Pub Date : 2025-07-31eCollection Date: 2025-01-01DOI: 10.2147/NSA.S529010
Pattarakamol Sarotsumpan, I-Hui Chiu, Pao-Chu Wu, Nicholas Mun Hoe Khong, Celine Valeria Liew, Romchat Chutoprapat
Purpose: This study investigated the development and characterization of trans-resveratrol-loaded transfersomes, with and without cholesterol, for potential non-irritating dermal applications.
Methods: Transfersomes were prepared using thin-film hydration combined with probe sonication, incorporating hydrogenated lecithin, cholesterol, and Tween® 60 in six different ratios. The formulations were characterized for their physicochemical properties, including particle size, polydispersity index, zeta potential, entrapment efficiency, morphology, in vitro release profiles, dermal permeation potential, and safety profile.
Results: All formulations exhibited particle sizes below 150 nm and zeta potentials below -30 mV, indicating favorable characteristics for dermal delivery. Cholesterol incorporation significantly increased particle size and enhanced zeta potential (p<0.05). Formulations containing 3-3.5% w/v hydrogenated lecithin achieved superior entrapment efficiency (>90%) compared to those with lower lecithin content (p<0.05), regardless of cholesterol incorporation. Transfersomes containing cholesterol displayed morphology with well-defined edges compared to cholesterol-free formulations. In vitro release studies revealed distinct release profiles, with cholesterol-free formulations releasing 70-83% of trans-resveratrol over 24 hours, compared to only 0-30% for cholesterol-containing formulations. Strat-M® membrane-based permeation studies confirmed enhanced trans-resveratrol delivery across all transfersomal systems compared to the saturated solution (p<0.05), though cholesterol showed no significant impact on permeation efficiency. These findings indicate that cholesterol influences release profile but has limited effect on permeation efficiency. Safety assessment using the Hen's Egg Test-Chorioallantoic Membrane (HET-CAM) assay classified the developed transfersomes as weak irritants, indicating their dermal safety. Notably, formulation F3, with a hydrogenated lecithin to cholesterol to Tween 60 ratio of 6:0:4, emerged as the optimal candidate, achieving the highest release rate (80.24% over 24 hours) while maintaining favorable permeation compared to control.
Conclusion: These findings feature the potential of transfersomal systems, particularly cholesterol-free variants, as promising carriers for the effective and safe dermal delivery of trans-resveratrol.
{"title":"Development and Evaluation of Trans-Resveratrol-Loaded Transfersomes: Role of Cholesterol in Formulation Design for Dermal Delivery.","authors":"Pattarakamol Sarotsumpan, I-Hui Chiu, Pao-Chu Wu, Nicholas Mun Hoe Khong, Celine Valeria Liew, Romchat Chutoprapat","doi":"10.2147/NSA.S529010","DOIUrl":"10.2147/NSA.S529010","url":null,"abstract":"<p><strong>Purpose: </strong>This study investigated the development and characterization of trans-resveratrol-loaded transfersomes, with and without cholesterol, for potential non-irritating dermal applications.</p><p><strong>Methods: </strong>Transfersomes were prepared using thin-film hydration combined with probe sonication, incorporating hydrogenated lecithin, cholesterol, and Tween<sup>®</sup> 60 in six different ratios. The formulations were characterized for their physicochemical properties, including particle size, polydispersity index, zeta potential, entrapment efficiency, morphology, in vitro release profiles, dermal permeation potential, and safety profile.</p><p><strong>Results: </strong>All formulations exhibited particle sizes below 150 nm and zeta potentials below -30 mV, indicating favorable characteristics for dermal delivery. Cholesterol incorporation significantly increased particle size and enhanced zeta potential (p<0.05). Formulations containing 3-3.5% w/v hydrogenated lecithin achieved superior entrapment efficiency (>90%) compared to those with lower lecithin content (p<0.05), regardless of cholesterol incorporation. Transfersomes containing cholesterol displayed morphology with well-defined edges compared to cholesterol-free formulations. In vitro release studies revealed distinct release profiles, with cholesterol-free formulations releasing 70-83% of trans-resveratrol over 24 hours, compared to only 0-30% for cholesterol-containing formulations. Strat-M<sup>®</sup> membrane-based permeation studies confirmed enhanced trans-resveratrol delivery across all transfersomal systems compared to the saturated solution (p<0.05), though cholesterol showed no significant impact on permeation efficiency. These findings indicate that cholesterol influences release profile but has limited effect on permeation efficiency. Safety assessment using the Hen's Egg Test-Chorioallantoic Membrane (HET-CAM) assay classified the developed transfersomes as weak irritants, indicating their dermal safety. Notably, formulation F3, with a hydrogenated lecithin to cholesterol to Tween 60 ratio of 6:0:4, emerged as the optimal candidate, achieving the highest release rate (80.24% over 24 hours) while maintaining favorable permeation compared to control.</p><p><strong>Conclusion: </strong>These findings feature the potential of transfersomal systems, particularly cholesterol-free variants, as promising carriers for the effective and safe dermal delivery of trans-resveratrol.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"359-375"},"PeriodicalIF":2.4,"publicationDate":"2025-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12323873/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144789600","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-07-28eCollection Date: 2025-01-01DOI: 10.2147/NSA.S535362
Justyna Srebro, Ewelina Łyszczarz, Witold Brniak, Dorota Majda, Aleksander Mendyk
Purpose: Electrospinning enables the formation of nanofibers by elongating a polymer solution droplet in a high-voltage electrostatic field. The drug substance incorporated into nanofibrous matrix exhibits unique dissolution characteristics, modifiable by polymers selection. The physicochemical properties of the drug substance may also influence structural and functional attributes of the nanofibers. This study aimed to produce nanofibers loaded with small-molecule drugs - omeprazole (OMZ) and bisoprolol hemifumarate (BIS) to investigate how drug and polymer properties influence fiber formation and drug release. The effect of compression into minitablets on dissolution parameters was also assessed.
