Artículos de revistas
Budesonide-hydroxypropyl-beta-cyclodextrin Inclusion Complex In Binary Poloxamer 407/403 System For Ulcerative Colitis Treatment: A Physico-chemical Study From Micelles To Hydrogels
Registro en:
Budesonide-hydroxypropyl-beta-cyclodextrin Inclusion Complex In Binary Poloxamer 407/403 System For Ulcerative Colitis Treatment: A Physico-chemical Study From Micelles To Hydrogels. Elsevier Science Bv, v. 138, p. 138-147 FEB-2016.
0927-7765
WOS:000368205100017
10.1016/j.colsurfb.2015.11.048
Autor
Santos Akkari
Alessandra Cristina; Ramos Campos
Estefania Vangelie; Keppler
Artur Franz; Fraceto
Leonardo Fernandes; de Paula
Eneida; Tofoli
Giovana Radomille; de Araujo
Daniele Ribeiro
Institución
Resumen
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) 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. 138
138 147 Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) FAPESP [FAPESP 2014/26200-9, 2014/14457-5] CNPq [CNPq 487619/2012-9, 309612/2013-6]