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Evaluation of Budesonide-Hydroxypropyl-β-Cyclodextrin Inclusion Complex in Thermoreversible Gels for Ulcerative Colitis. | LitMetric

Evaluation of Budesonide-Hydroxypropyl-β-Cyclodextrin Inclusion Complex in Thermoreversible Gels for Ulcerative Colitis.

Dig Dis Sci

Faculdade São Leopoldo Mandic, Instituto de Pesquisa São Leopoldo Mandic, Rua José Rocha Junqueira 13, Campinas, São Paulo, 13045-75, Brazil.

Published: November 2020

AI Article Synopsis

Article Abstract

Background: New formulations for topical treatment of ulcerative colitis with budesonide inclusion complex (BUD) 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-BUD systems were prepared by direct dispersion of the complex (BUD concentration 0.5 mg mL) 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: BUD + PL407 (18%); BUD 2: BUD + PL407 (20%); BUD 3: BUD + PL407 (18%) + PL403 (2%); BUD 4: plain BUD; BUD 5: BUD; 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: BUD poloxamer formulations had similar MPO activity when compared with the negative control group. All formulations presented lower MPO activity than BUD and plain BUD (p < 0.001). BUD 2 produced lower microscopic score values than plain BUD and BUD (p < 0.01). All formulations with BUD 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.

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Source
http://dx.doi.org/10.1007/s10620-020-06075-yDOI Listing

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