Zheng Peng, Wei Yongtao, Cao Keren, Xu Chen, Yu Shanshan, Liu Yang, Li Min, Zhang Chunyan, Wang Tao
Shandong University of Traditional Chinese Medicine, No. 4655 Daxue Road, Jinan, 250300, Shandong, China.
Jinan Third People's Hospital, No. 1 Wangsheren Road, Jinan, 250101, Shandong, China.
Biomed Microdevices. 2025 May 29;27(2):23. doi: 10.1007/s10544-025-00753-2.
Osteoarthritis (OA) is the common form of chronic joint disease. The disease progression can affect all joints of the body, seriously affecting patients’ quality of life. The most effective clinical treatment for OA at the moment is the oral or intravenous administration of non-steroidal anti-inflammatory drugs, such as meloxicam (MX). However, certain challenges associated with the conventional use of those drugs include long dosing cycles, poor patient compliance, and systemic toxic side effects, primarily gastrointestinal reactions. Joint synovial fluid mainly consists of sodium hyaluronate (HA). In recent years, HA has been developed and used to treat OA with local injections. However, it also faces the limitations of short injection cycle, frequent administration, and increases the risk of exogenous infection. In this study, a microsphere gel formulation containing PL407, HA and meloxicam microspheres was prepared and the MX-MS-Gel system showed good performance, syringeability and stability. The results of in vitro release studies showed that the MX-MS-Gel released 8.6% in vitro at 72 h and 28.0% at 480 h, with a more moderate drug release. By injecting iodoacetic acid into the knee joint of rats to establish an OA model, MX-MS-Gel significantly improved the inflammatory response of OA, while the safety of MX-MS-Gel was superior and evaluated in this study, which was safe. The results showed that MX-MS-Gel could realize the purpose of delaying the drug release rate and reducing the frequency of administration, thus improving patient compliance and medication safety.
[Image: see text]
The online version contains supplementary material available at 10.1007/s10544-025-00753-2.
骨关节炎（OA）是慢性关节疾病的常见形式。疾病进展会影响身体的所有关节，严重影响患者的生活质量。目前OA最有效的临床治疗方法是口服或静脉注射非甾体抗炎药，如美洛昔康（MX）。然而，这些药物常规使用存在一些挑战，包括给药周期长、患者依从性差以及全身毒性副作用，主要是胃肠道反应。关节滑液主要由透明质酸钠（HA）组成。近年来，HA已被开发用于局部注射治疗OA。然而，它也面临注射周期短、给药频繁以及增加外源感染风险的局限性。在本研究中，制备了一种含有PL407、HA和美洛昔康微球的微球凝胶制剂，MX-MS-Gel系统表现出良好的性能、可注射性和稳定性。体外释放研究结果表明，MX-MS-Gel在72小时体外释放8.6%，在480小时释放28.0%，药物释放较为适中。通过向大鼠膝关节注射碘乙酸建立OA模型，MX-MS-Gel显著改善了OA的炎症反应，同时本研究评估了MX-MS-Gel的安全性，其安全性良好。结果表明，MX-MS-Gel可以实现延缓药物释放速率和减少给药频率的目的，从而提高患者依从性和用药安全性。
[图像：见正文]
在线版本包含可在10.1007/s10544-025-00753-2获取的补充材料。
