Abstract

We report in this work coaxial electrospun fibers with potential applications in the treatment of Parkinson’s disease. The fibers comprise a fixed dose combination (FDC) containing the active ingredients levodopa and carbidopa, loaded in a fast dissolving polyvinylpyrrolidone (PVP) shell and an insoluble but swellable Eudragit^® RLPO core. Under appropriate processing conditions we are able to prepare fibers with distinct core/shell architectures and diameters of approximately 400 nm. X-ray diffraction and differential scanning calorimetry analyses revealed that the drugs are dispersed on the molecular level within the polymer carriers, and IR spectroscopy indicated the presence of intermolecular interactions. At pH 1, the composite fibers yields extended release over more than 8 h, with an initial loading dose being freed from the PVP shell and then a sustained release phase following from the insoluble core. This is markedly extended over the release period of the commercial FDC product, and thus the fibers generated here have the potential to be used to reduce the required dosing frequency.

Graphic Abstract

中文翻译：

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静电纺丝左旋多巴-卡比多巴固定剂量组合的制备

摘要

我们在这项工作中报告了同轴电纺纤维在治疗帕金森氏病方面的潜在应用。所述纤维包括含有活性成分左旋多巴和卡比多巴，在快速溶解的聚乙烯吡咯烷酮（PVP）壳和不溶性但可溶胀的Eudragit加载的固定剂量组合（FDC）^®RLPO核心。在适当的加工条件下，我们能够制备具有独特的核/壳结构和直径约为400 nm的纤维。X射线衍射和差示扫描量热法分析显示药物分散在聚合物载体内的分子水平上，红外光谱表明存在分子间相互作用。在pH值为1时，复合纤维的释放时间超过8小时，PVP外壳释放了最初的加载剂量，随后不溶核释放出了持续释放阶段。这在商用FDC产品的释放期内显着延长，因此，此处生成的纤维具有用于减少所需加药频率的潜力。

图形摘要