Small molecule inhibitors of osteoarthritis: Current development and future perspective

Abstract

Osteoarthritis (OA) is one of the common degenerative joint diseases in clinic. It mainly damages articular cartilage, causing pain, swelling and stiffness around joints, and is the main cause of disability of the elderly. Due to the unclear pathogenesis of osteoarthritis and the poor self-healing ability of articular cartilage, the treatment options for this disease are limited. At present, NSAIDs, Glucocorticoid and Duloxetine are the most commonly used treatment choice for osteoarthritis. Although it is somewhat effective, the adverse reactions are frequent and serious. The development of safer and more effective anti-osteoarthritis drugs is essential and urgent. This review summarizes recent advances in the pharmacological treatment of OA, focusing on small molecule inhibitors targeting cartilage remodeling in osteoarthritis as well as the research idea of reducing adverse effects by optimizing the dosage form of traditional drugs for the treatment of osteoarthritis. It should provide a reference for exploration of new potential treatment options.

Enhanced Surface Immunomodification of Engineered Hydrogel Materials through Chondrocyte Modulation for the Treatment of Osteoarthritis

“…Besides intra-articular delivery, transdermal drug delivery is also an efficient method [92,93]. However, transdermal medications are limited to those that alleviate symptoms but do not alter disease progression or repair cartilage [94]. Some medications may have side effects, like gastrointestinal issues with NSAIDs or joint destruction risks with glucocorticoids.…”

“…PRP, an autologous blood product derived from the patient's own blood, offers high safety and minimal side effects [95,96]. PRP contains bioactive factors like platelet-derived growth factor (PDGF), transforming growth factor β (TGF-β), insulin-like growth factor (IGF), and fibroblast growth factor (FGF), crucial for regulating chondrocyte survival and metabolism [94]. Studies indicated that PRP promoted chondrocyte proliferation and matrix production while reducing inflammation [97][98][99].…”

Regulating Chondro‐Bone Metabolism for Treatment of Osteoarthritis via High‐Permeability Micro/Nano Hydrogel Microspheres

“…Although the OA disease phenotype remains ambiguous, many animal and clinical trials have shown that targeting the early activation of osteoclasts can block the abnormal reconstruction of SB, thereby preventing articular cartilage degeneration. [12] Mitochondrial reactive oxygen species (ROS), as secondary messengers, initiate the differentiation of hematopoietic stem cell or monocyte/macrophage progenitor cells into osteoclasts. [13] Currently, Targeting mitochondria-generated ROS effectively inhibits osteoclast activation.…”

“…Although the OA disease phenotype remains ambiguous, many animal and clinical trials have shown that targeting the early activation of osteoclasts can block the abnormal reconstruction of SB, thereby preventing articular cartilage degeneration. [ 12 ]…”