Kaderli S, Boulocher C, Pillet E, Watrelot-Virieux D, Roger T, Viguier E, Gurny R, Scapozza L, Möller M
School of Pharmaceutical Sciences, University of Geneva and Lausanne, Geneva, Switzerland.
UPSP ICE 2011.03.101, Université de Lyon, VetAgro Sup, Lyon, France.
Eur J Pharm Biopharm. 2015 Feb;90:70-9. doi: 10.1016/j.ejpb.2014.10.016. Epub 2014 Nov 11.
To overcome the problem of fast degradation of Hyaluronic Acid (HA) in the treatment of osteoarthritis (OA), HA was protected against the oxidative stress generated by the pathology. Antioxidant conjugated HAs were synthesized and tested in vitro for their resistance in an oxidative environment mimicking OA. HA-4-aminoresorcinol (HA-4AR) displayed the interesting property of increasing in viscosity under oxidative conditions because of crosslinking induced by electron transfer. The novel HA polymer conjugate was shown to be biocompatible in vitro on fibroblast-like synoviocytes extracted from an arthritic patient. This HA conjugate was also assessed in vivo by intra-articular injection in healthy rabbits and was found to be comparable to the native polymer in terms of biocompatibility. This study suggests that HA-4AR is a promising candidate for a next generation viscosupplementation formulation.
为克服透明质酸(HA)在骨关节炎(OA)治疗中快速降解的问题,对HA进行了保护,使其免受该病理过程产生的氧化应激影响。合成了抗氧化剂共轭透明质酸,并在体外模拟OA的氧化环境中测试其抗性。HA-4-氨基间苯二酚(HA-4AR)表现出在氧化条件下由于电子转移诱导交联而导致粘度增加的有趣特性。新型HA聚合物共轭物在体外对从关节炎患者提取的成纤维细胞样滑膜细胞显示出生物相容性。还通过在健康兔体内进行关节内注射对这种HA共轭物进行了体内评估,发现其在生物相容性方面与天然聚合物相当。这项研究表明,HA-4AR是下一代粘弹性补充剂配方的有前途的候选物。