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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

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

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Autor(es):
Lazaro, Carolina Martins [1] ; de Oliveira, Carolina C. [1] ; Gambero, Alessandra [2] ; Rocha, Thalita [1] ; Saia Cereda, Cintia Maria [3] ; de Araujo, Daniele Ribeiro [4] ; Tofoli, Giovana Radomille [3]
Número total de Autores: 7
Afiliação do(s) autor(es):
[1] Univ Sao Francisco, Av Sao Francisco de Assis 218, BR-12916900 Braganca Paulista, SP - Brazil
[2] Univ Estadual Campinas, Av Alexandre Cazelatto 999, BR-13140000 Paulinia, SP - Brazil
[3] Fac Sao Leopoldo Mand, Inst Pesquisa Sao Leopoldo Mand, Rua Jose Rocha Junqueira 13, BR-1304575 Campinas, SP - Brazil
[4] Univ Fed ABC, Av Estados 5001, Bl A, Torre 3, Lab 503-3, BR-09210170 Santo Andre, SP - Brazil
Número total de Afiliações: 4
Tipo de documento: Artigo Científico
Fonte: Digestive Diseases and Sciences; v. 65, n. 11, p. 3297-3304, NOV 2020.
Citações Web of Science: 4
Resumo

Background New formulations for topical treatment of ulcerative colitis with budesonide inclusion complex (BUDHP-beta-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-BUD(HP-beta-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-beta-CD + PL407 (18%); BUD 2: BUDHP-beta-CD + PL407 (20%); BUD 3: BUDHP-beta-CD + PL407 (18%) + PL403 (2%); BUD 4: plain BUD; BUD 5: BUDHP-beta-CD; C1: HP-beta-CD + PL407 (18%); C2: HP-beta-CD + PL407 (20%); C3: HP-beta-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-alpha, IL-1 beta, IL-10 and endogenous glucocorticoids were obtained using ELISA. Results BUD(HP-beta-CD)poloxamer formulations had similar MPO activity when compared with the negative control group. All formulations presented lower MPO activity than BUD(HP-beta-CD)and plain BUD (p < 0.001). BUD 2 produced lower microscopic score values than plain BUD and BUDHP-beta-CD(p < 0.01). All formulations with BUD(HP-beta-CD)poloxamers reduced TNF-alpha levels (p < 0.05). Conclusion Novel budesonide inclusion complex formulations improved microscopic damage and reduced colonic MPO activity and TNF-alpha levels. (AU)

Processo FAPESP: 14/26200-9 - Sistemas híbridos nanoestruturados para liberação modificada de fármacos antiinflamatórios: desenvolvimento e avaliação farmacológica
Beneficiário:Daniele Ribeiro de Araujo
Modalidade de apoio: Auxílio à Pesquisa - Regular