当前位置: X-MOL 学术AMB Express › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Rhein laden pH-responsive polymeric nanoparticles for treatment of osteoarthritis.
AMB Express ( IF 3.7 ) Pub Date : 2020-08-31 , DOI: 10.1186/s13568-020-01095-3
Bo Hu 1, 2 , Feng Gao 2, 3 , Chunbao Li 2 , Boqing Zhang 2 , Mingyang An 2 , Ming Lu 2 , Yufeng Liu 2 , Yujie Liu 2
Affiliation  

Osteoarthritis (OA) is a condition associated with severe inflammation, cartilage destruction and degeneration of joints. Rhein (Rh) is an effective anti-inflammatory drug with proven efficacy in in-vitro and in-vivo models. pH sensitive Rh and NH4HCO3 laden poly (lactic-co-glycolic acid (PLGA) nanoparticles (NPs) (Rh-PLGA-NPs@NH4) are developed for an effective treatment of OA. The Rh-PLGA-NPs@NH4 are prepared along with Rh-PLGA-NPs as a control by double emulsion method. Rh-PLGA-NPs@NH4 was characterized for their size, shape, morphology and encapsulation efficiency (EE). The effect of pH on release of Rh from Rh-PLGA-NPs@NH4 was studied at different pH. Further, the cytotoxicity effect of Rh-PLGA-NPs@NH4 on THP-1 cells were evaluated. Anti-inflammatory efficacy was evaluated on LPS stimulated THP-1 cells and the release of pro-inflammatory cytokines was evaluated and compared with control. The size of Rh-PLGA-NPs@NH4 and Rh-PLGA-NPs was found to be 190.7 ± 1.2 nm and 134.6 ± 2.4 nm respectively with poly dispersity (PDI) 0.14 and 0.15. The zeta potential of Rh-PLGA-NPs@NH4 was found to be -22 ± 1.12 mV. Rh-PLGA-NPs@NH4 were uniform, smooth and spherical shape as confirmed using electron microscopy analysis. Rh-PLGA-NPs@NH4 release the Rh more effectively in the low pH of synovial fluid environment (SFE). Rh-PLGA-NPs@NH4 also significantly affect inflammatory cytokines TNF-α and IL-1β and reduced their release in LPS stimulated THP-1 cells. Reactive oxygen species (ROS), a mediator responsible for the cartilage collapse was also found to be reduced. Results proposes that Rh-PLGA-NPs could provide therapeutic solution to those patients who suffer from chronic joint ailments by reducing the progression of OA.

中文翻译:

大黄酸负载的pH响应性聚合物纳米颗粒,用于治疗骨关节炎。

骨关节炎(OA)是与严重炎症,软骨破坏和关节退化相关的疾病。大黄酸(Rh)是一种有效的抗炎药,在体外和体内模型中均证明具有疗效。pH敏感的Rh和NH 4 HCO 3负载的聚乳酸-乙醇酸(PLGA)纳米颗粒(NPs)(Rh-PLGA-NPs @ NH 4)用于有效治疗OA。通过双乳化法制备了NH 4和作为对照的Rh-PLGA-NPs,对Rh-PLGA-NPs @ NH 4的大小,形状,形态和包封率(EE)进行了表征,pH对释放量的影响。来自Rh-PLGA-NPs @ NH 4的Rh在不同的pH下进行了研究。此外,评价了Rh-PLGA-NPs @ NH 4对THP-1细胞的细胞毒性作用。在LPS刺激的THP-1细胞上评估抗炎功效,并评估促炎细胞因子的释放并将其与对照进行比较。发现Rh-PLGA-NPs @ NH 4和Rh-PLGA-NPs的大小分别为190.7±1.2 nm和134.6±2.4 nm,多分散度(PDI)为0.14和0.15。发现Rh-PLGA-NPs @ NH 4的ζ电势为-22±1.12mV。用电子显微镜分析证实,Rh-PLGA-NPs @ NH 4是均匀,光滑和球形的。Rh-PLGA-NPs @ NH 4在滑液环境(SFE)的低pH中更有效地释放Rh。Rh-PLGA-NPs @ NH4还显着影响炎性细胞因子TNF-α和IL-1β,并降低了它们在LPS刺激的THP-1细胞中的释放。活性氧(ROS),负责软骨崩溃的介体也被发现减少。结果表明,Rh-PLGA-NPs可以通过减少OA的发展为慢性关节疾病患者提供治疗解决方案。
更新日期:2020-08-31
down
wechat
bug