A pH-responsive mesoporous silica nanoparticles-based drug delivery system with controlled release of andrographolide for OA treatment.
A pH-responsive mesoporous silica nanoparticles-based drug delivery system with controlled release of andrographolide for OA treatment.
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DOI：
10.1093/rb/rbab020
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发表时间：
2021-08
影响因子：
6.7
通讯作者：
Zheng L
中科院分区：
文献类型：
--
作者：
He M;Qin Z;Liang X;He X;Zhu B;Lu Z;Wei Q;Zheng L
穿心莲具有良好的抗炎和抗氧化作用。然而，由于高亲脂性，其生物利用度低，并且在关节内注射后可以容易地被滑液清除，导致骨关节炎（OA）的治疗效率低。本研究采用pH响应性聚丙烯酸（PAA）修饰介孔二氧化硅纳米粒子（MSNs），将AG负载到MSNs-PAA纳米平台上，构建了一种用于OA治疗的纳米pH响应性药物递送系统（DDS）。纳米粒粒径均一（约120 nm），载药率高（22.38 ± 0.71%），具有pH响应性，有利于在OA环境中的缓释。与AG相比，AG@MSNs-PAA在IL-1β刺激的软骨细胞和前交叉韧带横断诱导的大鼠OA模型上显示出更强的抗关节炎疗效和软骨保护能力，表现为更低的炎性因子表达和更好的蛋白多糖损失预防。因此，AG@MSNs-PAA纳米平台可以被开发为有前途的OA特异性和按需DDS。
Andrographolide (AG) has favorable anti-inflammatory and antioxidative capacity. However, it has low bioavailability due to high lipophilicity and can be easily cleared by the synovial fluid after intra-articular injection, leading to low therapeutic efficiency in osteoarthritis (OA). Herein, we designed a nano-sized pH-responsive drug delivery system (DDS) for OA treatment by using modified mesoporous silica nanoparticles (MSNs) with pH-responsive polyacrylic acid (PAA) for loading of AG to form AG@MSNs-PAA nanoplatform. The nanoparticles have uniform size (∼120 nm), high drug loading efficiency (22.38 ± 0.71%) and pH-responsive properties, beneficial to sustained release in OA environment. Compared with AG, AG@MSNs-PAA showed enhanced antiarthritic efficacy and chondro-protective capacity based on IL-1β-stimulated chondrocytes and anterior cruciate ligament transection-induced rat OA model, as demonstrated by lower expression of inflammatory factors and better prevention of proteoglycan loss. Therefore, the AG@MSNs-PAA nanoplatform may be developed as a promising OA-specific and on-demand DDS.
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