Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders
Genistein has been reported to have antioxidant and neuroprotective activity. Despite encouraging in vitro and in vivo results, several disadvantages such as poor water solubility, rapid metabolism, and low oral bioavailability limit the clinical application of genistein. The aim of this study was t...
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| Format: | Article |
| Language: | English |
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MDPI AG
2018-12-01
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| Series: | Pharmaceutics |
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| Online Access: | http://www.mdpi.com/1999-4923/11/1/8 |
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| author | Giovanna Rassu Elena Piera Porcu Silvia Fancello Antonella Obinu Nina Senes Grazia Galleri Rossana Migheli Elisabetta Gavini Paolo Giunchedi |
| author_facet | Giovanna Rassu Elena Piera Porcu Silvia Fancello Antonella Obinu Nina Senes Grazia Galleri Rossana Migheli Elisabetta Gavini Paolo Giunchedi |
| author_sort | Giovanna Rassu |
| collection | DOAJ |
| description | Genistein has been reported to have antioxidant and neuroprotective activity. Despite encouraging in vitro and in vivo results, several disadvantages such as poor water solubility, rapid metabolism, and low oral bioavailability limit the clinical application of genistein. The aim of this study was to design and characterize genistein-loaded chitosan nanoparticles for intranasal drug delivery, prepared by the ionic gelation technique by using sodium hexametaphosphate. Nanoparticles were characterized in vitro and their cytotoxicity was tested on PC12 cells. Genistein-loaded nanoparticles were prepared, and sodium hexametaphosphate was used as a valid alternative to well-known cross-linkers. Nanoparticle characteristics as well as their physical stability were affected by formulation composition and manufacturing. Small (mean diameters of 200–300 nm) and homogeneous nanoparticles were obtained and were able to improve genistein penetration through the nasal mucosa as compared to pure genistein. Nanoparticle dispersions showed a pH consistent with the nasal fluid and preserved PC12 cell vitality. |
| first_indexed | 2024-04-14T02:21:16Z |
| format | Article |
| id | doaj.art-ae9f4715805b4ab8adf2eaaf62c78cc5 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-14T02:21:16Z |
| publishDate | 2018-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-ae9f4715805b4ab8adf2eaaf62c78cc52022-12-22T02:18:01ZengMDPI AGPharmaceutics1999-49232018-12-01111810.3390/pharmaceutics11010008pharmaceutics11010008Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative DisordersGiovanna Rassu0Elena Piera Porcu1Silvia Fancello2Antonella Obinu3Nina Senes4Grazia Galleri5Rossana Migheli6Elisabetta Gavini7Paolo Giunchedi8Department of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, ItalyDepartment of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, ItalyDepartment of Clinical and Experimental Medicine, University of Sassari, viale San Pietro 43/b, 07100 Sassari, ItalyExperimental Medicine, Department of Clinical-Surgical, Diagnostic and Paediatric Sciences, University of Pavia, 27100 Pavia, ItalyDepartment of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, ItalyDepartment of Clinical and Experimental Medicine, University of Sassari, viale San Pietro 43/b, 07100 Sassari, ItalyDepartment of Clinical and Experimental Medicine, University of Sassari, viale San Pietro 43/b, 07100 Sassari, ItalyDepartment of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, ItalyDepartment of Chemistry and Pharmacy, University of Sassari, via Muroni 23/a, 07100 Sassari, ItalyGenistein has been reported to have antioxidant and neuroprotective activity. Despite encouraging in vitro and in vivo results, several disadvantages such as poor water solubility, rapid metabolism, and low oral bioavailability limit the clinical application of genistein. The aim of this study was to design and characterize genistein-loaded chitosan nanoparticles for intranasal drug delivery, prepared by the ionic gelation technique by using sodium hexametaphosphate. Nanoparticles were characterized in vitro and their cytotoxicity was tested on PC12 cells. Genistein-loaded nanoparticles were prepared, and sodium hexametaphosphate was used as a valid alternative to well-known cross-linkers. Nanoparticle characteristics as well as their physical stability were affected by formulation composition and manufacturing. Small (mean diameters of 200–300 nm) and homogeneous nanoparticles were obtained and were able to improve genistein penetration through the nasal mucosa as compared to pure genistein. Nanoparticle dispersions showed a pH consistent with the nasal fluid and preserved PC12 cell vitality.http://www.mdpi.com/1999-4923/11/1/8chitosangenisteinsodium hexametaphosphatenose-to-brainintranasal deliveryneurodegenerative diseasenanoparticles |
| spellingShingle | Giovanna Rassu Elena Piera Porcu Silvia Fancello Antonella Obinu Nina Senes Grazia Galleri Rossana Migheli Elisabetta Gavini Paolo Giunchedi Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders Pharmaceutics chitosan genistein sodium hexametaphosphate nose-to-brain intranasal delivery neurodegenerative disease nanoparticles |
| title | Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders |
| title_full | Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders |
| title_fullStr | Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders |
| title_full_unstemmed | Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders |
| title_short | Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders |
| title_sort | intranasal delivery of genistein loaded nanoparticles as a potential preventive system against neurodegenerative disorders |
| topic | chitosan genistein sodium hexametaphosphate nose-to-brain intranasal delivery neurodegenerative disease nanoparticles |
| url | http://www.mdpi.com/1999-4923/11/1/8 |
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