Division of Orthopaedic Surgery, Department of Surgery, Duke University Medical Center, Duke University, Durham, North Carolina 27708-0281, USA.
Tissue Eng Part B Rev. 2010 Feb;16(1):81-92. doi: 10.1089/ten.teb.2009.0447.
Osteoarthritis (OA) is a degenerative joint disease that can result in joint pain, loss of joint function, and deleterious effects on activity levels and lifestyle habits. Current therapies for OA are largely aimed at symptomatic relief and may have limited effects on the underlying cascade of joint degradation. Local drug delivery strategies may provide for the development of more successful OA treatment outcomes that have potential to reduce local joint inflammation, reduce joint destruction, offer pain relief, and restore patient activity levels and joint function. As increasing interest turns toward intra-articular drug delivery routes, parallel interest has emerged in evaluating drug biodistribution, safety, and efficacy in preclinical models. Rodent models provide major advantages for the development of drug delivery strategies, chiefly because of lower cost, successful replication of human OA-like characteristics, rapid disease development, and small joint volumes that enable use of lower total drug amounts during protocol development. These models, however, also offer the potential to investigate the therapeutic effects of local drug therapy on animal behavior, including pain sensitivity thresholds and locomotion characteristics. Herein, we describe a translational paradigm for the evaluation of an intra-articular drug delivery strategy in a rat OA model. This model, a rat interleukin-1beta overexpression model, offers the ability to evaluate anti-interleukin-1 therapeutics for drug biodistribution, activity, and safety as well as the therapeutic relief of disease symptoms. Once the action against interleukin-1 is confirmed in vivo, the newly developed anti-inflammatory drug can be evaluated for evidence of disease-modifying effects in more complex preclinical models.
骨关节炎(OA)是一种退行性关节疾病,可导致关节疼痛、丧失关节功能,并对活动水平和生活方式习惯产生有害影响。目前针对 OA 的治疗方法主要是针对症状缓解,可能对关节退化的潜在级联反应效果有限。局部药物输送策略可能为开发更成功的 OA 治疗结果提供机会,这些结果有可能减轻局部关节炎症、减少关节破坏、提供疼痛缓解,并恢复患者的活动水平和关节功能。随着人们对关节内药物输送途径的兴趣不断增加,对药物生物分布、安全性和临床前模型疗效的评估也出现了平行的兴趣。啮齿动物模型为药物输送策略的开发提供了主要优势,主要是因为成本较低、成功复制了人类 OA 样特征、疾病发展迅速,以及关节体积小,在方案开发过程中可以使用较少的总药物量。然而,这些模型也提供了研究局部药物治疗对动物行为(包括疼痛敏感性阈值和运动特征)的治疗效果的潜力。本文描述了一种在大鼠 OA 模型中评估关节内药物输送策略的转化范例。该模型是一种大鼠白细胞介素-1β过表达模型,能够评估针对白细胞介素-1 的治疗药物的生物分布、活性和安全性,以及疾病症状的治疗缓解。一旦在体内确认了针对白细胞介素-1 的作用,就可以在更复杂的临床前模型中评估新开发的抗炎药物是否具有疾病修饰作用的证据。