School of Animal and Veterinary Sciences, Charles Sturt University, Wagga Wagga, New South Wales, Australia.
Vet J. 2011 Oct;190(1):15-21. doi: 10.1016/j.tvjl.2010.09.019. Epub 2010 Oct 13.
The rationale behind developing sustained release microsphere formulations of non-steroidal anti-inflammatory drugs (NSAIDs) administered via the intra-articular (IA) route is to minimise the systemic bioavailability and attendant side-effects associated with oral drug administration. Overall dose is reduced whilst therapeutic benefit within the joint is maintained. The potential benefits of IA therapy for osteoarthritis (OA) are not achieved using currently available medications and delivery vehicles due to the rapid clearance of therapeutic substances from the synovial space. There is a need for sustained release delivery systems if the potential of IA drug administration is to be realised. Rationally designed microspheres taken up by synovial macrophages offer a strategy to sustain drug delivery within the joint, and to deliver NSAIDs directly to pivotal inflammatory cells. The efficacy of microsphere candidates may be evaluated in large animal models of OA. The principles of IA microsphere drug delivery may also be applicable to other classes of drugs.
通过关节内（IA）途径给予非甾体抗炎药（NSAIDs）的缓控释微球制剂的研发原理在于将与口服药物治疗相关的全身生物利用度和副作用最小化。在维持关节内治疗效果的同时，减少整体剂量。由于治疗物质从滑膜空间中迅速清除，目前可用的药物和给药载体无法实现关节内治疗对骨关节炎（OA）的潜在益处。如果要实现关节内药物给药的潜力，则需要缓控释给药系统。被滑膜巨噬细胞摄取的合理设计的微球为在关节内持续提供药物输送提供了一种策略，并将 NSAIDs 直接递送至关键炎症细胞。微球候选物的疗效可以在 OA 的大动物模型中进行评估。IA 微球药物输送的原理也可能适用于其他类别的药物。
