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Type: Artigo
Title: Evaluation of budesonide-hydroxypropyl-β-cyclodextrin inclusion complex in thermoreversible gels for ulcerative colitis
Author: Lázaro, C.M.
de Oliveira, C.C.
Gambero, A.
Rocha, T.
Cereda, C.M.S.
de Araújo, D.R.
Tofoli, G.R.
Abstract: Background: New formulations for topical treatment of ulcerative colitis with budesonide inclusion complex (BUDHP-β-CD) and poloxamers (PL) were developed for future clinical use. Aims: This study evaluated the efficacy of such novel formulations in a rat model of colitis. Methods: The PL-BUDHP-β-CD systems were prepared by direct dispersion of the complex (BUD concentration 0.5 mg mL−1) in solutions with PL407 or PL403. Male Wistar rats underwent TNBS-induced colitis and were treated for 5 days by a rectal route, as follows: BUD 1: BUDHP-β-CD + PL407 (18%); BUD 2: BUDHP-β-CD + PL407 (20%); BUD 3: BUDHP-β-CD + PL407 (18%) + PL403 (2%); BUD 4: plain BUD; BUD 5: BUDHP-β-CD; C1: HP-β-CD + PL407 (18%); C2: HP-β-CD + PL407 (20%); C3: HP-β-CD + PL407 (18%) + PL403 (2%); C4: saline. A negative control group without colitis was also used. Colitis was assessed via myeloperoxidase (MPO) activity, and macroscopic and microscopic damage score in colon tissues. Protein levels of TNF-α, IL-1β, IL-10 and endogenous glucocorticoids were obtained using ELISA. Results: BUDHP-β-CD poloxamer formulations had similar MPO activity when compared with the negative control group. All formulations presented lower MPO activity than BUDHP-β-CD and plain BUD (p < 0.001). BUD 2 produced lower microscopic score values than plain BUD and BUDHP-β-CD (p < 0.01). All formulations with BUDHP-β-CD poloxamers reduced TNF-α levels (p < 0.05). Conclusion: Novel budesonide inclusion complex formulations improved microscopic damage and reduced colonic MPO activity and TNF-α levels.
Subject: Colite ulcerativa
Country: Estados Unidos
Editor: Springer
Rights: Fechado
Identifier DOI: 10.1007/s10620-020-06075-y
Date Issue: 2020
Appears in Collections:CPQBA - Artigos e Outros Documentos

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