Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and Cyclodextrin
In this present study, we developed and characterized a series of supramolecular G4 hydrogels by integrating <i>β</i>-cyclodextrin (<i>β</i>-CD) and boronic acid linkers into a supramolecular matrix to enhance antibacterial activity against <i>Staphylococcus aureus</...
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2025-01-01
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| author | Monica-Cornelia Sardaru Irina Rosca Simona Morariu Elena-Laura Ursu Alexandru Rotaru |
| author_facet | Monica-Cornelia Sardaru Irina Rosca Simona Morariu Elena-Laura Ursu Alexandru Rotaru |
| author_sort | Monica-Cornelia Sardaru |
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| description | In this present study, we developed and characterized a series of supramolecular G4 hydrogels by integrating <i>β</i>-cyclodextrin (<i>β</i>-CD) and boronic acid linkers into a supramolecular matrix to enhance antibacterial activity against <i>Staphylococcus aureus</i> (<i>S. aureus</i>). We systematically investigated how varying the number of free boronic acid moieties (ranging from two to six), along with guanosine and β-CD content, influences both the structural integrity and antimicrobial efficacy of these materials. Comprehensive characterization using FTIR, circular dichroism, X-ray diffraction, SEM, AFM, and rheological measurements confirmed successful synthesis and revealed that higher boronic acid content correlated with a stronger, more organized network. The most effective hydrogel displayed an inhibition zone of 25 mm in disk diffusion assays, and was further explored as a drug delivery platform, with the aim to exploit the capacity of the free <i>β</i>-CD cavity of the hydrogels to incorporate hydrophobic drugs. Norfloxacin (Nfx), a poorly water-soluble antibiotic, was successfully encapsulated within the hydrogel matrix through the inclusion of complex formation with <i>β</i>-CD, improving its solubility and enabling sustained, targeted release. The Nfx-loaded hydrogel expanded the inhibition zone to 49 mm and completely eradicated <i>S. aureus</i> cells within 24 h, outperforming both the unloaded hydrogel and free Nfx. These results highlight the synergistic effect of boronic acid moieties and controlled drug release, underlining the potential of these hydrogels as versatile platforms for localized antimicrobial therapy, such as in wound dressings or implant coatings. Nevertheless, further in vivo studies and long-term stability assessments are needed to fully establish clinical relevance, safety, and scalability before these systems can be translated into routine healthcare applications. |
| format | Article |
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| institution | Kabale University |
| issn | 2310-2861 |
| language | English |
| publishDate | 2025-01-01 |
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| series | Gels |
| spelling | doaj-art-b55eb79017bc418ba0d2431af6a3a70e2025-01-24T13:33:51ZengMDPI AGGels2310-28612025-01-011113510.3390/gels11010035Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and CyclodextrinMonica-Cornelia Sardaru0Irina Rosca1Simona Morariu2Elena-Laura Ursu3Alexandru Rotaru4The Research Institute of the University of Bucharest (ICUB), 90 Sos. Panduri, 050663 Bucharest, Romania“Petru Poni” Institute of Macromolecular Chemistry, Romanian Academy, Centre of Advanced Research in Bionanoconjugates and Biopolymers, Grigore Ghica Voda Alley 41 A, 700487 Iasi, Romania“Petru Poni” Institute of Macromolecular Chemistry, Romanian Academy, Natural Polymers, Bioactive and Biocompatible Materials, Grigore Ghica Voda Alley 41 A, 700487 Iasi, Romania“Petru Poni” Institute of Macromolecular Chemistry, Romanian Academy, Centre of Advanced Research in Bionanoconjugates and Biopolymers, Grigore Ghica Voda Alley 41 A, 700487 Iasi, Romania“Petru Poni” Institute of Macromolecular Chemistry, Romanian Academy, Centre of Advanced Research in Bionanoconjugates and Biopolymers, Grigore Ghica Voda Alley 41 A, 700487 Iasi, RomaniaIn this present study, we developed and characterized a series of supramolecular G4 hydrogels by integrating <i>β</i>-cyclodextrin (<i>β</i>-CD) and boronic acid linkers into a supramolecular matrix to enhance antibacterial activity against <i>Staphylococcus aureus</i> (<i>S. aureus</i>). We systematically investigated how varying the number of free boronic acid moieties (ranging from two to six), along with guanosine and β-CD content, influences both the structural integrity and antimicrobial efficacy of these materials. Comprehensive characterization using FTIR, circular dichroism, X-ray diffraction, SEM, AFM, and rheological measurements confirmed successful synthesis and revealed that higher boronic acid content correlated with a stronger, more organized network. The most effective hydrogel displayed an inhibition zone of 25 mm in disk diffusion assays, and was further explored as a drug delivery platform, with the aim to exploit the capacity of the free <i>β</i>-CD cavity of the hydrogels to incorporate hydrophobic drugs. Norfloxacin (Nfx), a poorly water-soluble antibiotic, was successfully encapsulated within the hydrogel matrix through the inclusion of complex formation with <i>β</i>-CD, improving its solubility and enabling sustained, targeted release. The Nfx-loaded hydrogel expanded the inhibition zone to 49 mm and completely eradicated <i>S. aureus</i> cells within 24 h, outperforming both the unloaded hydrogel and free Nfx. These results highlight the synergistic effect of boronic acid moieties and controlled drug release, underlining the potential of these hydrogels as versatile platforms for localized antimicrobial therapy, such as in wound dressings or implant coatings. Nevertheless, further in vivo studies and long-term stability assessments are needed to fully establish clinical relevance, safety, and scalability before these systems can be translated into routine healthcare applications.https://www.mdpi.com/2310-2861/11/1/35supramolecular hydrogelguanosine quartet<i>β</i>-cyclodextrin<i>Staphylococcus aureus</i>Norfloxacin |
| spellingShingle | Monica-Cornelia Sardaru Irina Rosca Simona Morariu Elena-Laura Ursu Alexandru Rotaru Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and Cyclodextrin Gels supramolecular hydrogel guanosine quartet <i>β</i>-cyclodextrin <i>Staphylococcus aureus</i> Norfloxacin |
| title | Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and Cyclodextrin |
| title_full | Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and Cyclodextrin |
| title_fullStr | Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and Cyclodextrin |
| title_full_unstemmed | Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and Cyclodextrin |
| title_short | Synergistic Antibacterial Action of Norfloxacin-Encapsulated G4 Hydrogels: The Role of Boronic Acid and Cyclodextrin |
| title_sort | synergistic antibacterial action of norfloxacin encapsulated g4 hydrogels the role of boronic acid and cyclodextrin |
| topic | supramolecular hydrogel guanosine quartet <i>β</i>-cyclodextrin <i>Staphylococcus aureus</i> Norfloxacin |
| url | https://www.mdpi.com/2310-2861/11/1/35 |
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