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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Evaluation of Budesonide-Hydroxypropyl-β-Cyclodextrin Inclusion Complex in Thermoreversible Gels for Ulcerative
Carolina Martins Lázaro1, Carolina C de Oliveira1, Alessandra Gambero2
1Universidade São Francisco, Av. São Francisco de Assis 218, Bragança Paulista, São Paulo, 12916-900, Brazil.
Background:
New formulations for topical treatment of ulcerative colitis with budesonide inclusion complex (BUDHP-β-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-BUDHP-β-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-β-CD + PL407 (18%); BUD 2: BUDHP-β-CD + PL407 (20%); BUD 3: BUDHP-β-CD + PL407 (18%) + PL403 (2%); BUD 4: plain BUD; BUD 5: BUDHP-β-CD; 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:
BUDHP-β-CD poloxamer formulations had similar MPO activity when compared with the negative control group. All formulations presented lower MPO activity than BUDHP-β-CD and plain BUD (p < 0.001). BUD 2 produced lower microscopic score values than plain BUD and BUDHP-β-CD (p < 0.01). All formulations with BUDHP-β-CD 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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