New mesalamine polymeric conjugate for controlled release: preparation, characterization and biodistribution study

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dc.creatorAina Liz Alves Cesar
dc.creatorFernanda Alves Abrantes
dc.creatorLuana Farah
dc.creatorRachel Oliveira Castilho
dc.creatorValbert Nascimento Cardoso
dc.creatorSimone Odília Antunes Fernandes
dc.creatorIvana Duval de Araújo
dc.creatorAndré Augusto Gomes Faraco
dc.date.accessioned2022-05-09T20:06:45Z
dc.date.accessioned2025-09-09T01:24:42Z
dc.date.available2022-05-09T20:06:45Z
dc.date.issued2018-01-01
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.identifier.doi10.1016/j.ejps.2017.09.037
dc.identifier.issn0928-0987
dc.identifier.urihttps://hdl.handle.net/1843/41489
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofEuropean Journal of Pharmaceutical Sciences
dc.rightsAcesso Restrito
dc.subjectMesalazina
dc.subjectCintilografia
dc.subjectSistema de liberação controlada
dc.subject.otherTechnetium-99m
dc.subject.otherScintigraphy
dc.subject.otherChondroitin sulfate
dc.subject.other5-Aminosalicylic acid
dc.subject.otherControlled release system
dc.titleNew mesalamine polymeric conjugate for controlled release: preparation, characterization and biodistribution study
dc.typeArtigo de periódico
local.citation.epage64
local.citation.spage57
local.citation.volume111
local.description.resumoMesalamine (5-ASA) consists of the first-line therapy for the treatment of ulcerative colitis; however, it has low bioavailability, can cause several systemic adverse events, and has low treatment adherence due to the inconvenient dosing scheme. In this work, a new drug delivery system consisting of chondroitin sulfate linked to 5-ASA was synthesized using a carbodiimide as conjugating agent. The system was characterized by spectroscopic techniques (UV, ATR-FTIR, XRD, and NMR 1H) and thermal analysis (TG/DTG and DSC), suggesting the conjugation between the drug and the polymer. The in vitro release and the corresponding kinetics were also evaluated, revealing that approximately 40% of the drug linked was released at pH 9 for up to 50 h, following Higuchi's model. The conjugate did not show cytotoxicity for the human monocytic cell line at the doses tested, and an in vivo biodistribution study showed that the conjugate remained in the lower GIT for up to 8 h with no uptake in the upper GIT. These data corroborate with the radiation found per segment of GIT and in blood. For this last test the conjugate was radiolabeled with Technetium-99m to allow the scintigraphy evaluation and radiation quantification. In conclusion, the polymeric conjugate was successfully synthesized and demonstrated a mucoadhesiveness on the colon as desired, thus supporting its potential use in the treatment of ulcerative colitis.
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.departmentMED - DEPARTAMENTO DE CIRURGIA
local.publisher.initialsUFMG
local.url.externahttps://www.sciencedirect.com/science/article/pii/S0928098717305274?via%3Dihub

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