Center for Stem Cell and Tissue Engineering, School of Medicine, Zhejiang University, Hangzhou, China; Zhejiang Provincial Key Laboratory of Tissue Engineering and Regenerative Medicine, Hangzhou, China.
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
Biomaterials. 2014 Aug;35(24):6585-94. doi: 10.1016/j.biomaterials.2014.04.042. Epub 2014 May 5.
The cell-cycle inhibitor flavopiridol has been shown to improve recovery from spinal cord injury in animal models. However, the systemic dose of flavopiridol has side-effects and the mechanism of action is not clear. This study aimed to develop a strategy for the local delivery of flavopiridol and investigate its mechanisms of action. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) were used for the sustained delivery of flavopiridol. The spinal cord was right-hemisectioned and NPs were delivered into the injury site. Transparent spinal cord technology was used for the three-dimensional observation of anterograde tracing. The results showed that flavopiridol NPs had a sustained release of up to 3 days in vitro. Flavopiridol NPs significantly decreased inflammatory factor synthesis by astrocytes, including TNF-α, IL-1β, and IL-6, while the IL-10 expression was elevated. In vivo study demonstrated that flavopiridol NPs decreased cell-cycle activation, inflammatory expression and glial scarring, and facilitated neuronal survival and regeneration. The cavitation volume was decreased by ~90%. Administration of flavopiridol NPs also improved the motor recovery of injured animals. These findings demonstrated that local delivery of flavopiridol in PLGA NPs improves recovery from spinal cord injury by inhibiting astrocyte growth and inflammatory factor synthesis.
细胞周期抑制剂 flavopiridol 已被证明可改善动物模型中的脊髓损伤恢复。然而,flavopiridol 的全身剂量有副作用,其作用机制尚不清楚。本研究旨在开发 flavopiridol 的局部递送策略,并研究其作用机制。聚(乳酸-共-乙醇酸)(PLGA)纳米颗粒(NPs)用于 flavopiridol 的持续递送。将 NPs 递送至脊髓半切损伤部位。采用透明脊髓技术对顺行示踪进行三维观察。结果表明,flavopiridol NPs 在体外具有长达 3 天的持续释放。Flavopiridol NPs 显著降低了星形胶质细胞合成的炎症因子,包括 TNF-α、IL-1β 和 IL-6,同时升高了 IL-10 的表达。体内研究表明,flavopiridol NPs 减少了细胞周期激活、炎症表达和神经胶质瘢痕形成,促进了神经元存活和再生。空洞体积减少了约 90%。Flavopiridol NPs 的给药还改善了受伤动物的运动恢复。这些发现表明,PLGA NPs 中 flavopiridol 的局部递送通过抑制星形胶质细胞生长和炎症因子合成来改善脊髓损伤的恢复。