title: Enhanced targeting efficiency of PLGA microspheres loaded with Lornoxicam for intra-articular administration.
abstract: Owing to its rationale of targeting the drug to the site of action and minimizing systemic toxic effects of the drug, intra-articular drug delivery system has gained growing interests. In this study, emphasis was placed on intra-articular Lornoxicam-loaded PLGA microspheres (Lnxc-PLGA-MS) preparation and improving the targeting of lornoxicam (Lnxc) in knee joint. The microspheres were prepared by a process involving solid-in-oil-in-water(S/O/W) emulsion, and evaluated for physicochemical properties. Joint cavity's drug leakage into systemic circulation in rabbits was examined to define the drug stagnation. Meanwhile, drug retention in synovial fluid in rats was investigated to further validate the drug targeting. The microspheres were spherical as evidenced by the SEM photographs with mean size of 7.47 μm, and encapsulation efficiency was observed 82.22% along with drug loading 12.17%. DSC revealed that the drug in the microspheres existed in the phase of uncrystallization. The formulated microspheres could prolong the drug release up to 32 days in vitro. Comparing with animals injected with lornoxicam solution, the plasma drug concentration decreased in rabbits and retention time increased in rats' synovial fluid with intra-articular injections of microspheres, revealing good targeting efficiency. In conclusion, PLGA microspheres could be used to deliver lornoxicam following intra-articular administration for enhancing targeting efficiency.
authors.affiliation: The School of Pharmaceutical Science, Shandong University, 44 Wenhua Xi Road, Ji'nan, China.
authors.forename: Zhiyue
authors.initials: Z
authors.lastname: Zhang
authors.forename: Xiuli
authors.initials: X
authors.lastname: Bi
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.forename: Guihua
authors.initials: G
authors.lastname: Huang
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004655:Emulsions; D007270:Injections, Intra-Articular; D007719:Knee Joint / Q000378:metabolism; D019344:Lactic Acid / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D010894:Piroxicam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013582:Synovial Fluid / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D010894:Piroxicam; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C059451:lornoxicam