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首页> 外文期刊>Journal of pharmaceutical sciences. >Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems
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Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems

机译：无溶剂熔体静电纺丝，用于制备快速溶解的药物输送系统，并与基于溶剂的电纺丝和熔体挤出系统进行比较

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The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit? E type was used as a fiber forming polymer matrix. For comparison, ethanol-based electrospinning and melt extrusion (EX) methods were used to produce samples that had the same composition as the melt electrospun system. According to the results of scanning electron microscopy, X-ray diffraction, differential scanning calorimetry, and Fourier transformed infrared spectrometry investigations, amorphous solid nanodispersions/solutions of CAR in Eudragit? E matrix were obtained in all cases with 20 m/m% drug content. In vitro drug release in acidic media from the extrudates was significantly faster (5 min) than that from crystalline CAR. Moreover, ultrafast drug release was achieved from the solvent-free melt and ethanol-based electrospun samples because of their huge surface area and the soluble polymer matrix in the acidic media. These results demonstrate that solvent-free MES is a promising, novel technique for the production of drug delivery systems with enhanced dissolution because it can combine the advantages of EX (e.g., solvent-free, continuous process, and effective amorphization) and solvent-based electrospinning (huge product surface area).
机译：开发了无溶剂熔融静电纺丝（MES）方法，以制备具有快速释放的卡维地洛（CAR）（水溶性差的药物）的药物递送系统。据作者所知，这是制备载有药物的熔融电纺纤维的第一份报告。 Eudragit的阳离子甲基丙烯酸酯共聚物？ E型用作形成纤维的聚合物基质。为了进行比较，使用基于乙醇的静电纺丝和熔融挤出（EX）方法来生产具有与熔融电纺丝系统相同组成的样品。根据扫描电子显微镜，X射线衍射，差示扫描量热法和傅立叶变换红外光谱研究的结果，Eudragit？中CAR的无定形固体纳米分散体/溶液？在所有情况下均获得药物含量为20 m / m％的E基质。挤出物中在酸性介质中的体外药物释放（5分钟）明显快于结晶CAR。此外，由于无溶剂熔体和乙醇基电纺丝样品具有巨大的表面积和在酸性介质中的可溶性聚合物基质，因此可以实现超快的药物释放。这些结果表明，无溶剂MES是生产具有增强溶解性的药物递送系统的有前途的新颖技术，因为它可以结合EX的优势（例如，无溶剂，连续过程和有效的无定形性）和基于溶剂的静电纺丝（巨大的产品表面积）。

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