Methods: Ethanolic solutions of Eudragit® RL (ERL), Eudragit® RS (ERS), and polyvinylpyrrolidone (PVP) were mixed in 13 combinations. OMZ or BIS was dissolved in each mixture and electrospun. Selected nanofibers were compressed into minitablets. Nanofiber morphology, diameter, drug crystallinity and content uniformity were assessed. Dissolution profiles and release kinetics were evaluated for nanofibers and minitablets.
Results: Nanofibers morphology depended on the API and polymers composition. The BIS fibers were nanosized, while OMZ fibers showed heterogeneous thicknesses ranging from 0.54 µm to 5.7 µm. The drug substances were amorphous in nanofibers. OMZ formulations exhibited a sustained release except OMZ_PVP fibers, which released OMZ immediately. The BIS-loaded nanofibers demonstrated a rapid and nearly complete drug release, except for the BIS_ERL+ERS_7+3 formulation, which exhibited prolonged release. Compression of fibers into minitablets preserved the sustained drug release for both drug substances.
Conclusion: The study proves that nanofibers based on Eudragit RL/RS and PVP can be obtained by the electrospinning method. BIS properties such as good solubility, balanced hydrophobic-lipophilic nature, surface charge, and amorphous form contributed to its rapid release, unlike OMZ.
{"title":"Evaluation of the Effect of Formulation Composition and Physicochemical Properties of Omeprazole and Bisoprolol Hemifumarate on Electrospun Nanofibers Characteristics.","authors":"Justyna Srebro, Ewelina Łyszczarz, Witold Brniak, Dorota Majda, Aleksander Mendyk","doi":"10.2147/NSA.S535362","DOIUrl":"10.2147/NSA.S535362","url":null,"abstract":"<p><strong>Purpose: </strong>Electrospinning enables the formation of nanofibers by elongating a polymer solution droplet in a high-voltage electrostatic field. The drug substance incorporated into nanofibrous matrix exhibits unique dissolution characteristics, modifiable by polymers selection. The physicochemical properties of the drug substance may also influence structural and functional attributes of the nanofibers. This study aimed to produce nanofibers loaded with small-molecule drugs - omeprazole (OMZ) and bisoprolol hemifumarate (BIS) to investigate how drug and polymer properties influence fiber formation and drug release. The effect of compression into minitablets on dissolution parameters was also assessed.</p><p><strong>Methods: </strong>Ethanolic solutions of Eudragit<sup>®</sup> RL (ERL), Eudragit<sup>®</sup> RS (ERS), and polyvinylpyrrolidone (PVP) were mixed in 13 combinations. OMZ or BIS was dissolved in each mixture and electrospun. Selected nanofibers were compressed into minitablets. Nanofiber morphology, diameter, drug crystallinity and content uniformity were assessed. Dissolution profiles and release kinetics were evaluated for nanofibers and minitablets.</p><p><strong>Results: </strong>Nanofibers morphology depended on the API and polymers composition. The BIS fibers were nanosized, while OMZ fibers showed heterogeneous thicknesses ranging from 0.54 µm to 5.7 µm. The drug substances were amorphous in nanofibers. OMZ formulations exhibited a sustained release except OMZ_PVP fibers, which released OMZ immediately. The BIS-loaded nanofibers demonstrated a rapid and nearly complete drug release, except for the BIS_ERL+ERS_7+3 formulation, which exhibited prolonged release. Compression of fibers into minitablets preserved the sustained drug release for both drug substances.</p><p><strong>Conclusion: </strong>The study proves that nanofibers based on Eudragit RL/RS and PVP can be obtained by the electrospinning method. BIS properties such as good solubility, balanced hydrophobic-lipophilic nature, surface charge, and amorphous form contributed to its rapid release, unlike OMZ.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"295-318"},"PeriodicalIF":2.4,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12315909/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144775835","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-07-28eCollection Date: 2025-01-01DOI: 10.2147/NSA.S500407
Hao Huang, Yan Xuan, Zeng-Chun Ma
Background: Ferulic acid (FA) exhibits therapeutic potential for various disorders, but its clinical application is hindered by poor bioavailability and solubility. This study aimed to develop and evaluate FA-loaded lipid nanoparticles (FA-LNPs) as a safe and efficient drug delivery system.
