Electrospun Nimodipine-loaded fibers for nerve regeneration: development and in vitro performance.
Electrospun Nimodipine-loaded fibers for nerve regeneration: development and in vitro performance.
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DOI：
10.1016/j.ejpb.2020.03.021
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发表时间：
2020-04
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通讯作者：
Johanna Zech;S. Leisz;Benedikt Göttel;F. Syrowatka;A. Greiner;C. Strauss;W. Knolle;C. Scheller;K. Mäder
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文献类型：
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作者：
Johanna Zech;S. Leisz;Benedikt Göttel;F. Syrowatka;A. Greiner;C. Strauss;W. Knolle;C. Scheller;K. Mäder
尼莫地平是一种1，4-二氢吡啶类钙拮抗剂，常规用于控制血压和降低蛛网膜下腔出血后继发性缺血的风险。此外，尼莫地平具有独特的神经保护特性。对于脑相关应用，由于全身副作用，全身给药后通常不能实现所需局部作用的全部潜力。因此，我们的目标是开发一种可生物降解的药物释放系统，作为一个合适的和可生物降解的系统，我们成功地静电纺丝PLGA纤维含有1和10%的药物。DSC和X-射线衍射分析结果表明尼莫地平以非晶态的形式存在于聚合物基体中。长达6个月未检测到药物重结晶。尝试了电子束灭菌，但大大减少了纤维垫的药物含量。尼莫地平纤维毡的药物缓释时间可达4-8天，药物的缓释依赖于释放条件，无细胞毒性。相比之下，静电纺丝纤维能够显着减少细胞死亡在体外细胞模型中的氧化，渗透和热诱导的细胞应激在雪旺细胞，神经元细胞以及永生化和初级星形胶质细胞。因此，静电纺丝尼莫地平负载PLGA纤维代表了一种有前途的药物递送系统，以实现其颅内使用的药物益处。
Nimodipine is a 1,4-Dihydropyridine type calcium antagonist routinely used to control blood pressure and reduce the risk of secondary ischemia after aneurismal subarachnoid hemorrhage. Additionally, Nimodipine has unique neuroprotective properties. With respect to brain related applications, the full potential of the desired local effect can often not be realized after systemic administration due to systemic side effects. Therefore, it was our aim to develop a biodegradable drug delivery system for the local controlled release of the drug inside the brain.As a suitable and biodegradable system we successfully electrospun PLGA fibers containing 1 and 10% drug. The results of DSC and X-Ray diffractometry measurements indicate that Nimodipine was incorporated in the polymer matrix in the amorphous state. No drug recrystallization was detected for up to 6 months. Electron-beam sterilization was tried but reduced the drug content of the fiber mats considerably. A sustained drug release over 4–8 days was observed, highly depended on release conditions.The Nimodipine fiber mats exhibited no cell toxicity. In contrast, the electrospun fibers were able to significantly reduce cell death inin vitrocell models of oxidative, osmotic and heat-induced cell stress in Schwann cells, neuronal cells as well as immortalized and primary astrocytes. Therefore, electrospun Nimodipine loaded PLGA fibers represent a promising drug delivery system to realize the druǵs benefits for its intracranial use.