betadex and Colitis--Ulcerative

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-β-CD inclusion complex incorporated into PL 407 and PL407-PL403 thermoreversible hydrogels, considering physico-chemical and pharmaceutical aspects. Complexation between BUD and HP-β-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-β-CD and PL 407 or PL407-PL403 association. Micellar hydrodynamic diameter studies showed the interaction between HP-β-CD and PL blocks, as well as the reorganization of the micellar system in the presence of BUD and its inclusion complex. Micellization temperature (Tm) was not shifted, but sol-gel phase transition studies showed that in the presence of BUD, HP-β-CD or BUD:HP-β-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-β-CD cavity evoked by PL407 or PL407-PL403 addition. These findings point out the BUD-HP-β-CD in PL-based hydrogels as strategies for future investigations on development of new pharmaceutical formulations for the treatment of ulcerative colitis.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Animals; Anti-Inflammatory Agents; beta-Cyclodextrins; Budesonide; Calorimetry, Differential Scanning; Chemical Phenomena; Colitis, Ulcerative; Drug Liberation; Humans; Hydrodynamics; Hydrogels; Micelles; Microscopy, Electron, Scanning; Phase Transition; Poloxamer; Solubility; Spectroscopy, Fourier Transform Infrared; Temperature

To prepare paeonol-beta-cyclodextrin inclusion complex (Pae-beta-CYD) loaded colon-specific release tablets.. The core tablets were prepared with the mixture of Pae-beta-CYD inclusion complex, peotin and calcium acetate, and coated with ethanolic solution of Eudragit S100. The effects of coating weight, amount of plasticizer, curing time and temperature on the release of drug from tablets were investigated in vitro.. About 5-6 h retarded release of paeonol in the dissolution media of pectinase or rats colon contents were obtained by 12% coating weight gain and 20% Dibutyl phthalate (DBP) was used as plasticizer, and subsequently curing the tablets at 45 degrees C for 12 h.. Pae-beta-CYD loaded colon-specific release tablets showed pH environment and enzyme dependant release properties.

Topics: Acetophenones; Animals; beta-Cyclodextrins; Colitis, Ulcerative; Colon; Drug Delivery Systems; Excipients; Humans; Hydrogen-Ion Concentration; Rats; Rats, Sprague-Dawley; Tablets, Enteric-Coated