Methods: FA-LNPs were prepared via an optimized active loading method. The Morris water maze test was conducted to evaluate FA efficacy against LPS-induced cognitive impairment in rats. Comprehensive neurotoxicity assessment was performed in three brain regions (striatum, hippocampus, and cerebellum-brain stem) using multiple staining techniques (LFB, GFAP, IBA-1, and Fluoro-Jade) to evaluate myelin integrity, glial activation, and neuronal degeneration. Acute toxicity, pharmacokinetics, and network pharmacology analysis were conducted to assess safety profiles and potential mechanisms.
Results: FA-LNPs were successfully prepared using an optimized active loading method, achieving high drug loading (≥4 mg/mL), superior encapsulation efficiency (EE%) ≥80%, and uniform particle size distribution (<200 nm, PDI=0.053), zeta potential of +5.97 mV (Quality Factor = 1.701), excellent storage stability over two weeks, and was scaled up for batch production. The Morris water maze test revealed an effective FA concentration of 50 mg/kg, with FA-LNPs achieving 46.5 mg/kg through active loading method. Toxicological studies demonstrated favorable safety profiles. Pharmacokinetic analysis showed a prolonged elimination half-life (12.8 ± 1.88 hours) and moderate systemic clearance (0.535 ± 0.0851 L/h/kg). Short-term administration did not elicit significant neuroprotection. Network pharmacology analysis identified 141 potential therapeutic targets and five key proteins (EGFR, ESR1, PTGS2, CTNNB1, and STAT3), with molecular docking confirming favorable binding energies (-7.6 to -5.2 kcal/mol).
Conclusion: FA-LNPs enhanced FA's bioavailability without apparent systemic toxicity or neurotoxicity. While safe for short-term use, longer treatment durations may be necessary to observe potential neuroprotective benefits and toxicity. This study provides a foundation for further investigation of FA-LNPs as a promising drug delivery system for neurological disorders.
{"title":"Safety Profile of Intravenous Ferulic Acid Nanoparticles: Acute Toxicity and Neurological Effects in Sprague-Dawley Rats.","authors":"Hao Huang, Yan Xuan, Zeng-Chun Ma","doi":"10.2147/NSA.S500407","DOIUrl":"10.2147/NSA.S500407","url":null,"abstract":"<p><strong>Background: </strong>Ferulic acid (FA) exhibits therapeutic potential for various disorders, but its clinical application is hindered by poor bioavailability and solubility. This study aimed to develop and evaluate FA-loaded lipid nanoparticles (FA-LNPs) as a safe and efficient drug delivery system.</p><p><strong>Methods: </strong>FA-LNPs were prepared via an optimized active loading method. The Morris water maze test was conducted to evaluate FA efficacy against LPS-induced cognitive impairment in rats. Comprehensive neurotoxicity assessment was performed in three brain regions (striatum, hippocampus, and cerebellum-brain stem) using multiple staining techniques (LFB, GFAP, IBA-1, and Fluoro-Jade) to evaluate myelin integrity, glial activation, and neuronal degeneration. Acute toxicity, pharmacokinetics, and network pharmacology analysis were conducted to assess safety profiles and potential mechanisms.</p><p><strong>Results: </strong>FA-LNPs were successfully prepared using an optimized active loading method, achieving high drug loading (≥4 mg/mL), superior encapsulation efficiency (EE%) ≥80%, and uniform particle size distribution (<200 nm, PDI=0.053), zeta potential of +5.97 mV (Quality Factor = 1.701), excellent storage stability over two weeks, and was scaled up for batch production. The Morris water maze test revealed an effective FA concentration of 50 mg/kg, with FA-LNPs achieving 46.5 mg/kg through active loading method. Toxicological studies demonstrated favorable safety profiles. Pharmacokinetic analysis showed a prolonged elimination half-life (12.8 ± 1.88 hours) and moderate systemic clearance (0.535 ± 0.0851 L/h/kg). Short-term administration did not elicit significant neuroprotection. Network pharmacology analysis identified 141 potential therapeutic targets and five key proteins (EGFR, ESR1, PTGS2, CTNNB1, and STAT3), with molecular docking confirming favorable binding energies (-7.6 to -5.2 kcal/mol).</p><p><strong>Conclusion: </strong>FA-LNPs enhanced FA's bioavailability without apparent systemic toxicity or neurotoxicity. While safe for short-term use, longer treatment durations may be necessary to observe potential neuroprotective benefits and toxicity. This study provides a foundation for further investigation of FA-LNPs as a promising drug delivery system for neurological disorders.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"319-358"},"PeriodicalIF":2.4,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12315901/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144775847","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-07-10eCollection Date: 2025-01-01DOI: 10.2147/NSA.S525423
Haitham Al-Madhagi
Mangiferin, a naturally occurring C-glucosylxanthone derived from various parts of the mango tree (Mangifera indica), has gained significant attention for its diverse pharmacological properties, including antioxidant, anti-inflammatory, antimicrobial, anticancer, and anti-diabetic activities. This mini-review provides an updated overview of the phytochemistry, pharmacokinetics, and medicinal properties of mangiferin. However, the low solubility (0.111 mg/mL) and oral bioavailability (less than 2%) of mangiferin pose significant challenges for its clinical application. To address these issues, the development of nanoformulations such as nanoparticles, micelles, and liposomes has been explored, which was proven to improve mangiferin's solubility, stability, and targeted delivery. These nanocarriers enhance the bioavailability and therapeutic efficacy of mangiferin, making it a promising candidate for various therapeutic applications. The review ends with the discussion of the safety of mangiferin and its formulations in addition to the potential for clinical translation.
