Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual Cooperation
A pyrazole derivative (CB1) was previously evaluated in vivo for various pharmacological activities (with the exception of antimicrobial effects), using DMSO as the administrative medium, mainly due to its water insolubility. Considering the global necessity for new antimicrobial agents, CB1 attract...
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| Format: | Article |
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MDPI AG
2022-04-01
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| Series: | Nanomaterials |
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| Online Access: | https://www.mdpi.com/2079-4991/12/7/1215 |
| _version_ | 1797438198806216704 |
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| author | Silvana Alfei Guendalina Zuccari Debora Caviglia Chiara Brullo |
| author_facet | Silvana Alfei Guendalina Zuccari Debora Caviglia Chiara Brullo |
| author_sort | Silvana Alfei |
| collection | DOAJ |
| description | A pyrazole derivative (CB1) was previously evaluated in vivo for various pharmacological activities (with the exception of antimicrobial effects), using DMSO as the administrative medium, mainly due to its water insolubility. Considering the global necessity for new antimicrobial agents, CB1 attracted our attention as a candidate to meet this need, mainly because the secondary amine group in its structure would make it possible to obtain its hydrochloride salt (CB1H), thus effortlessly solving its water-solubility drawbacks. In preliminary microbiologic investigations on Gram-negative and Gram-positive bacteria, CB1H displayed weak antibacterial effects on MDR isolates of Gram-positive species, nonetheless better than those displayed by the commonly-used available antibiotics. Therefore, aiming at improving such activity and extending the antibacterial spectrum of CB1H to Gram-negative pathogens, in this first work CB1 was strategically formulated in nanoparticles using a cationic copolymer (P7) previously developed by us, possessing potent broad-spectrum bactericidal activity. Using the nanoprecipitation method, CB1H-loaded polymer nanoparticles (CB1H-P7 NPs) were obtained, which were analyzed by attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopy to confirm the successful loading. Additionally, CB1H-P7 NPs were fully characterized in terms of morphology, size, polydispersity indices, surface charge, DL%, and EE%, as well as release and potentiometric profiles. |
| first_indexed | 2024-03-09T11:33:25Z |
| format | Article |
| id | doaj.art-4b1806e405a842cea75e89e98ae9269d |
| institution | Directory Open Access Journal |
| issn | 2079-4991 |
| language | English |
| last_indexed | 2024-03-09T11:33:25Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Nanomaterials |
| spelling | doaj.art-4b1806e405a842cea75e89e98ae9269d2023-11-30T23:46:08ZengMDPI AGNanomaterials2079-49912022-04-01127121510.3390/nano12071215Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual CooperationSilvana Alfei0Guendalina Zuccari1Debora Caviglia2Chiara Brullo3Department of Pharmacy, University of Genoa, Viale Cembrano, 16148 Genoa, ItalyDepartment of Pharmacy, University of Genoa, Viale Cembrano, 16148 Genoa, ItalyDepartment of Surgical Sciences and Integrated Diagnostics (DISC), University of Genoa, Viale Benedetto XV, 6, I-16132 Genova, ItalyDepartment of Pharmacy, University of Genoa, Viale Cembrano, 16148 Genoa, ItalyA pyrazole derivative (CB1) was previously evaluated in vivo for various pharmacological activities (with the exception of antimicrobial effects), using DMSO as the administrative medium, mainly due to its water insolubility. Considering the global necessity for new antimicrobial agents, CB1 attracted our attention as a candidate to meet this need, mainly because the secondary amine group in its structure would make it possible to obtain its hydrochloride salt (CB1H), thus effortlessly solving its water-solubility drawbacks. In preliminary microbiologic investigations on Gram-negative and Gram-positive bacteria, CB1H displayed weak antibacterial effects on MDR isolates of Gram-positive species, nonetheless better than those displayed by the commonly-used available antibiotics. Therefore, aiming at improving such activity and extending the antibacterial spectrum of CB1H to Gram-negative pathogens, in this first work CB1 was strategically formulated in nanoparticles using a cationic copolymer (P7) previously developed by us, possessing potent broad-spectrum bactericidal activity. Using the nanoprecipitation method, CB1H-loaded polymer nanoparticles (CB1H-P7 NPs) were obtained, which were analyzed by attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopy to confirm the successful loading. Additionally, CB1H-P7 NPs were fully characterized in terms of morphology, size, polydispersity indices, surface charge, DL%, and EE%, as well as release and potentiometric profiles.https://www.mdpi.com/2079-4991/12/7/1215polystyrene-based cationic copolymer (P7)physical entrapment1-(3,5-diphenyl-1H-pyrazol-1-yl)-3-(isopropyl amino) propan-2-ol) hydrochloride salt (CB1H)water-soluble CB1H-P7 NPsspherical morphologytriphasic release profile |
| spellingShingle | Silvana Alfei Guendalina Zuccari Debora Caviglia Chiara Brullo Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual Cooperation Nanomaterials polystyrene-based cationic copolymer (P7) physical entrapment 1-(3,5-diphenyl-1H-pyrazol-1-yl)-3-(isopropyl amino) propan-2-ol) hydrochloride salt (CB1H) water-soluble CB1H-P7 NPs spherical morphology triphasic release profile |
| title | Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual Cooperation |
| title_full | Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual Cooperation |
| title_fullStr | Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual Cooperation |
| title_full_unstemmed | Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual Cooperation |
| title_short | Synthesis and Characterization of Pyrazole-Enriched Cationic Nanoparticles as New Promising Antibacterial Agent by Mutual Cooperation |
| title_sort | synthesis and characterization of pyrazole enriched cationic nanoparticles as new promising antibacterial agent by mutual cooperation |
| topic | polystyrene-based cationic copolymer (P7) physical entrapment 1-(3,5-diphenyl-1H-pyrazol-1-yl)-3-(isopropyl amino) propan-2-ol) hydrochloride salt (CB1H) water-soluble CB1H-P7 NPs spherical morphology triphasic release profile |
| url | https://www.mdpi.com/2079-4991/12/7/1215 |
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