Kim Sang Jun, Choi Youngbo, Min Khee Tae, Hong Surin
Seoul Jun Research Center, Seoul Jun Rehabilitation Clinic, Seoul 06737, Korea.
Department of Safety Engineering, Chungbuk National University, Gyeongju 28644, Korea.
Pharmaceutics. 2022 May 4;14(5):985. doi: 10.3390/pharmaceutics14050985.
Radially mesoporous silica nanoparticles (RMSNs) with protonated amine functionality are proposed to be a dexamethasone (Dex) carrier that could achieve a sustained anti-inflammatory effect in rheumatoid arthritis (RA). High-capacity loading and a sustained release of target drugs were achieved by radially oriented mesopores and surface functionality. The maximum loading efficiency was confirmed to be about 76 wt%, which is about two times greater than that of representative mesopores silica, SBA-15. In addition, Dex-loaded RMSNs allow a sustained-release profile with about 92% of the loaded Dex for 100 h in vitro, resulting in 2.3-fold better delivery efficiency of Dex than that of the SBA-15 over the same period. In vivo evaluation of the inhibitory effects on inflammation in a RA disease rat model showed that, compared with the control groups, the group treated with Dex-loaded RMSNs sustained significant anti-inflammatory effects and recovery of cartilage over a period of 8 weeks. The in vivo effects were confirmed via micro-computed tomography, bone mineral density measurements, and modified Mankin scoring. The proposed Dex-loaded RMSNs prolonged the life of the in vivo concentrations of therapeutic agents and maximized their effect, which should encourage its application.
具有质子化胺功能的径向介孔二氧化硅纳米颗粒（RMSNs）被认为是一种地塞米松（Dex）载体，可在类风湿性关节炎（RA）中实现持续的抗炎作用。通过径向排列的介孔和表面功能实现了高容量负载和目标药物的持续释放。最大负载效率经证实约为76 wt%，约为代表性介孔二氧化硅SBA - 15的两倍。此外，负载地塞米松的RMSNs在体外100小时内可实现约92%负载地塞米松的持续释放曲线，在此期间地塞米松的递送效率比SBA - 15高2.3倍。在RA疾病大鼠模型中对炎症抑制作用的体内评估表明，与对照组相比，用负载地塞米松的RMSNs治疗的组在8周内持续具有显著的抗炎作用和软骨恢复。通过微型计算机断层扫描、骨密度测量和改良的曼金评分证实了体内效果。所提出的负载地塞米松的RMSNs延长了治疗剂在体内的浓度寿命并使其效果最大化，这应会促进其应用。
