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| Format: | Recurso digital |
| Idioma: | anglès |
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Zenodo
2024
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| Accés en línia: | https://doi.org/10.3390/ph16101446 |
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| author | Rodrigues-Braz, Daniela Linxin, Zhu Clarin, Jean-Pierre Gélizé, Emmanuelle Chatagnon, Xavier Benzine, Youcef Rampignon, Philippe Thouvenin, Agathe Bourges, Jean-Louis Behar-Cohen, Francine Zhao, Min |
| author_facet | Rodrigues-Braz, Daniela Linxin, Zhu Clarin, Jean-Pierre Gélizé, Emmanuelle Chatagnon, Xavier Benzine, Youcef Rampignon, Philippe Thouvenin, Agathe Bourges, Jean-Louis Behar-Cohen, Francine Zhao, Min |
| contents | <p>Abnormal corneal wound healing can compromise corneal transparency and lead to visual impairment. Mineralocorticoid receptor antagonists (MRA) are promising candidates to promote corneal remodeling with anti-inflammatory properties and lack gluococorticoids-associated side effects. In this preclinical study, a new polymer-free hydroxypropyl-gamma-cyclodextrin-based eyedrop containing 0.1% spironolactone (SPL), a potent but non-water-soluble MRA, was investigated for its ocular surface tolerance and efficacy in a rat model of corneal wound healing. SPL eyedrops were stable for up to 9 months at 4 ◦C. The formulation was well-tolerated since no morphological changes or inflammatory reactions were observed in the rat cornea after multiple daily instillations over 7 days. SPL eyedrops accelerated rat corneal wound healing, reduced corneal edema and inflammation, enhanced epithelial integrity, and improved nerve regeneration, suggesting restoration of corneal homeostasis, while potassium canrenoate, an active and soluble metabolite of SPL, had no effect. SPL eyedrops could benefit patients with impaired corneal wound healing, including that secondary to glucocorticoid therapy. Repurposing known drugs with known excipients will expedite translation to the clinic.</p> |
| format | Recurso digital |
| id | zenodo_https___doi_org_10_3390_ph16101446 |
| institution | Zenodo |
| language | eng |
| publishDate | 2024 |
| publisher | Zenodo |
| record_format | zenodo |
| spellingShingle | Spironolactone Eyedrop Favors Restoration of Corneal Integrity after Wound Healing in the Rat Rodrigues-Braz, Daniela Linxin, Zhu Clarin, Jean-Pierre Gélizé, Emmanuelle Chatagnon, Xavier Benzine, Youcef Rampignon, Philippe Thouvenin, Agathe Bourges, Jean-Louis Behar-Cohen, Francine Zhao, Min spironolactone drug development topical administration eyedrop corneal wound healing ocular surface cornea <p>Abnormal corneal wound healing can compromise corneal transparency and lead to visual impairment. Mineralocorticoid receptor antagonists (MRA) are promising candidates to promote corneal remodeling with anti-inflammatory properties and lack gluococorticoids-associated side effects. In this preclinical study, a new polymer-free hydroxypropyl-gamma-cyclodextrin-based eyedrop containing 0.1% spironolactone (SPL), a potent but non-water-soluble MRA, was investigated for its ocular surface tolerance and efficacy in a rat model of corneal wound healing. SPL eyedrops were stable for up to 9 months at 4 ◦C. The formulation was well-tolerated since no morphological changes or inflammatory reactions were observed in the rat cornea after multiple daily instillations over 7 days. SPL eyedrops accelerated rat corneal wound healing, reduced corneal edema and inflammation, enhanced epithelial integrity, and improved nerve regeneration, suggesting restoration of corneal homeostasis, while potassium canrenoate, an active and soluble metabolite of SPL, had no effect. SPL eyedrops could benefit patients with impaired corneal wound healing, including that secondary to glucocorticoid therapy. Repurposing known drugs with known excipients will expedite translation to the clinic.</p> |
| title | Spironolactone Eyedrop Favors Restoration of Corneal Integrity after Wound Healing in the Rat |
| topic | spironolactone drug development topical administration eyedrop corneal wound healing ocular surface cornea |
| url | https://doi.org/10.3390/ph16101446 |