UCD School of Veterinary Medicine, University College Dublin, Belfield, Dublin 4, Ireland.
School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland.
Drug Deliv Transl Res. 2018 Oct;8(5):1421-1435. doi: 10.1007/s13346-018-0557-x.
Polyelectrolyte nanoparticle constructs (NPs) comprising salmon calcitonin (sCT), chitosan (CS), and hyaluronic acid (HA) were previously established as having anti-inflammatory potential when injected via the intra-articular (i.a.) route to a mouse model. We attempted to translate the formulation to a large animal model, the lipopolysaccharide (LPS)-stimulated equine model of joint inflammation. The aim was to manufacture under aseptic conditions to produce sterile pyrogen-free NPs, to confirm physicochemical characteristics, and to test toxicity and efficacy in a pilot study. NP dispersions were successfully formulated using pharmaceutical-grade source materials and were aseptically manufactured under GMP-simulated conditions in a grade A modular aseptic processing workstation. The NP formulation had no detectable pathogen or endotoxin contamination. NPs were then tested versus a lactated Ringer's solution control following single i.a. injections to the radiocarpal joints of two groups of four horses pre-treated with LPS, followed by arthrocentesis at set intervals over 1 week. There was no evidence of treatment-related toxicity over the period. While there were no differences between clinical read-outs of the NP and the control, two synovial fluid-derived biomarkers associated with cartilage turnover revealed a beneficial effect of NPs. In conclusion, NPs comprising well-known materials were manufactured for an equine i.a.-injectable pilot study and yielded no NP-attributable toxicity. Evidence of NP-associated benefit at the level of secondary endpoints was detected as a result of decreases in synovial fluid inflammatory biomarkers.
聚电解质纳米颗粒构建体(NPs)由鲑鱼降钙素(sCT)、壳聚糖(CS)和透明质酸(HA)组成,此前已被证实具有抗炎潜力,可通过关节内(i.a.)途径注射到小鼠模型中。我们试图将该配方转化为大型动物模型,即脂多糖(LPS)刺激的马关节炎症模型。目的是在无菌条件下制造,以生产无菌无热原的 NPs,确认理化特性,并在初步研究中测试其毒性和疗效。使用制药级原料成功配制了 NP 分散体,并在 A 级模块化无菌处理工作站中在 GMP 模拟条件下无菌制造。NP 配方没有检测到病原体或内毒素污染。然后,在 LPS 预处理的两组四匹马的桡腕关节中单次关节内注射后,将 NP 制剂与乳酸林格氏液对照进行测试,然后在 1 周内每隔一段时间进行关节穿刺。在此期间,没有证据表明与治疗相关的毒性。虽然 NP 和对照的临床读数之间没有差异,但与软骨周转率相关的两种滑膜液衍生生物标志物显示 NP 具有有益作用。总之,制造了包含众所周知的材料的 NPs,用于马关节内注射的初步研究,并且没有产生任何与 NP 相关的毒性。由于滑膜液炎症生物标志物的减少,检测到与 NP 相关的次要终点的有益效果。