PVP-Stabilized Ag@SiO₂ Nanocarriers for Usnic Acid: Physicochemical Characterization and Exploratory in vitro Anticancer, Antimicrobial, and Immunomodulatory Activity.
5 affiliations
- 1Department of Physiology, Medical University of Gdańsk, Gdańsk, Poland.
- 2Department of Analytical Chemistry, Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland.
- 3Department of Bacterial Molecular Genetics, University of Gdańsk, Gdańsk, Poland.
- 4Department of Medical Biology and Genetics, Faculty of Biology, University of Gdańsk, Gdańsk, Poland.
- 5Department of Biochemistry, Medical University of Gdańsk, Gdańsk, Poland.
Abstract
Background
Usnic acid (UA) is a lichen-derived metabolite with recognized anticancer, anti-inflammatory, and antibacterial properties; however, its clinical application is limited by poor aqueous solubility and dose-dependent toxicity. This study aimed to develop a multifunctional nanosystem to improve UA aqueous dispersibility and efficacy against breast cancer cells in vitro.Methods
A nanosystem consisting of a silver core-silica shell coated with polyvinylpyrrolidone (PVP) and conjugated UA (Ag@SiO₂/PVP/UA) was synthesized and characterized regarding morphology, physicochemical properties, colloidal stability, drug loading, and release behavior. Antiproliferative activity was evaluated using breast cancer cells (MCF-7 and MDA-MB-231). Cytotoxicity was assessed using the MTT viability assay, reactive oxygen species (ROS) production by flow cytometry, and metabolic alterations through LC-MS/MS-based metabolomic analysis. Antimicrobial activity against Gram-positive and Gram-negative bacteria was expressed by minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). Immunomodulatory properties were assessed in human peripheral blood mononuclear cells (PBMCs) using ELISA, while fibroblast migration was analyzed using an in vitro wound healing assay.Results
The developed nanostructures exhibited a stable core-shell architecture, uniform particle size (~200 nm), and enhanced hydrophilicity, resulting in improved aqueous dispersibility and sustained UA release. Nanoencapsulation significantly enhanced UA's anticancer activity against breast cancer cells in vitro while maintaining lower toxicity toward normal cells. Mechanistically, Ag@SiO₂/PVP/UA induced ROS-mediated oxidative stress and metabolic reprogramming associated with altered purine metabolism, lipid biosynthesis, redox balance, and activation of glycolytic pathways. The nanosystem also demonstrated broad-spectrum antimicrobial activity, including improved efficacy against methicillin-resistant Staphylococcus aureus (MRSA) and selected Gram-negative bacteria, while exerting immunomodulatory effects by reducing pro-inflammatory cytokine secretion and enhancing IL-10 production without affecting fibroblast migration.Conclusion
Ag@SiO₂/PVP/UA represents a promising multifunctional therapeutic platform combining enhanced anticancer efficacy with antimicrobial and anti-inflammatory properties, potentially improving the therapeutic applicability of UA.
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BibTeX
@article{pyrczakfelczykowska2026pvpstabilized,
title = {{PVP-Stabilized Ag@SiO₂ Nanocarriers for Usnic Acid: Physicochemical Characterization and Exploratory in vitro Anticancer, Antimicrobial, and Immunomodulatory Activity.}},
author = {Agnieszka Pyrczak-Felczykowska and Agata Kowalska and Elżbieta Adamska and Aleksandra Bogucka and Katarzyna Zima and Dariusz Nowicki and Klaudia Żuczek and Anna Wcisło and Beata Grobelna and Krzysztof Urbanowicz and Magdalena Zabielska-Kaczorowska and Anna Herman-Antosiewicz},
journal = {International journal of nanomedicine},
year = {2026},
month = oct,
doi = {10.2147/ijn.s629377},
url = {https://europepmc.org/article/MED/42898922},
note = {CC BY-NC},
}
RIS
TY - JOUR
TI - PVP-Stabilized Ag@SiO₂ Nanocarriers for Usnic Acid: Physicochemical Characterization and Exploratory in vitro Anticancer, Antimicrobial, and Immunomodulatory Activity.
AU - Agnieszka Pyrczak-Felczykowska
AU - Agata Kowalska
AU - Elżbieta Adamska
AU - Aleksandra Bogucka
AU - Katarzyna Zima
AU - Dariusz Nowicki
AU - Klaudia Żuczek
AU - Anna Wcisło
AU - Beata Grobelna
AU - Krzysztof Urbanowicz
AU - Magdalena Zabielska-Kaczorowska
AU - Anna Herman-Antosiewicz
PY - 2026
DA - 2026/10/15
JO - International journal of nanomedicine
DO - 10.2147/ijn.s629377
UR - https://europepmc.org/article/MED/42898922
AB - Background Usnic acid (UA) is a lichen-derived metabolite with recognized anticancer, anti-inflammatory, and antibacterial properties; however, its clinical application is limited by poor aqueous solubility and dose-dependent toxicity. This study aimed to develop a multifunctional nanosystem to improve UA aqueous dispersibility and efficacy against breast cancer cells in vitro.Methods A nanosystem consisting of a silver core-silica shell coated with polyvinylpyrrolidone (PVP) and conjugated UA (Ag@SiO₂/PVP/UA) was synthesized and characterized regarding morphology, physicochemical properties, colloidal stability, drug loading, and release behavior. Antiproliferative activity was evaluated using breast cancer cells (MCF-7 and MDA-MB-231). Cytotoxicity was assessed using the MTT viability assay, reactive oxygen species (ROS) production by flow cytometry, and metabolic alterations through LC-MS/MS-based metabolomic analysis. Antimicrobial activity against Gram-positive and Gram-negative bacteria was expressed by minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). Immunomodulatory properties were assessed in human peripheral blood mononuclear cells (PBMCs) using ELISA, while fibroblast migration was analyzed using an in vitro wound healing assay.Results The developed nanostructures exhibited a stable core-shell architecture, uniform particle size (~200 nm), and enhanced hydrophilicity, resulting in improved aqueous dispersibility and sustained UA release. Nanoencapsulation significantly enhanced UA's anticancer activity against breast cancer cells in vitro while maintaining lower toxicity toward normal cells. Mechanistically, Ag@SiO₂/PVP/UA induced ROS-mediated oxidative stress and metabolic reprogramming associated with altered purine metabolism, lipid biosynthesis, redox balance, and activation of glycolytic pathways. The nanosystem also demonstrated broad-spectrum antimicrobial activity, including improved efficacy against methicillin-resistant Staphylococcus aureus (MRSA) and selected Gram-negative bacteria, while exerting immunomodulatory effects by reducing pro-inflammatory cytokine secretion and enhancing IL-10 production without affecting fibroblast migration.Conclusion Ag@SiO₂/PVP/UA represents a promising multifunctional therapeutic platform combining enhanced anticancer efficacy with antimicrobial and anti-inflammatory properties, potentially improving the therapeutic applicability of UA.
SN - 1176-9114
SN - 1178-2013
ER -