Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect

Carregando...
Imagem de Miniatura

Data

2012-11-01

Autores

dos Santos, Jean Leandro [UNESP]
Moreira, Vanessa
Campos, Michel Leandro [UNESP]
Chelucci, Rafael Consolin [UNESP]
Barbieri, Karina Pereira [UNESP]
Maggio de Castro Souto, Pollyana Cristina
Matsubara, Marcio Hideki
Teixeira, Catarina
Bosquesi, Priscila Longhin [UNESP]
Peccinini, Rosangela Goncalves [UNESP]

Título da Revista

ISSN da Revista

Título de Volume

Editor

Mdpi Ag

Resumo

Long-term nonsteroidal anti-inflammatory drugs (NSAIDs) therapy has been associated with several adverse effects such as gastric ulceration and cardiovascular events. Among the molecular modifications strategies, the prodrug approach is a useful tool to discover new safe NSAIDs. The 1-(2,6-dichlorophenyl)indolin-2-one is a diclofenac prodrug which demonstrated relevant anti-inflammatory properties without gastro ulceration effect. In addition, the prodrug decreases PGE(2) levels, COX-2 expression and cellular influx into peritoneal cavity induced by carrageenan treatment. Preliminary pharmacokinetic studies have shown in vivo bioconversion of prodrug to diclofenac. This prodrug is a new nonulcerogenic NSAID useful to treat inflammatory events by long-term therapy.

Descrição

Palavras-chave

NSAIDs, anti-inflammatory, diclofenac, prodrugs, molecular modification, lactam, COX-inhibitor, bioconversion, chronic inflammation

Como citar

International Journal of Molecular Sciences. Basel: Mdpi Ag, v. 13, n. 11, p. 15305-15320, 2012.