title: Albumin microspheres as carriers for the antiarthritic drug celecoxib.
abstract: The present study investigates the preparation of celecoxib-loaded albumin microspheres and the biodistribution of technetium-99m ((99m)Tc)-labeled celecoxib as well as its microspheres after intravenous administration. Microspheres were prepared using a natural polymer BSA using emulsification chemical cross-linking method. The prepared microspheres were characterized for entrapment efficiency, particle size, and in vitro drug release. Surface morphology was studied by scanning electron microscopy. Biodistribution studies were performed by radiolabeling celecoxib (CS) and its microspheres (CMS) using (99m)Tc and injecting arthritic rats intravenously. The geometric mean diameter of the microspheres was found to be 5.46 microm. In vitro release studies indicated that the microspheres sustained the release of the drug for 6 days. Radioactivity measured in different organs after intravenous administration of celecoxib solution showed a significant amount of radioactivity in the liver and spleen. In case of celecoxib-loaded microspheres, a significant amount of radioactivity accumulated in the lungs. No significant difference (P > .1) in the radioactivity was observed between the inflamed joint and the noninflamed joint following intravenous injection of (99m)Tc-CS. However, in case of the microspheres (CMS), the radioactivity present in the inflamed joint was 2.5-fold higher than in the noninflamed joint. The blood kinetic studies revealed that celecoxib-loaded albumin microspheres exhibited prolonged circulation than the celecoxib solution.
authors.affiliation: Drug Delivery Laboratory, Centre of Relevance and Excellence in New Drug Delivery system Pharmacy Department, MS University of Baroda, Fatehgunj, Vadodara-390 002, India.
authors.forename: Hetal
authors.initials: H
authors.lastname: Thakkar
authors.forename: Rakesh Kumar
authors.initials: RK
authors.lastname: Sharma
authors.forename: Anil Kumar
authors.initials: AK
authors.lastname: Mishra
authors.forename: Krishna
authors.initials: K
authors.lastname: Chuttani
authors.forename: Rayasa Ramchandra
authors.initials: RR
authors.lastname: Murthy
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000097:blood; D001169:Arthritis, Experimental / Q000097:blood / Q000188:drug therapy; D002417:Cattle; D000068579:Celecoxib; D004337:Drug Carriers / Q000008:administration & dosage* / Q000378:metabolism; D008863:Microspheres; D011720:Pyrazoles / Q000008:administration & dosage* / Q000097:blood; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D012710:Serum Albumin, Bovine / Q000008:administration & dosage* / Q000378:metabolism; D013449:Sulfonamides / Q000008:administration & dosage* / Q000097:blood
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D011720:Pyrazoles; D013449:Sulfonamides; D012710:Serum Albumin, Bovine; D000068579:Celecoxib