax were detected, as well as the expression of several genes including PI3K, AKT, PEPCK, GLUT2, and PK. In conclusion, the in vitro analysis showed the detrimental effects of PS-NPs on cells, such as high levels of apoptosis and low cell viability, while the in vivo studies displayed the impairment of liver tissue and disturbances in glucose metabolism regulation. Full article
(This article belongs to the Section Molecular Pathology, Diagnostics, and Therapeutics)
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24 pages, 3344 KiB  
Article
Enzymatic Extraction of Hawthorn Pectin Under Ultrahigh Pressure: Optimization and Characterization
by Zheng Ye, Qiaoshuang Lu, Dihu Lv and Chun Yang
Molecules 2025, 30(10), 2210; https://doi.org/10.3390/molecules30102210 - 19 May 2025
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Abstract
This study employed response surface methodology to optimize the conditions for ultrahigh-pressure-assisted enzymatic extraction (UHPEE) of pectin from hawthorn using cellulase. The effects of this method on the characteristics of the extracted pectin were investigated. The optimal extraction parameters were determined to be [...] Read more.
This study employed response surface methodology to optimize the conditions for ultrahigh-pressure-assisted enzymatic extraction (UHPEE) of pectin from hawthorn using cellulase. The effects of this method on the characteristics of the extracted pectin were investigated. The optimal extraction parameters were determined to be a solid-to-liquid ratio of 1:70 g/mL, an extraction pressure of approximately 300 MPa, and a holding time of roughly 600 s, yielding a pectin recovery of 4.02%. The optimized UHPEE process resulted in reductions in both the degree of esterification and molecular weight of the pectin, while concurrently increasing the content of total galacturonic acid and total polyphenols. Ion chromatography analysis identified five monosaccharides in the hawthorn pectin, with galacturonic acid being the most predominant. Fourier-transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM) analyses revealed the presence of characteristic absorption peaks of pectin and a rough surface topology with a loose, flaky structure, respectively. Rheological measurements demonstrated that the hawthorn pectin exhibited shear-thinning behavior, characteristic of a pseudoplastic fluid. In vitro antioxidant assays showed that hawthorn pectin scavenged 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals with a rate of 92.72%, comparably to vitamin C at the same concentration (96.30%). These results indicate that the optimized UHPEE method is a more efficient technique for extracting hawthorn pectin and effectively enhances its antioxidant activity, suggesting its potential application in the food industry. Full article
(This article belongs to the Special Issue Chemical Analysis for Food and Beverage Bioactive Compounds)
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