Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial Activity
Currently, problems related to antibiotic resistance are shifting the focus of pharmaceutical research towards natural molecules with antibacterial properties. Among them, flavonoids represent promising molecules with strong antibacterial features; however, they have poor biopharmaceutical propertie...
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| Format: | Article |
| Language: | English |
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MDPI AG
2025-02-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/18/2/232 |
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| author | Federica De Gaetano Francesco Caridi Noemi Totaro Consuelo Celesti Valentina Venuti Giovanna Ginestra Antonia Nostro Silvana Tommasini Cinzia Anna Ventura Rosanna Stancanelli |
| author_facet | Federica De Gaetano Francesco Caridi Noemi Totaro Consuelo Celesti Valentina Venuti Giovanna Ginestra Antonia Nostro Silvana Tommasini Cinzia Anna Ventura Rosanna Stancanelli |
| author_sort | Federica De Gaetano |
| collection | DOAJ |
| description | Currently, problems related to antibiotic resistance are shifting the focus of pharmaceutical research towards natural molecules with antibacterial properties. Among them, flavonoids represent promising molecules with strong antibacterial features; however, they have poor biopharmaceutical properties. In this study, we developed solid lipid nanoparticles (SLNs) loaded with the flavanone naringenin (NRG) to offer an option for treating bacterial infections. NRG-SLNs systems were prepared by a solvent emulsification/diffusion and ultrasonication method, using Compritol<sup>®</sup> 888 ATO (COM) as the lipid. The optimal formulation was obtained using a 10% (<i>w</i>/<i>w</i>) theoretical amount of NRG (NRG<sub>10</sub>-SLNs), exhibiting homogeneous sizes (approximately 50 nm and 0.15 polydispersity index), negative zeta potential (−30 mV), and excellent encapsulation parameters (an encapsulation efficiency percentage of 97.9% and a drug content of 4%). NRG<sub>10</sub>-SLNs presented good physical stability over 4 weeks. A cumulative drug release of 55% in 24 h and the prolonged release of the remaining amount over 10 days was observed. In addition, µ-Raman spectroscopy, differential scanning calorimetry, thermogravimetric analysis, and X-ray diffraction measurements were carried out to characterize the drug–lipid interactions. Finally, the in vitro antibacterial and antibiofilm activities of NRG<sub>10</sub>-SLNs were assayed and compared to free NRG. NRG<sub>10</sub>-SLNs were bacteriostatic against <i>Staphylococcus aureus,</i> including the methicillin-resistant <i>S. aureus</i> (MRSA) and <i>Escherichia coli</i> strains. An improvement in the antibacterial activity of NRG-loaded SLNs compared to the free molecule was observed against <i>S. aureus</i> strains, probably due to the interaction of the surfactant-coated SLNs with the bacterial surface. A similar trend was observed for the biofilm inhibition. |
| first_indexed | 2025-03-14T14:54:01Z |
| format | Article |
| id | doaj.art-58aa97e5f8834d8499242da8be8ad95e |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2025-03-14T14:54:01Z |
| publishDate | 2025-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-58aa97e5f8834d8499242da8be8ad95e2025-02-25T13:42:43ZengMDPI AGPharmaceuticals1424-82472025-02-0118223210.3390/ph18020232Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial ActivityFederica De Gaetano0Francesco Caridi1Noemi Totaro2Consuelo Celesti3Valentina Venuti4Giovanna Ginestra5Antonia Nostro6Silvana Tommasini7Cinzia Anna Ventura8Rosanna Stancanelli9Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Mathematical and Computer Sciences, Physical Sciences and Earth Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Engineering, University of Messina, Contrada Di Dio, 98166 Messina, ItalyDepartment of Mathematical and Computer Sciences, Physical Sciences and Earth Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, V.le Ferdinando Stagno D’Alcontres 31, 98166 Messina, ItalyCurrently, problems related to antibiotic resistance are shifting the focus of pharmaceutical research towards natural molecules with antibacterial properties. Among them, flavonoids represent promising molecules with strong antibacterial features; however, they have poor biopharmaceutical properties. In this study, we developed solid lipid nanoparticles (SLNs) loaded with the flavanone naringenin (NRG) to offer an option for treating bacterial infections. NRG-SLNs systems were prepared by a solvent emulsification/diffusion and ultrasonication method, using Compritol<sup>®</sup> 888 ATO (COM) as the lipid. The optimal formulation was obtained using a 10% (<i>w</i>/<i>w</i>) theoretical amount of NRG (NRG<sub>10</sub>-SLNs), exhibiting homogeneous sizes (approximately 50 nm and 0.15 polydispersity index), negative zeta potential (−30 mV), and excellent encapsulation parameters (an encapsulation efficiency percentage of 97.9% and a drug content of 4%). NRG<sub>10</sub>-SLNs presented good physical stability over 4 weeks. A cumulative drug release of 55% in 24 h and the prolonged release of the remaining amount over 10 days was observed. In addition, µ-Raman spectroscopy, differential scanning calorimetry, thermogravimetric analysis, and X-ray diffraction measurements were carried out to characterize the drug–lipid interactions. Finally, the in vitro antibacterial and antibiofilm activities of NRG<sub>10</sub>-SLNs were assayed and compared to free NRG. NRG<sub>10</sub>-SLNs were bacteriostatic against <i>Staphylococcus aureus,</i> including the methicillin-resistant <i>S. aureus</i> (MRSA) and <i>Escherichia coli</i> strains. An improvement in the antibacterial activity of NRG-loaded SLNs compared to the free molecule was observed against <i>S. aureus</i> strains, probably due to the interaction of the surfactant-coated SLNs with the bacterial surface. A similar trend was observed for the biofilm inhibition.https://www.mdpi.com/1424-8247/18/2/232naringeninsolid lipid nanoparticlestechnological characterizationphysical–chemical characterizationin vitro antibacterial activitybiofilm inhibition |
| spellingShingle | Federica De Gaetano Francesco Caridi Noemi Totaro Consuelo Celesti Valentina Venuti Giovanna Ginestra Antonia Nostro Silvana Tommasini Cinzia Anna Ventura Rosanna Stancanelli Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial Activity Pharmaceuticals naringenin solid lipid nanoparticles technological characterization physical–chemical characterization in vitro antibacterial activity biofilm inhibition |
| title | Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial Activity |
| title_full | Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial Activity |
| title_fullStr | Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial Activity |
| title_full_unstemmed | Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial Activity |
| title_short | Naringenin-Loaded Solid Lipid Nanoparticles: Physical–Chemical Characterization and In Vitro Antibacterial Activity |
| title_sort | naringenin loaded solid lipid nanoparticles physical chemical characterization and in vitro antibacterial activity |
| topic | naringenin solid lipid nanoparticles technological characterization physical–chemical characterization in vitro antibacterial activity biofilm inhibition |
| url | https://www.mdpi.com/1424-8247/18/2/232 |
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