{"title":"From Nature to Nanotechnology: The Bioactivities of Mangiferin Explored.","authors":"Haitham Al-Madhagi","doi":"10.2147/NSA.S525423","DOIUrl":"10.2147/NSA.S525423","url":null,"abstract":"<p><p>Mangiferin, a naturally occurring C-glucosylxanthone derived from various parts of the mango tree (<i>Mangifera indica</i>), has gained significant attention for its diverse pharmacological properties, including antioxidant, anti-inflammatory, antimicrobial, anticancer, and anti-diabetic activities. This mini-review provides an updated overview of the phytochemistry, pharmacokinetics, and medicinal properties of mangiferin. However, the low solubility (0.111 mg/mL) and oral bioavailability (less than 2%) of mangiferin pose significant challenges for its clinical application. To address these issues, the development of nanoformulations such as nanoparticles, micelles, and liposomes has been explored, which was proven to improve mangiferin's solubility, stability, and targeted delivery. These nanocarriers enhance the bioavailability and therapeutic efficacy of mangiferin, making it a promising candidate for various therapeutic applications. The review ends with the discussion of the safety of mangiferin and its formulations in addition to the potential for clinical translation.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"277-294"},"PeriodicalIF":4.9,"publicationDate":"2025-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12258238/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144637592","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-07eCollection Date: 2025-01-01DOI: 10.2147/NSA.S515639
Elżbieta Gumieniczek-Chłopek, Joanna Odrobińska-Baliś, Adriana Gilarska, Gabriela Opiła, Manuel Ricardo Ibarra, Czesław Kapusta, Szczepan Zapotoczny
Introduction: Drug delivery systems typically need to be equipped with targeting moieties in order to be efficiently internalized by cells. Alternatively, magnetic nanoparticles (MNs) combined with active compounds may be driven by magnetic field to the site of action. Delivery of hydrophobic drugs using this approach is challenging as it would require coupling of MNs and hydrophobic environment within nanocarriers and triggering of the drug release.
Methods: We propose an approach enabling a magnetically induced forced uptake of core-shell nanocapsules carrying hydrophobic actives together with hydrophobized MNs. Such capsules, formed in a facile emulsification process, are composed of amphiphilic cationic or anionic chitosan (shell) and oil-dispersible MNs (oil core). The capsules were characterized using DLS, cryo-TEM. They were loaded with a model fluorescent dye, Nile Red, and pulled into cells applying a static magnetic field. Then, they were treated with an alternating magnetic field to disrupt the capsules thanks to the action of MNs.
Results: Cryo-TEM imaging confirmed the presence of MNs inside the capsules (d≈200 nm). Confocal microscopy imaging showed the efficient capsules' intracellular uptake only after exposition to static magnetic field (some spontaneous uptake was observed for anionic capsules). Then, application of alternating magnetic fields induced rapture of the capsules inside the cells and release of the cargo.
Discussion: This approach is very versatile as various lipophilic compounds could be encapsulated, then transported to desired tissues without active or passive targeting and kept there using static magnetic field, limiting undesired side effects of a therapy to the whole organism. The proposed capsules with MNs respond efficiently to magnetic field stimulation - they can be magnetically navigated into the cells and release their cargo after application of alternating magnetic field. This approach opens opportunities for controlled intracellular delivery of hydrophobic actives using easily applicable magnetic stimuli for both delivery and release.
