Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal Neovascularization
The wet type of age-related macular degeneration (AMD) accompanies the subfoveal choroidal neovascularization (CNV) caused by the abnormal extension or remodeling of blood vessels to the macula and retinal pigment epithelium (RPE). Vascular endothelial growth factor (VEGF) is known to play a crucial...
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2021-09-01
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| Online Access: | https://www.mdpi.com/1999-4923/13/10/1548 |
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| author | E Seul Kim Min Sang Lee Hayoung Jeong Su Yeon Lim Doha Kim Dahwun Kim Jaeback Jung Siyan Lyu Hee Joo Cho Dong Min Kim Wonhee Suh Ji Hoon Jeong |
| author_facet | E Seul Kim Min Sang Lee Hayoung Jeong Su Yeon Lim Doha Kim Dahwun Kim Jaeback Jung Siyan Lyu Hee Joo Cho Dong Min Kim Wonhee Suh Ji Hoon Jeong |
| author_sort | E Seul Kim |
| collection | DOAJ |
| description | The wet type of age-related macular degeneration (AMD) accompanies the subfoveal choroidal neovascularization (CNV) caused by the abnormal extension or remodeling of blood vessels to the macula and retinal pigment epithelium (RPE). Vascular endothelial growth factor (VEGF) is known to play a crucial role in the pathogenesis of the disease. In this study, we tried to repurpose an investigational anticancer drug, rivoceranib, which is a selective inhibitor of VEGF receptor-2 (VEGFR2), and evaluate the therapeutic potential of the drug for the treatment of wet-type AMD in a laser-induced CNV mouse model using microsphere-based sustained drug release formulations. The PLGA-based rivoceranib microsphere can carry out a sustained delivery of rivoceranib for 50 days. When administered intravitreally, the sustained microsphere formulation of rivoceranib effectively inhibited the formation of subfoveal neovascular lesions in mice. |
| first_indexed | 2024-03-10T06:17:33Z |
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| id | doaj.art-bc26622f79db4873bc5483dfec62eb0c |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T06:17:33Z |
| publishDate | 2021-09-01 |
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| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-bc26622f79db4873bc5483dfec62eb0c2023-11-22T19:37:20ZengMDPI AGPharmaceutics1999-49232021-09-011310154810.3390/pharmaceutics13101548Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal NeovascularizationE Seul Kim0Min Sang Lee1Hayoung Jeong2Su Yeon Lim3Doha Kim4Dahwun Kim5Jaeback Jung6Siyan Lyu7Hee Joo Cho8Dong Min Kim9Wonhee Suh10Ji Hoon Jeong11School of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaDepartment of Global Innovative Drug, Graduate School of Chung-Ang University, Seoul 06974, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaDepartment of Global Innovative Drug, Graduate School of Chung-Ang University, Seoul 06974, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaDepartment of Global Innovative Drug, Graduate School of Chung-Ang University, Seoul 06974, KoreaSchool of Pharmacy, Sungkyunkwan University, Suwon 16419, KoreaThe wet type of age-related macular degeneration (AMD) accompanies the subfoveal choroidal neovascularization (CNV) caused by the abnormal extension or remodeling of blood vessels to the macula and retinal pigment epithelium (RPE). Vascular endothelial growth factor (VEGF) is known to play a crucial role in the pathogenesis of the disease. In this study, we tried to repurpose an investigational anticancer drug, rivoceranib, which is a selective inhibitor of VEGF receptor-2 (VEGFR2), and evaluate the therapeutic potential of the drug for the treatment of wet-type AMD in a laser-induced CNV mouse model using microsphere-based sustained drug release formulations. The PLGA-based rivoceranib microsphere can carry out a sustained delivery of rivoceranib for 50 days. When administered intravitreally, the sustained microsphere formulation of rivoceranib effectively inhibited the formation of subfoveal neovascular lesions in mice.https://www.mdpi.com/1999-4923/13/10/1548rivoceranibdrug repositioningmicrospheresubfoveal choroidal neovascularizationmacular degeneration |
| spellingShingle | E Seul Kim Min Sang Lee Hayoung Jeong Su Yeon Lim Doha Kim Dahwun Kim Jaeback Jung Siyan Lyu Hee Joo Cho Dong Min Kim Wonhee Suh Ji Hoon Jeong Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal Neovascularization Pharmaceutics rivoceranib drug repositioning microsphere subfoveal choroidal neovascularization macular degeneration |
| title | Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal Neovascularization |
| title_full | Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal Neovascularization |
| title_fullStr | Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal Neovascularization |
| title_full_unstemmed | Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal Neovascularization |
| title_short | Sustained-Release Microspheres of Rivoceranib for the Treatment of Subfoveal Choroidal Neovascularization |
| title_sort | sustained release microspheres of rivoceranib for the treatment of subfoveal choroidal neovascularization |
| topic | rivoceranib drug repositioning microsphere subfoveal choroidal neovascularization macular degeneration |
| url | https://www.mdpi.com/1999-4923/13/10/1548 |
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