Infrared microspectroscopy analysis of Ibuprofen release from drug eluting beads in uterine tissue

• Published in: Journal of controlled release Vol. 135; no. 3; pp. 198 - 202
• Main Authors: Namur, J., Wassef, M., Pelage, J.P., Lewis, A., Manfait, M., Laurent, A.
• Format: Journal Article
• Language: English
• Published: Kidlington Elsevier B.V 05.05.2009; Elsevier
• Subjects: Animals; Anti-Inflammatory Agents, Non-Steroidal - analysis; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Biological and medical sciences; Calibration; Delayed-Action Preparations; Dose-Response Relationship, Drug; Drug eluting beads; Embolization; Embolization, Therapeutic; Female; General pharmacology; Ibuprofen; Ibuprofen - analysis; Ibuprofen - pharmacokinetics; In vivo drug release; Infrared microspectroscopy; Medical sciences; Microspheres; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Sensitivity and Specificity; Sheep, Domestic; Spectrophotometry, Infrared; Spectrophotometry, Ultraviolet; Spectroscopy, Fourier Transform Infrared; Time Factors; Uterus - blood supply; Embolization; In vivo drug release; Drug eluting beads; Infrared microspectroscopy; Ibuprofen; Drug; Prostaglandin-endoperoxide synthase; Pharmaceutical technology; Enzyme; Enzyme inhibitor; Non steroidal antiinflammatory agent; In vivo; Tissue; Arylpropionic acid derivatives; Oxidoreductases; Release
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/j.jconrel.2008.12.017

Ibuprofen loaded embolization beads (IBU-BB) have been developed to reduce inflammation and pain following uterine artery embolization for the treatment of uterine fibroids. The present work has investigated the elution properties of IBU-BB in situ after embolization with Fourier Transform Infrared Microspectroscopy (FTIRMS). Twelve sheep underwent uterine artery embolization with IBU-BB (485 mM) or control unloaded beads. IBU concentration was determined inside the beads and in the tissue surrounding the beads using FTIRMS of uterine tissue sections sampled 24 h or 1 week after embolization. After 24 h, IBU concentration inside the bead was only 18.6 mM out of the 485 mM initially loaded ( p < 0.0001, univariate sign test). The concentration in the tissue around the beads was 8 mM, which is well above the in vitro therapeutic levels (6 µM). After one week the concentration of IBU had decreased to 4.9 mM in the beads ( p = 0.0502, Mann Whitney) and no IBU was detected in the surrounding tissue. This work has demonstrated that IBU-BB can provide a sustained release of the anti-inflammatory drug over at least one week. The in vivo elution properties of IBU-BB may be suitable to alleviate pain and inflammation after embolization. [Display omitted]