{"title":"Intracellular Uptake of Magnetic Nanocapsules with Ionic Chitosan Shells and Magnetically Triggered Cargo Release.","authors":"Elżbieta Gumieniczek-Chłopek, Joanna Odrobińska-Baliś, Adriana Gilarska, Gabriela Opiła, Manuel Ricardo Ibarra, Czesław Kapusta, Szczepan Zapotoczny","doi":"10.2147/NSA.S515639","DOIUrl":"10.2147/NSA.S515639","url":null,"abstract":"<p><strong>Introduction: </strong>Drug delivery systems typically need to be equipped with targeting moieties in order to be efficiently internalized by cells. Alternatively, magnetic nanoparticles (MNs) combined with active compounds may be driven by magnetic field to the site of action. Delivery of hydrophobic drugs using this approach is challenging as it would require coupling of MNs and hydrophobic environment within nanocarriers and triggering of the drug release.</p><p><strong>Methods: </strong>We propose an approach enabling a magnetically induced forced uptake of core-shell nanocapsules carrying hydrophobic actives together with hydrophobized MNs. Such capsules, formed in a facile emulsification process, are composed of amphiphilic cationic or anionic chitosan (shell) and oil-dispersible MNs (oil core). The capsules were characterized using DLS, cryo-TEM. They were loaded with a model fluorescent dye, Nile Red, and pulled into cells applying a static magnetic field. Then, they were treated with an alternating magnetic field to disrupt the capsules thanks to the action of MNs.</p><p><strong>Results: </strong>Cryo-TEM imaging confirmed the presence of MNs inside the capsules (d≈200 nm). Confocal microscopy imaging showed the efficient capsules' intracellular uptake only after exposition to static magnetic field (some spontaneous uptake was observed for anionic capsules). Then, application of alternating magnetic fields induced rapture of the capsules inside the cells and release of the cargo.</p><p><strong>Discussion: </strong>This approach is very versatile as various lipophilic compounds could be encapsulated, then transported to desired tissues without active or passive targeting and kept there using static magnetic field, limiting undesired side effects of a therapy to the whole organism. The proposed capsules with MNs respond efficiently to magnetic field stimulation - they can be magnetically navigated into the cells and release their cargo after application of alternating magnetic field. This approach opens opportunities for controlled intracellular delivery of hydrophobic actives using easily applicable magnetic stimuli for both delivery and release.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"263-275"},"PeriodicalIF":4.9,"publicationDate":"2025-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12153966/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144275440","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-06-06eCollection Date: 2025-01-01DOI: 10.2147/NSA.S520030
Anna Kieronska-Rudek, Agnieszka Kij, Anna Bar, Magdalena Sternak, Aleksandra Paterek, Filip Rolski, Izabela Czyzynska-Cichon, Filip A Fedak, Kamila Wojnar-Lason, Justyna Bednorz, Małgorzata Janik-Hazuka, Renata B Kostogrys, Magdalena Franczyk-Zarow, Katarzyna Z Czyżowska, Lenka Michalkova, Michał Mączewski, Szczepan Zapotoczny, Edyta Kus, Stefan Chlopicki
Introduction: As vitamin K1 (phylloquinone, PK) displays vasoprotective effect, low dietary intake and poor bioavailability of PK may result in insufficient systemic levels for maintaining vascular health. This study aimed to test whether PK in hyaluronan-based nanocapsules (PK-Oil-HyC12) improves PK pharmacokinetics and endothelial function compared to PK in oil emulsion (PK-Oil).
Methods: PK pharmacokinetics in plasma, liver and aorta were analysed after single, oral administration of PK (10 mg/kg) in oil (PK-Oil) or encapsulated in hyaluronan-based nanocapsules with oil core (PK-Oil-HyC12) in mice using liquid chromatography-tandem mass spectrometry with atmospheric pressure chemical ionization method. PK-Oil-HyC12 absorption and nanocapsules distribution in lymphatic system was determined using a cycloheximide-based chylomicron flow blockage and intravital confocal microscopy. The endothelial function was analyzed in vivo by MRI in mice with dietary PK deficiency after 7-day supplementation with PK-Oil or PK-Oil-HyC12 (0.5 mg PK/kg).
Results: After a single, oral dose of PK-Oil-HyC12 in mice total exposure of PK (AUC values) was 2-4 times higher as compared to PK-Oil in plasma and liver, with no difference in PK content in the aorta. The efficient absorption and distribution of nanocapsules occurred mainly via a chylomicron-independent lymphatic route. Importantly, 7-day PK-Oil-HyC12 supplementation restored impaired endothelium-dependent vasodilation in the aorta of PK-deficient mice, while PK-Oil was ineffective.
Conclusion: The improved bioavailability of PK, when administered in the form of hyaluronan-based nanocapsules, afforded the rapid replenishment of systemic PK and the reversal of endothelial dysfunction induced by low PK levels.
