Zhang Tingting, Chen Shiqi, Dou Haibo, Liu Quanjin, Shu Gang, Lin Juchun, Zhang Wei, Peng Guangneng, Zhong Zhijun, Fu Hualin
Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, People's Republic of China.
Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan 611130, People's Republic of China.
Mater Sci Eng C Mater Biol Appl. 2021 Jan;118:111352. doi: 10.1016/j.msec.2020.111352. Epub 2020 Aug 11.
Glucosamine (GlcN) is a common drug used to treat osteoarthritis (OA). To prolong the action time of glucosamine on OA and improve its therapeutic effect, this research explored the potential application of GlcN-loaded thermosensitive hydrogels based on poloxamer 407 and poloxamer 188 for OA therapy by intra-articular injection. The thermosensitive hydrogels were prepared by cold method, and the effects of P407, P188, and GlcN on sol-gel transition temperature (T) were compared. After screening was performed, the optimized formulation showed good temperature sensitivity, and T was approximately 35 °C. In vitro release tests showed that GlcN was slowly released from the thermosensitive hydrogels. After the gels were intra-articularly administered to treat OA in rabbits, the degree of swelling and inflammatory factors were significantly decreased in the hydrogel group compared with those in the OA model group (P < 0.05). Histological results showed that the GlcN-administered group had a good repair effect on damaged cartilage. At the same dose, the effect of the thermosensitive hydrogels was better than that of the aqueous solution. Therefore, GlcN-loaded thermosensitive hydrogels based on poloxamers are promising sustainable delivery systems for OA therapy by intra-articular injection.
氨基葡萄糖(GlcN)是一种用于治疗骨关节炎(OA)的常用药物。为了延长氨基葡萄糖对OA的作用时间并提高其治疗效果,本研究探索了基于泊洛沙姆407和泊洛沙姆188的载氨基葡萄糖热敏水凝胶通过关节内注射在OA治疗中的潜在应用。热敏水凝胶采用冷法制备,并比较了P407、P188和GlcN对溶胶-凝胶转变温度(T)的影响。筛选后,优化配方显示出良好的温度敏感性,T约为35℃。体外释放试验表明,GlcN从热敏水凝胶中缓慢释放。将凝胶关节内给药治疗兔OA后,水凝胶组的肿胀程度和炎症因子与OA模型组相比显著降低(P<0.05)。组织学结果表明,给予GlcN的组对受损软骨有良好的修复作用。在相同剂量下,热敏水凝胶的效果优于水溶液。因此,基于泊洛沙姆的载氨基葡萄糖热敏水凝胶是通过关节内注射进行OA治疗的有前景的可持续给药系统。