Ibuprofen-loaded porous microspheres suppressed the progression of monosodium iodoacetate-induced osteoarthritis in a rat model

The objectives of this study were (1) to fabricate ibuprofen-loaded porous microspheres (IBU/PMSs), (2) to evaluate the in vitro anti-inflammatory effects of the microspheres using LPS-induced inflammation in cultured synoviocytes, and (3) to evaluate the in vivo effect of the IBU/PMSs on the progression of monosodium iodoacetate (MIA)-induced osteoarthritis (OA) in a rat model. A dose-dependent in vitro anti-inflammatory effect on pro-inflammatory cytokine markers (matrix metallopeptidase-3 (MMP-3), matrix metallopeptidase-13 (MMP-13), cyclooxygenase-2 (COX-2), a disintegrin and metalloproteinase with thrombospondin motifs-5 (ADAMTS-5)), interleukin-6 (IL-6), and tumor necrosis factor (TNF-α) was observed by confirming with real-time PCR analyses. In vivo, treatment with IBU/PMSs reduced MIA-stimulated mRNA expression of MMP-3, MMP-13, COX-2, ADAMTS-5, IL-6, and TNF-α in rat synoviocytes. In addition, we demonstrated that intra-articular IBU/PMSs suppressed the progression of MIA-induced OA in the rat model via anti-inflammatory mechanisms. In conclusion, IBU/PMSs are a promising therapeutic material to control the pain and progression of OA.