{"title":"Rapid Replenishment of Phylloquinone in the Plasma and Liver Using Hyaluronan-Based Nanocapsules Reverses Endothelial Dysfunction in Mice.","authors":"Anna Kieronska-Rudek, Agnieszka Kij, Anna Bar, Magdalena Sternak, Aleksandra Paterek, Filip Rolski, Izabela Czyzynska-Cichon, Filip A Fedak, Kamila Wojnar-Lason, Justyna Bednorz, Małgorzata Janik-Hazuka, Renata B Kostogrys, Magdalena Franczyk-Zarow, Katarzyna Z Czyżowska, Lenka Michalkova, Michał Mączewski, Szczepan Zapotoczny, Edyta Kus, Stefan Chlopicki","doi":"10.2147/NSA.S520030","DOIUrl":"10.2147/NSA.S520030","url":null,"abstract":"<p><strong>Introduction: </strong>As vitamin K<sub>1</sub> (phylloquinone, PK) displays vasoprotective effect, low dietary intake and poor bioavailability of PK may result in insufficient systemic levels for maintaining vascular health. This study aimed to test whether PK in hyaluronan-based nanocapsules (PK-Oil-HyC12) improves PK pharmacokinetics and endothelial function compared to PK in oil emulsion (PK-Oil).</p><p><strong>Methods: </strong>PK pharmacokinetics in plasma, liver and aorta were analysed after single, oral administration of PK (10 mg/kg) in oil (PK-Oil) or encapsulated in hyaluronan-based nanocapsules with oil core (PK-Oil-HyC12) in mice using liquid chromatography-tandem mass spectrometry with atmospheric pressure chemical ionization method. PK-Oil-HyC12 absorption and nanocapsules distribution in lymphatic system was determined using a cycloheximide-based chylomicron flow blockage and intravital confocal microscopy. The endothelial function was analyzed in vivo by MRI in mice with dietary PK deficiency after 7-day supplementation with PK-Oil or PK-Oil-HyC12 (0.5 mg PK/kg).</p><p><strong>Results: </strong>After a single, oral dose of PK-Oil-HyC12 in mice total exposure of PK (AUC values) was 2-4 times higher as compared to PK-Oil in plasma and liver, with no difference in PK content in the aorta. The efficient absorption and distribution of nanocapsules occurred mainly via a chylomicron-independent lymphatic route. Importantly, 7-day PK-Oil-HyC12 supplementation restored impaired endothelium-dependent vasodilation in the aorta of PK-deficient mice, while PK-Oil was ineffective.</p><p><strong>Conclusion: </strong>The improved bioavailability of PK, when administered in the form of hyaluronan-based nanocapsules, afforded the rapid replenishment of systemic PK and the reversal of endothelial dysfunction induced by low PK levels.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"245-262"},"PeriodicalIF":4.9,"publicationDate":"2025-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12151077/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144266659","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-05-07eCollection Date: 2025-01-01DOI: 10.2147/NSA.S519229
Shadha Nasser Aziz, Abduh Mohammad Abdulwahab, Thana Shuga Aldeen, Abdullah Ahmed Ali Ahmed
Introduction: The use of metal oxide nanoparticles as anticancer agents is of great interest due to their unique properties that allow targeted delivery at low concentrations with minimal toxicity to healthy cells.
Methods: In this work, CdO-CuO-ZnO mixed metal oxide nanocomposites were synthesized by the co-precipitation method, and their structural and optical properties, along with their anticancer activity, were investigated. The samples were characterized by X-ray diffraction (XRD), total reflection X-ray fluorescence (TXRF), transmission electron microscopy (TEM), selected area electron diffraction (SAED), UV-Vis spectroscopy, electrometer/high resistance material, and vibrating sample magnetometers (VSM).
Results: X-ray diffraction (XRD) measurements showed that CdO exhibits a cubic structure, CuO possesses a monoclinic structure, ZnO displays a hexagonal structure, and the mixture showed peaks corresponding to all three oxides. TEM images revealed that the prepared nanoparticles have quasi-spherical shapes. Anticancer studies confirmed that the CdO-CuO-ZnO nanocomposite demonstrates excellent cytotoxicity, with moderate activity against human colon (Caco-2) and lung (A549) cancer cell lines, exhibiting IC50 values of 10.57 μg/mL and 6.61 μg/mL, respectively.
Conclusion: Our study shows that the prepared CdO-CuO-ZnO nanocomposite has massive potential in cancer therapy.
{"title":"Tailoring CdO-CuO-ZnO Mixed Metal Oxide Nanocomposites for Anticancer Activity via Co-Precipitation Method.","authors":"Shadha Nasser Aziz, Abduh Mohammad Abdulwahab, Thana Shuga Aldeen, Abdullah Ahmed Ali Ahmed","doi":"10.2147/NSA.S519229","DOIUrl":"https://doi.org/10.2147/NSA.S519229","url":null,"abstract":"<p><strong>Introduction: </strong>The use of metal oxide nanoparticles as anticancer agents is of great interest due to their unique properties that allow targeted delivery at low concentrations with minimal toxicity to healthy cells.</p><p><strong>Methods: </strong>In this work, CdO-CuO-ZnO mixed metal oxide nanocomposites were synthesized by the co-precipitation method, and their structural and optical properties, along with their anticancer activity, were investigated. The samples were characterized by X-ray diffraction (XRD), total reflection X-ray fluorescence (TXRF), transmission electron microscopy (TEM), selected area electron diffraction (SAED), UV-Vis spectroscopy, electrometer/high resistance material, and vibrating sample magnetometers (VSM).</p><p><strong>Results: </strong>X-ray diffraction (XRD) measurements showed that CdO exhibits a cubic structure, CuO possesses a monoclinic structure, ZnO displays a hexagonal structure, and the mixture showed peaks corresponding to all three oxides. TEM images revealed that the prepared nanoparticles have quasi-spherical shapes. Anticancer studies confirmed that the CdO-CuO-ZnO nanocomposite demonstrates excellent cytotoxicity, with moderate activity against human colon (Caco-2) and lung (A549) cancer cell lines, exhibiting IC50 values of 10.57 μg/mL and 6.61 μg/mL, respectively.</p><p><strong>Conclusion: </strong>Our study shows that the prepared CdO-CuO-ZnO nanocomposite has massive potential in cancer therapy.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"225-244"},"PeriodicalIF":4.9,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067457/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143991007","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-05-07eCollection Date: 2025-01-01DOI: 10.2147/NSA.S520121
