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http://hdl.handle.net/1843/40841| Type: | Artigo de Periódico |
| Title: | Chitosan/hydroxyethyl cellulose inserts for sustained-release of dorzolamide for glaucoma treatment: in vitro and in vivo evaluation |
| Authors: | Juçara Ribeiro França Giselle Foureaux Leonardo Lima Fuscaldi Tatiana Gomes Ribeiro Rachel Oliveira Castilho Maria Irene Yoshida Valbert Nascimento Cardoso Simone Odília Antunes Fernandes Sebastião Cronemberger José Carlos Nogueira Anderson José Ferreira André Augusto Gomes Faraco |
| Abstract: | Eye drops containing hydrophilic drugs are commonly used to reduce intraocular pressure (IOP) in glaucoma patients, but compliance to the treatement is commonly reduced by frequent dosing and eventual systemic side effects. Sustained-release drug delivery systems, such as ocular inserts, can reduce dosing, limit systemic exposure, reduce side effects, and, then, improve patient adherence to therapy. Here, we developed and evaluated chitosan/hydroxyethyl cellulose-based ocular inserts for sustained release of dorzolamide, a hydrophilic drug. Dorzolamide inserts (DI) were produced by solvent/casting method and characterized by various physicochemical techniques. Pharmacokinetics studies were performed using scintigraphic images and ex vivo biodistribution. The effectiveness of inserts was tested in glaucomatous rats. Characterization studies showed that the drug strongly interacted with the polymeric matrix, but in vitro results showed that DI took only 3 h to release 75% of dorzolamide entraped. However, scintigraphic images and ex vivo biodistribution studies revealed that more than 50% of 99mTc-dorzolamide remained in the eye after 18 h of DI administration, while only about 30% of the drug remained in the eye after drops instilation. DI exerted significant hypotensive effect for two weeks, after single administration, while IOP values remained high in placebo and untreated groups. Eye drops were effective only during the treatment period. Only DI treatment prevented retinal ganglion cells death. Altogether, these findings evidenced the potential application of polymeric-based inserts for sustained release of dorzolamide in glaucoma management. |
| Subject: | Glaucoma Quitosana Hidroxietilcelulose Dorzolamida |
| language: | eng |
| metadata.dc.publisher.country: | Brasil |
| Publisher: | Universidade Federal de Minas Gerais |
| Publisher Initials: | UFMG |
| metadata.dc.publisher.department: | FAR - DEPARTAMENTO DE ALIMENTOS FAR - DEPARTAMENTO DE ANÁLISES CLÍNICAS E TOXICOLÓGICAS FAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS ICB - DEPARTAMENTO DE MORFOLOGIA ICX - DEPARTAMENTO DE QUÍMICA MED - DEPARTAMENTO DE OFTALMOLOGIA E OTORRINOLARINGOLOGIA |
| Rights: | Acesso Aberto |
| metadata.dc.identifier.doi: | 10.1016/j.ijpharm.2019.118662 |
| URI: | http://hdl.handle.net/1843/40841 |
| Issue Date: | Oct-2019 |
| metadata.dc.url.externa: | https://www.sciencedirect.com/science/article/pii/S0378517319307070?via%3Dihub |
| metadata.dc.relation.ispartof: | International Journal of Pharmaceutics |
| Appears in Collections: | Artigo de Periódico |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| Chitosanhydroxyethyl cellulose inserts for sustained-release of dorzolamide for glaucoma treatment In vitro and in vivo evaluation.pdf | 2.06 MB | Adobe PDF | View/Open |
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