Possible Toxic Effect of Tranexamic Acid and Aminocaproic Acid on Articular Cartilage: An In Vitro and In Vivo Analysis

Objective To compare the dose-dependent chondrotoxicity of tranexamic acid (TXA) and aminocaproic acid (ACA) in vitro and in vivo. Design In vitro , human chondrocytes were exposed to TXA or ACA (0-50 mg/ml), and cytotoxicity was assessed. In vivo , a rat model of monoiodoacetate-induced osteoarthritis was used to evaluate cartilage damage following intra-articular injections of TXA or ACA. Results In vitro , both TXA and ACA reduced chondrocyte viability in a dose-dependent manner, with significant cytotoxicity observed at concentrations ≥20 mg/ml. TXA was more toxic than ACA at these higher concentrations. Apoptosis increased markedly at 30 mg/ml for both agents. In the rat osteoarthritis model, joints treated with TXA or ACA showed greater cartilage erosion and matrix loss compared to controls, with TXA causing more severe damage. Conclusion Both TXA and ACA are chondrotoxic in a dose-dependent manner, with TXA demonstrating greater potency. Lower concentrations (≤10 mg/ml) are recommended for topical use in cartilage-preserving surgery to minimize potential damage.