Yohannes Gelaye, Huaiyong Luo
Aflatoxin contamination poses a significant challenge to global food safety, public health, and agricultural sustainability. Traditional methods for mitigating aflatoxins, such as chemical and physical detoxification techniques, often raise concerns about environmental harm, nutrient loss, and potential toxicity. In contrast, green-synthesized nanomaterials have emerged as an environmentally friendly and effective solution for controlling aflatoxins. This study explores the potential of green-synthesized nanomaterials for aflatoxin mitigation, focusing on their mechanisms of action, effectiveness, and long-term applicability in agricultural and food safety contexts. A comprehensive review of 116 articles on the latest developments in green nanotechnology was used, focusing on the creation, characterization, and application of nanoparticles, including silver, zinc oxide, titanium dioxide, and iron-based nanomaterials. Green nanoparticles reduce aflatoxin load primarily through their antioxidant properties, which neutralize oxidative stress, and their high adsorption capacity, which binds aflatoxins and reduces their bioavailability. Photocatalytic degradation, adsorption, and enzymatic detoxification were also evaluated. The results indicate that green-synthesized nanoparticles exhibit high efficacy, biocompatibility, and minimal environmental impact, especially when compared to traditional detoxification methods. However, challenges such as nanoparticle stability, large-scale production, regulatory issues, and potential long-term toxicity still require further investigation. To advance this field, future studies should focus on refining green synthesis processes, enhancing nanoparticle stability, and exploring the integration of nanotechnology with biosensors and smart packaging for real-time aflatoxin monitoring. By advancing these sustainable technologies, this research aims to contribute to the development of effective and safe methods for aflatoxin mitigation, thereby supporting global food security, public health, and environmental sustainability.
{"title":"Green-Synthesized Nanomaterials for Aflatoxin Mitigation: A Review.","authors":"Yohannes Gelaye, Huaiyong Luo","doi":"10.2147/NSA.S520121","DOIUrl":"https://doi.org/10.2147/NSA.S520121","url":null,"abstract":"<p><p>Aflatoxin contamination poses a significant challenge to global food safety, public health, and agricultural sustainability. Traditional methods for mitigating aflatoxins, such as chemical and physical detoxification techniques, often raise concerns about environmental harm, nutrient loss, and potential toxicity. In contrast, green-synthesized nanomaterials have emerged as an environmentally friendly and effective solution for controlling aflatoxins. This study explores the potential of green-synthesized nanomaterials for aflatoxin mitigation, focusing on their mechanisms of action, effectiveness, and long-term applicability in agricultural and food safety contexts. A comprehensive review of 116 articles on the latest developments in green nanotechnology was used, focusing on the creation, characterization, and application of nanoparticles, including silver, zinc oxide, titanium dioxide, and iron-based nanomaterials. Green nanoparticles reduce aflatoxin load primarily through their antioxidant properties, which neutralize oxidative stress, and their high adsorption capacity, which binds aflatoxins and reduces their bioavailability. Photocatalytic degradation, adsorption, and enzymatic detoxification were also evaluated. The results indicate that green-synthesized nanoparticles exhibit high efficacy, biocompatibility, and minimal environmental impact, especially when compared to traditional detoxification methods. However, challenges such as nanoparticle stability, large-scale production, regulatory issues, and potential long-term toxicity still require further investigation. To advance this field, future studies should focus on refining green synthesis processes, enhancing nanoparticle stability, and exploring the integration of nanotechnology with biosensors and smart packaging for real-time aflatoxin monitoring. By advancing these sustainable technologies, this research aims to contribute to the development of effective and safe methods for aflatoxin mitigation, thereby supporting global food security, public health, and environmental sustainability.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"211-223"},"PeriodicalIF":4.9,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067452/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144007949","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-04-14eCollection Date: 2025-01-01DOI: 10.2147/NSA.S509925
Anna Pajor-Świerzy, Krzysztof Szczepanowicz
This mini-review paper gives a brief summary of recent works in the development of bimetallic core@shell nanoparticles composed of nickel (as a core) and a silver shell (Ni@Ag NPs). We present the methods of Ni@Ag NPs synthesis, ink preparation, and their coatings formation. We also place emphasis on the selection and optimization of the sintering process of materials based on Ni@Ag NPs. Finally, the challenges in the application of Ni@Ag NPs in printed conductive structures are presented.
