Long‐Acting Microparticle Formulation of Griseofulvin for Ocular Neovascularization Therapy
Abstract: Neovascular age‐related macular degeneration (nAMD) is a leading cause of vision loss in older adults. nAMD is treated with biologics targeting vascular endothelial growth factor; however, many patients do not respond to the current therapy. Here, a small molecule drug, griseofulvin (GRF), is used due to its inhibitory effect on ferrochelatase, an enzyme important for choroidal neovascularization (CNV). For local and sustained delivery to the eyes, GRF is encapsulated in microparticles based on poly (lactide‐co‐glycolide) (PLGA), a biodegradable polymer with a track record in long‐acting formulations. The GRF‐loaded PLGA microparticles (GRF MPs) are designed for intravitreal application, considering constraints in size, drug loading content, and drug release kinetics. Magnesium hydroxide is co‐encapsulated to enable sustained GRF release over >30 days in phosphate‐buffered saline with Tween 80. Incubated in cell culture medium over 30 days, the GRF MPs and the released drug show antiangiogenic effects in retinal endothelial cells. A single intravitreal injection of MPs containing 0.18 µg GRF releases the drug over 6 weeks in vivo to inhibit the progression of laser‐induced CNV in mice with no abnormality in the fundus and retina. Intravitreally administered GRF MPs prove effective in preventing CNV, providing proof‐of‐concept toward a novel, cost‐effective nAMD therapy.
- Standort
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Deutsche Nationalbibliothek Frankfurt am Main
- Umfang
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Online-Ressource
- Sprache
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Englisch
- Erschienen in
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Long‐Acting Microparticle Formulation of Griseofulvin for Ocular Neovascularization Therapy ; day:08 ; month:11 ; year:2023 ; extent:14
Small ; (08.11.2023) (gesamt 14)
- Urheber
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Chobisa, Dhawal
Muniyandi, Anbukkarasi
Sishtla, Kamakshi
Corson, Timothy W.
Yeo, Yoon
- DOI
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10.1002/smll.202306479
- URN
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urn:nbn:de:101:1-2023110914172949013123
- Rechteinformation
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
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14.08.2025, 10:48 MESZ
Datenpartner
Deutsche Nationalbibliothek. Bei Fragen zum Objekt wenden Sie sich bitte an den Datenpartner.
Beteiligte
- Chobisa, Dhawal
- Muniyandi, Anbukkarasi
- Sishtla, Kamakshi
- Corson, Timothy W.
- Yeo, Yoon
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