Preparation, Characterization and ex vivo Intestinal Permeability Studies of Ibuprofen Solid Dispersion

• Published in: Journal of dispersion science and technology Vol. 40; no. 4; pp. 546 - 554
• Main Authors: Alves, Thais Francine Ribeiro, Barros, Cecília Torqueti, Baldo, Denicezar, Amaral, Venâncio Alves, Sever, Mirella, Santos, Carolina, Severino, Patrícia, Chaud, Marco Vinicius
• Format: Journal Article
• Language: English
• Published: Philadelphia Taylor & Francis 03.04.2019; Taylor & Francis Ltd
• Subjects: Crystal structure; Crystallinity; Dispersions; Dissolution; dissolution rate; Ibuprofen; intestinal permeability; Nonsteroidal anti-inflammatory drugs; Penetration; Permeability; solid dispersion; Solubility; solubility equilibrium; Wettability
• ISSN: 0193-2691; 1532-2351
• DOI: 10.1080/01932691.2018.1472014

The aim of the present study was to improve the solubility and dissolution rate of ibuprofen and to evaluate, ex vivo, the intestinal permeation. Solid dispersions (SD) were prepared with Kollicoat IR ® by solvent evaporation technique in different drug:carrier ratios. The permeation intestinal of ibuprofen was evaluated by inverted intestinal sac method. The SD was characterized by solubility equilibrium, FT-IR, DSC, PXRD, SEM, and dissolution rate. The solubility, dissolution rate, and permeability were significantly greater for SD 1:2. The PXRD, SEM and DSC indicated a partial change in the crystalline state of ibuprofen. The solubility equilibrium of SD (1:2) was approximately 15 times greater than the solubility of ibuprofen. Dissolution rate enhancement was attributed to the decreased crystallinity of the ibuprofen, and increase of wettability and decrease of particle size. In conclusion, dissolution rate and intestinal permeability of ibuprofen were enhanced by the use of Kollicoat IR ® carrier in the SD formulation.