Author(s): 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
Date: 2018
Persistent ID: http://hdl.handle.net/11449/165036
Origin: Oasisbr
Subject(s): Budesonide; Cyclodextrin; Poloxamer; Micelle; Hydrogel; Ulcerative colitis; Polyrotaxane
Made available in DSpace on 2018-11-27T07:08:26Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-02-01
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
Fundacao de Amparo Pesquisa do Estado de Sao Paulo
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.
Univ Fed Abc, Ctr Ciencias Nat & Humanas, BR-09210580 Santo Andre, SP, Brazil
State Univ Julio de Mesquita Filho, Dept Enviroment Engn, Sorocaba, SP, Brazil
Univ Estadual Campinas, Inst Biol, Dept Biochem, Campinas, SP, Brazil
Fac Dent Sao Leopoldo Mand, Campinas, SP, Brazil
State Univ Julio de Mesquita Filho, Dept Enviroment Engn, Sorocaba, SP, Brazil
Fundacao de Amparo Pesquisa do Estado de Sao Paulo: FAPESP 2014/26200-9
Fundacao de Amparo Pesquisa do Estado de Sao Paulo: 2014/14457-5
CNPq: CNPq 487619/2012-9
CNPq: 309612/2013-6