{"title":"The Recent Progress on Nickel@Silver Metals Core@Shell Nanoparticles Application in Printed Conductive Materials - A Mini-Review.","authors":"Anna Pajor-Świerzy, Krzysztof Szczepanowicz","doi":"10.2147/NSA.S509925","DOIUrl":"https://doi.org/10.2147/NSA.S509925","url":null,"abstract":"<p><p>This mini-review paper gives a brief summary of recent works in the development of bimetallic core@shell nanoparticles composed of nickel (as a core) and a silver shell (Ni@Ag NPs). We present the methods of Ni@Ag NPs synthesis, ink preparation, and their coatings formation. We also place emphasis on the selection and optimization of the sintering process of materials based on Ni@Ag NPs. Finally, the challenges in the application of Ni@Ag NPs in printed conductive structures are presented.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"197-210"},"PeriodicalIF":4.9,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12007610/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144018730","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2025-04-12eCollection Date: 2025-01-01DOI: 10.2147/NSA.S495377
Piotr Gas, Muhammad Suleman, Farah Khaliq
Background: Nanotechnology can be used to treat a diversity of cancers with different physiological properties. Skin cancers are common among people affected by an excessive solar radiation of the ultraviolet (UV) range.
Introduction: This paper describes a mathematical formulation and simulation approach for the magnetic hyperthermia therapy of skin cancer using gold-coated iron oxide (Fe3O4@Au) magnetic nanoparticles (MNPs).
Methods: The authors created an artificial 3D geometry model of skin cancer with tissue-mimicking materials, constructed a mesh, and solved all the required physics for electro-thermal simulation using FEM-based software. The heat transfer in the skin tissue was modeled using the Pennes bioheat equation, and the Helmholtz-type equation of quasi-static magnetic field produced by a three-turned coil surrounding the tumor.
Results: The simulated magnetic field pattern was compared with that of the analytical solution along the symmetry axis of the helical coil with good agreement. The obtained results show that the tumor damage is maximum in the tumor center and decreases towards its outer boundaries. Additionally, the impact of varying values of blood perfusion rate, blood density, blood specific heat capacity, heat dissipation produced by Fe3O4@Au MNPs, and metabolic heat generation has been examined for thermal therapy. The performed simulations show that all these parameters influences heating characteristics of tumor tissues by gold-coated magnetic nanoparticles.
Conclusion: Gold-iron oxide magnetic nanoparticles succeeded to damage 90-99% skin cancer. Among all the contributing parameters, the blood perfusion is the most sensitive parameter in thermal therapy of skin tumor.
Recommendations: On the bases of results obtained, we recommend physicians to use Fe3O4@Au MNPs in real time medical skin cancer treatments.
{"title":"3D Computational Modeling of Fe<sub>3</sub>O<sub>4</sub>@Au Nanoparticles in Hyperthermia Treatment of Skin Cancer.","authors":"Piotr Gas, Muhammad Suleman, Farah Khaliq","doi":"10.2147/NSA.S495377","DOIUrl":"https://doi.org/10.2147/NSA.S495377","url":null,"abstract":"<p><strong>Background: </strong>Nanotechnology can be used to treat a diversity of cancers with different physiological properties. Skin cancers are common among people affected by an excessive solar radiation of the ultraviolet (UV) range.</p><p><strong>Introduction: </strong>This paper describes a mathematical formulation and simulation approach for the magnetic hyperthermia therapy of skin cancer using gold-coated iron oxide (Fe<sub>3</sub>O<sub>4</sub>@Au) magnetic nanoparticles (MNPs).</p><p><strong>Methods: </strong>The authors created an artificial 3D geometry model of skin cancer with tissue-mimicking materials, constructed a mesh, and solved all the required physics for electro-thermal simulation using FEM-based software. The heat transfer in the skin tissue was modeled using the Pennes bioheat equation, and the Helmholtz-type equation of quasi-static magnetic field produced by a three-turned coil surrounding the tumor.</p><p><strong>Results: </strong>The simulated magnetic field pattern was compared with that of the analytical solution along the symmetry axis of the helical coil with good agreement. The obtained results show that the tumor damage is maximum in the tumor center and decreases towards its outer boundaries. Additionally, the impact of varying values of blood perfusion rate, blood density, blood specific heat capacity, heat dissipation produced by Fe<sub>3</sub>O<sub>4</sub>@Au MNPs, and metabolic heat generation has been examined for thermal therapy. The performed simulations show that all these parameters influences heating characteristics of tumor tissues by gold-coated magnetic nanoparticles.</p><p><strong>Conclusion: </strong>Gold-iron oxide magnetic nanoparticles succeeded to damage 90-99% skin cancer. Among all the contributing parameters, the blood perfusion is the most sensitive parameter in thermal therapy of skin tumor.</p><p><strong>Recommendations: </strong>On the bases of results obtained, we recommend physicians to use Fe<sub>3</sub>O<sub>4</sub>@Au MNPs in real time medical skin cancer treatments.</p>","PeriodicalId":18881,"journal":{"name":"Nanotechnology, Science and Applications","volume":"18 ","pages":"173-196"},"PeriodicalIF":4.9,"publicationDate":"2025-04-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12002342/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143971925","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}