Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterization
Lutein and zeaxanthin, prominent carotenoids with antioxidant properties, contribute notably to maintaining of ocular health. These substances reduce the harmful effect of oxidative stress and blue light and ensure the vision quality. Carotenoids-rich dietary could have ophthalmic benefits, such as...
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| Format: | Article |
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Elsevier
2025-03-01
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| Series: | Carbohydrate Polymer Technologies and Applications |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S266689392500057X |
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| author | Réka Angi Attila János Kalóczkai Anna Kovács András Marton Vivien Bárdos Péter Dormán Gábor Katona Attila Agócs Anita Csorba Zoltán Zs. Nagy Anna Vincze György T. Balogh |
| author_facet | Réka Angi Attila János Kalóczkai Anna Kovács András Marton Vivien Bárdos Péter Dormán Gábor Katona Attila Agócs Anita Csorba Zoltán Zs. Nagy Anna Vincze György T. Balogh |
| author_sort | Réka Angi |
| collection | DOAJ |
| description | Lutein and zeaxanthin, prominent carotenoids with antioxidant properties, contribute notably to maintaining of ocular health. These substances reduce the harmful effect of oxidative stress and blue light and ensure the vision quality. Carotenoids-rich dietary could have ophthalmic benefits, such as enhanced contrast perception and reduced eye fatigue, while also show potential in mitigating the risk of age-related macular degeneration (AMD). Nonetheless, ocular administration of carotenoids could enhance the local ophthalmic bioavailability of these compounds. The aim of this study was to investigate ophthalmic applicability of lutein (LutD) and zeaxanthin disuccinates (ZeaD) in aqueous solutions applying cyclodextrins to improve their solubility and permeability. Among the tested cyclodextrins, randomly methylated beta-cyclodextrin (RAMEB) was identified as the most effective solubilizing agent, achieving solubility values of 572±55 μM and 1470±103 μM for LutD and ZeaD, respectively. In vitro corneal-PAMPA and ex vivo porcine eye models demonstrated that RAMEB-based formulations significantly improved the permeability of both carotenoid derivatives by increasing their solubility (corneal concentration at 15 mins), markedly surpassing those of the reference suspensions. The findings suggest that RAMEB may be essential for developing carotenoid-based aqueous eye drops, leveraging its antioxidant properties to improve ocular health and ameliorate various degenerative eye conditions. |
| format | Article |
| id | doaj-art-2522416c78a442fd93116ee78b7cd970 |
| institution | DOAJ |
| issn | 2666-8939 |
| language | English |
| publishDate | 2025-03-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Carbohydrate Polymer Technologies and Applications |
| spelling | doaj-art-2522416c78a442fd93116ee78b7cd9702025-08-20T02:52:21ZengElsevierCarbohydrate Polymer Technologies and Applications2666-89392025-03-01910071810.1016/j.carpta.2025.100718Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterizationRéka Angi0Attila János Kalóczkai1Anna Kovács2András Marton3Vivien Bárdos4Péter Dormán5Gábor Katona6Attila Agócs7Anita Csorba8Zoltán Zs. Nagy9Anna Vincze10György T. Balogh11Department of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre u. 9., H-1092 Budapest, Hungary; Center for Pharmacology and Drug Research & Development, Semmelweis University, Üllői u. 26. H-1092 Budapest, HungaryDepartment of Chemical and Process Engineering, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem Quay 3., H-1111 Budapest, HungaryDepartment of Chemical and Process Engineering, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem Quay 3., H-1111 Budapest, HungaryDepartment of Chemical and Process Engineering, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem Quay 3., H-1111 Budapest, HungaryDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre u. 9., H-1092 Budapest, Hungary; Center for Pharmacology and Drug Research & Development, Semmelweis University, Üllői u. 26. H-1092 Budapest, HungaryCenter for Pharmacology and Drug Research & Development, Semmelweis University, Üllői u. 26. H-1092 Budapest, Hungary; Department of Ophthalmology, Semmelweis University, Maria Str. 39., H-1085 Budapest, HungaryInstitute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös utca 6., H-6720 Szeged, HungaryDepartment of Biochemistry and Medical Chemistry, Medical School, University of Pécs, Szigeti út 12, H-7624 Pécs, HungaryCenter for Pharmacology and Drug Research & Development, Semmelweis University, Üllői u. 26. H-1092 Budapest, Hungary; Department of Ophthalmology, Semmelweis University, Maria Str. 39., H-1085 Budapest, HungaryCenter for Pharmacology and Drug Research & Development, Semmelweis University, Üllői u. 26. H-1092 Budapest, Hungary; Department of Ophthalmology, Semmelweis University, Maria Str. 39., H-1085 Budapest, HungaryDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre u. 9., H-1092 Budapest, Hungary; Center for Pharmacology and Drug Research & Development, Semmelweis University, Üllői u. 26. H-1092 Budapest, Hungary; Corresponding authors.Department of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre u. 9., H-1092 Budapest, Hungary; Center for Pharmacology and Drug Research & Development, Semmelweis University, Üllői u. 26. H-1092 Budapest, Hungary; Department of Chemical and Process Engineering, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem Quay 3., H-1111 Budapest, Hungary; Corresponding authors.Lutein and zeaxanthin, prominent carotenoids with antioxidant properties, contribute notably to maintaining of ocular health. These substances reduce the harmful effect of oxidative stress and blue light and ensure the vision quality. Carotenoids-rich dietary could have ophthalmic benefits, such as enhanced contrast perception and reduced eye fatigue, while also show potential in mitigating the risk of age-related macular degeneration (AMD). Nonetheless, ocular administration of carotenoids could enhance the local ophthalmic bioavailability of these compounds. The aim of this study was to investigate ophthalmic applicability of lutein (LutD) and zeaxanthin disuccinates (ZeaD) in aqueous solutions applying cyclodextrins to improve their solubility and permeability. Among the tested cyclodextrins, randomly methylated beta-cyclodextrin (RAMEB) was identified as the most effective solubilizing agent, achieving solubility values of 572±55 μM and 1470±103 μM for LutD and ZeaD, respectively. In vitro corneal-PAMPA and ex vivo porcine eye models demonstrated that RAMEB-based formulations significantly improved the permeability of both carotenoid derivatives by increasing their solubility (corneal concentration at 15 mins), markedly surpassing those of the reference suspensions. The findings suggest that RAMEB may be essential for developing carotenoid-based aqueous eye drops, leveraging its antioxidant properties to improve ocular health and ameliorate various degenerative eye conditions.http://www.sciencedirect.com/science/article/pii/S266689392500057XLuteinZeaxanthinCyclodextrinsSolubilityCorneal permeabilityEx vivo |
| spellingShingle | Réka Angi Attila János Kalóczkai Anna Kovács András Marton Vivien Bárdos Péter Dormán Gábor Katona Attila Agócs Anita Csorba Zoltán Zs. Nagy Anna Vincze György T. Balogh Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterization Carbohydrate Polymer Technologies and Applications Lutein Zeaxanthin Cyclodextrins Solubility Corneal permeability Ex vivo |
| title | Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterization |
| title_full | Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterization |
| title_fullStr | Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterization |
| title_full_unstemmed | Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterization |
| title_short | Harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives: From development to ex vivo characterization |
| title_sort | harnessing cyclodextrins for enhanced ocular delivery of carotenoid derivatives from development to ex vivo characterization |
| topic | Lutein Zeaxanthin Cyclodextrins Solubility Corneal permeability Ex vivo |
| url | http://www.sciencedirect.com/science/article/pii/S266689392500057X |
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