Budesonide-hydroxypropyl-beta-cyclodextrin inclusion complex in binary poloxamer 407/403 system for ulcerative colitis treatment: A physico-chemical study from micelles to hydrogels
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Data
2016-02-01
Autores
Santos Akkari, Alessandra Cristina
Ramos Campos, Estefania Vangelie [UNESP]
Keppler, Artur Franz
Fraceto, Leonardo Fernandes [UNESP]
Paula, Eneida de
Tofoli, Giovana Radomille
Araujo, Daniele Ribeiro de
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Editor
Elsevier B.V.
Resumo
Budesonide (BUD) is a glucocorticoid widely used for the treatment of ulcerative colitis. In this work, we propose the study of the system BUD-HP-beta-CD inclusion complex incorporated into PL 407 and PL407-PL403 thermoreversible hydrogels, considering physico-chemical and pharmaceutical aspects. Complexation between BUD and HP-beta-CD was confirmed by phase solubility studies (1:1 stoichiometry, Kc = 8662.8 M-1), DSC, FTIR and microscopy analyzes. BUD solubility in simulated upper and lower colon fluids was improved in a dependence of HP-beta-CD and PL 407 or PL407-PL403 association. Micellar hydrodynamic diameter studies showed the interaction between HP-beta-CD and PL blocks, as well as the reorganization of the micellar system in the presence of BUD and its inclusion complex. Micellization temperature (T-m) was not shifted, but sol-gel phase transition studies showed that in the presence of BUD, HP-beta-CD or BUD:HP-beta-CD complex, the association PL407-PL403 favored the gel formation close to the physiological temperature. Physico-chemical and in vitro release assays studies revealed no competitive displacement of BUD from the HP-beta-CD cavity evoked by PL407 or PL407-PL403 addition. These findings point out the BUD-HP-beta-CD in PL-based hydrogels as strategies for future investigations on development of new pharmaceutical formulations for the treatment of ulcerative colitis. (C) 2015 Elsevier B.V. All rights reserved.
Descrição
Palavras-chave
Budesonide, Cyclodextrin, Poloxamer, Micelle, Hydrogel, Ulcerative colitis, Polyrotaxane
Como citar
Colloids And Surfaces B-biointerfaces. Amsterdam: Elsevier Science Bv, v. 138, p. 138-147, 2016.