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Self-assembled lyotropic liquid crystal gel for osteoarthritis treatment via anti-inflammation and cartilage protection
Biomaterials Science ( IF 5.8 ) Pub Date : 2021-09-08 , DOI: 10.1039/d1bm00727k
Liling Mei 1 , Hui Wang 1 , Jintian Chen 1 , Ziqian Zhang 1 , Feng Li 1 , Yecheng Xie 1 , Ying Huang 2 , Tingting Peng 2 , Guohua Cheng 2 , Xin Pan 1 , Chuanbin Wu 2
Affiliation  

Osteoarthritis (OA) is a chronic joint disease with occurrence of articular inflammation and cartilage degeneration. An ideal drug delivery system for effective treatment of OA should integrate inflammation alleviation with cartilage protection. Herein, a lyotropic liquid crystal (LLC) precursor co-loading hyaluronic acid (HA) and celecoxib, formulated as the HLC precursor, was developed for the combined therapeutic efficacy. The in situ gelling property of the HLC precursor effectively prolongs drug retention in the articular cavity to achieve a long-term anti-inflammation effect. Based on the rheological tests, HLC gel with a cubic lattice structure endows it with a spring-like effect to buffer joint shock and shows great potential in providing cartilage protection by resisting mechanical destruction, lubricating joint, and decomposing intensive stress (about 50%). Meanwhile, the pharmacodynamics study on the OA-induced SD rats demonstrated that HLC gel was the most effective to reduce inflammation levels and to protect the cartilage against abrasion and degeneration. Furthermore, the in vivo degradation behavior and the intra-articular irritation results of LLC/HLC gel demonstrated that it was biodegradable and biocompatible. These results collectively demonstrated that HLC gel with anti-inflammation and cartilage protection performance provides a useful approach to treat OA.

中文翻译:

自组装溶致液晶凝胶通过抗炎和软骨保护治疗骨关节炎

骨关节炎(OA)是一种慢性关节疾病,发生关节发炎和软骨退变。有效治疗 OA 的理想给药系统应将炎症缓解与软骨保护相结合。在此,开发了一种溶致液晶 (LLC) 前体共负载透明质酸 (HA) 和塞来昔布,配制成 HLC 前体,用于联合治疗效果。在原位HLC前体的胶凝特性有效延长药物在关节腔内的滞留时间,达到长期抗炎作用。根据流变学测试,立方晶格结构的HLC凝胶赋予其类似弹簧的效果来缓冲关节冲击,并在通过抵抗机械破坏、润滑关节和分解强应力(约50%)提供软骨保护方面显示出巨大潜力. 同时,对 OA 诱导的 SD 大鼠的药效学研究表明,HLC 凝胶在降低炎症水平和保护软骨免受磨损和变性方面最有效。此外,体内LLC/HLC 凝胶的降解行为和关节内刺激结果表明它具有生物可降解性和生物相容性。这些结果共同证明了具有抗炎和软骨保护性能的 HLC 凝胶为治疗 OA 提供了一种有用的方法。
更新日期:2021-09-24
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