Rudnik-Jansen Imke, Woike Nina, de Jong Suzanne, Versteeg Sabine, Kik Marja, Emans Pieter, Mihov George, Thies Jens, Eijkelkamp Niels, Tryfonidou Marianna, Creemers Laura
Department of Orthopedics, University Medical Center Utrecht, Heidelberglaan 100, 3508 GA Utrecht, The Netherlands.
DSM Biomedical B.V., Koestraat 1, 6167 RA Geleen, The Netherlands.
Pharmaceutics. 2019 Feb 7;11(2):70. doi: 10.3390/pharmaceutics11020070.
Episodes of inflammation and pain are predominant features of arthritic joint diseases. Drug delivery systems (DDS) could reduce inflammation and pain long-term without chances of infection upon multiple injections. To allow for long-term evaluation of DDS, we modified a previously published acute arthritis model by extending follow-up periods between flare-ups. Unilateral synovial inflammation of the knee was induced by intra-articular injection of streptococcal cell wall peptidoglycan polysaccharide (PGPS), and flare-ups were induced by intravenous PGPS injections every 4 weeks for a total duration of 84 days. In PGPS-reactivated animals, joint swelling, pain behavior, post mortem synovitis, and osteophyte formation were notable features. Hepatitis, splenitis and inflammation of non-primed joints were observed as systemic side effects. To test the applicability of the modified arthritis model for long-term testing of DDS, the duration of anti-inflammatory and analgesic effects of a corticosteroid released from two different polymer-based platforms was evaluated. The current modified arthritis model has good applicability for testing of DDS for a prolonged period of time. Furthermore, the novel autoregulatory polyesteramide (PEA) microsphere platform releasing triamcinolone acetonide (TAA) was benchmarked against poly lactic-co-glycolic acid (PLGA) and reduced joint swelling and pain behavior more potently compared to TAA-loaded PLGA microspheres.
炎症和疼痛发作是关节炎性关节疾病的主要特征。药物递送系统(DDS)可以长期减轻炎症和疼痛,多次注射时不会有感染风险。为了对DDS进行长期评估,我们通过延长发作之间的随访期,对先前发表的急性关节炎模型进行了改良。通过关节内注射链球菌细胞壁肽聚糖多糖(PGPS)诱导膝关节单侧滑膜炎,并每4周静脉注射PGPS诱导发作,总持续时间为84天。在PGPS重新激活的动物中,关节肿胀、疼痛行为、死后滑膜炎和骨赘形成是显著特征。观察到肝炎、脾炎和未致敏关节的炎症作为全身副作用。为了测试改良关节炎模型在DDS长期测试中的适用性,评估了从两种不同的基于聚合物的平台释放的皮质类固醇的抗炎和镇痛作用持续时间。当前的改良关节炎模型在长时间测试DDS方面具有良好的适用性。此外,将释放曲安奈德(TAA)的新型自调节聚(酯-酰胺)(PEA)微球平台与聚乳酸-乙醇酸共聚物(PLGA)进行了比较,与载有TAA的PLGA微球相比,其更有效地减轻了关节肿胀和疼痛行为。