Chitosan/hydroxyethyl cellulose inserts for sustained-release of dorzolamide for glaucoma treatment: in vitro and in vivo evaluation

dc.creatorJuçara Ribeiro França
dc.creatorGiselle Foureaux
dc.creatorLeonardo Lima Fuscaldi
dc.creatorTatiana Gomes Ribeiro
dc.creatorRachel Oliveira Castilho
dc.creatorMaria Irene Yoshida
dc.creatorValbert Nascimento Cardoso
dc.creatorSimone Odília Antunes Fernandes
dc.creatorSebastião Cronemberger
dc.creatorJosé Carlos Nogueira
dc.creatorAnderson José Ferreira
dc.creatorAndré Augusto Gomes Faraco
dc.date.accessioned2022-04-06T20:42:25Z
dc.date.accessioned2025-09-09T01:01:03Z
dc.date.available2022-04-06T20:42:25Z
dc.date.issued2019-10
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.format.mimetypepdf
dc.identifier.doi10.1016/j.ijpharm.2019.118662
dc.identifier.issn0378-5173
dc.identifier.urihttps://hdl.handle.net/1843/40841
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofInternational Journal of Pharmaceutics
dc.rightsAcesso Aberto
dc.subjectGlaucoma
dc.subjectQuitosana
dc.subjectHidroxietilcelulose
dc.subjectDorzolamida
dc.subject.otherSustained-release drug delivery systems
dc.subject.otherOcular inserts
dc.subject.otherHydroxyethyl cellulose
dc.subject.otherChitosan
dc.subject.otherGlaucoma
dc.subject.otherDorzolamide
dc.titleChitosan/hydroxyethyl cellulose inserts for sustained-release of dorzolamide for glaucoma treatment: in vitro and in vivo evaluation
dc.typeArtigo de periódico
local.citation.epage10
local.citation.spage1
local.citation.volume570
local.description.resumoEye 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.
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE ALIMENTOS
local.publisher.departmentFAR - DEPARTAMENTO DE ANÁLISES CLÍNICAS E TOXICOLÓGICAS
local.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS
local.publisher.departmentICB - DEPARTAMENTO DE MORFOLOGIA
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.departmentMED - DEPARTAMENTO DE OFTALMOLOGIA E OTORRINOLARINGOLOGIA
local.publisher.initialsUFMG
local.url.externahttps://www.sciencedirect.com/science/article/pii/S0378517319307070?via%3Dihub

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