Preparation and characterization of ketoprofen-loaded microspheres for embolization

• DOI: 10.1007/s10856-011-4492-3
• Publication Date: 2011-11-21T09:07:00Z
• Authors: Chao Zhou; Daichao Cui; Yuan Zhang; Huiyan Yuan; Tianyuan Fan
• Keywords: Ethanol; Polymers; Drug Compounding; T-Lymphocytes; Water; Complement System Proteins; 04 agricultural and veterinary sciences; Embolization, Therapeutic; Models, Biological; Elasticity; Microspheres; Drug Delivery Systems; Freeze Drying; 0404 agricultural biotechnology; Ketoprofen; Calibration; Wettability; Animals; Humans; 0405 other agricultural sciences

To deliver drug locally and relieve the syndrome of pain after uterine artery embolization, N-[tris (hydroxymethyl) methyl] acrylamide-gelatin microspheres were prepared based on inverse suspension polymerization and then separated into a number of subgroups (150-350, 350-560, 560-710, 710-1,000, and 1,000-1,430 μm) by wet-sieving. The microspheres were dried by lyophilization or by washing with anhydrous ethanol. And ketoprofen was loaded by soaking dried blank microspheres into concentrated ketoprofen ethanol solution. The ketoprofen loading level in different subgroups of microspheres was measured and found higher when the microspheres were dried by lyophilization. Equilibrium water content and mean diameters of microspheres decreased after drug loading, especially in subgroups with larger size. The microspheres went through the catheter without any difficulty. Compression and relaxation tests were performed on microspheres before lyophilization, embosphere™, microspheres after lyophilization and ketoprofen loading microspheres. The Young's moduli were 54.74, 64.19, 98.15, and 120.44 kPa, respectively. The release of ketoprofen from microspheres in different subgroups was studied by using the USPII method and T-cell apparatus, respectively. The results indicate that the release rate of ketoprofen depends upon the diameter of microspheres, the type of dissolution apparatus and the flow rate of media in the case that T-cell apparatus was applied. The CH50 test shows that the activation of complement by ketoprofen-loaded microspheres was lower than by blank ones.