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仿生聚合物的体外药物释放和软骨界面润滑性能。

In vitro drug release and cartilage interface lubrication properties of biomimetic polymers.

机构信息

School of Materials Science and Engineering, Nanjing University of Science and Technology, Nanjing, 210009, Jiangsu, PR China.

School of Materials Science and Engineering, Nanjing University of Science and Technology, Nanjing, 210009, Jiangsu, PR China.

出版信息

J Mech Behav Biomed Mater. 2024 Apr;152:106439. doi: 10.1016/j.jmbbm.2024.106439. Epub 2024 Jan 29.

DOI:10.1016/j.jmbbm.2024.106439
PMID:38325166
Abstract

Osteoarthritis is a degenerative disease that is widely found in the elderly population, with a trend towards a younger age group in recent years. In the early stages of arthritis, patients are treated with hyaluronic acid injections and anti-inflammatory drugs. However, it has been found that hyaluronic acid can only play a supportive role and does not have a lubricating effect, and due to the absence of blood vessels, nerves, and lymphatic vessels in the articular cartilage, the oral anti-inflammatory drugs cannot reach the interface of the inflammatory joints adequately, and the drug utilisation rate is low. Herein, we designed and prepared a brush-like bionic lubricant for joint lubrication and drug loading. The poly(2-methyl-2-oxazoline) branched chain was grafted onto the hyaluronic acid main chain by ring-opening polymerisation and graft polymerisation to form a brush-like bionic lubricin containing multiple hydrophilic groups, which was self-assembled to encapsulate the drug by using its multi-branched special structure for drug loading. The friction behaviour tests on the articular cartilage surface showed that the prepared bionic lubricin has excellent lubrication effect, with a minimum friction coefficient of 0.036 close to the lubrication effect of natural synovial fluid, which is mainly due to the hydrophilic groups on its molecular chain that can adsorb the water molecules and form a hydration layer at the cartilage interface, which plays the role of hydration lubrication. In addition, in vitro drug release studies showed that the synthesised drug-loading biomimetic lubricin had a certain drug release capacity, and the maximum drug release rate could reach 77.8 % at 72 h. The synthesis of this bionic lubricant with dual functions of lubrication and drug release provides a new idea for the treatment of osteoarthritis.

摘要

骨关节炎是一种退行性疾病,在老年人群中广泛存在,近年来呈年轻化趋势。在关节炎的早期,患者接受透明质酸注射和抗炎药物治疗。然而,已经发现透明质酸只能起到支持作用,没有润滑效果,并且由于关节软骨中没有血管、神经和淋巴管,口服抗炎药物无法充分到达炎症关节界面,药物利用率低。在此,我们设计并制备了一种用于关节润滑和药物加载的仿生性刷状润滑剂。通过开环聚合和接枝聚合将聚(2-甲基-2-恶唑啉)支链接枝到透明质酸主链上,形成具有多个亲水基团的仿生性仿生润滑素,利用其多分支的特殊结构进行药物负载,自组装包载药物。在关节软骨表面的摩擦行为测试表明,所制备的仿生润滑素有优异的润滑效果,其最小摩擦系数为 0.036,接近天然滑液的润滑效果,这主要是由于其分子链上的亲水基团可以吸附水分子并在软骨界面形成水化层,从而起到水化润滑的作用。此外,体外药物释放研究表明,合成的载药仿生润滑素有一定的药物释放能力,在 72 小时时最大药物释放率可达 77.8%。这种具有润滑和药物释放双重功能的仿生润滑剂的合成,为骨关节炎的治疗提供了新的思路。

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