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用于提高溶出度的熔喷和电纺载药聚合物纤维垫:一项比较研究。

Melt-blown and electrospun drug-loaded polymer fiber mats for dissolution enhancement: a comparative study.

作者信息

Balogh Attila, Farkas Balázs, Faragó Kornél, Farkas Attila, Wagner István, Van Assche Ivo, Verreck Geert, Nagy Zsombor K, Marosi György

机构信息

Budapest University of Technology and Economics, Organic Chemistry and Technology Department, Budapest, H-1111, Hungary.

出版信息

J Pharm Sci. 2015 May;104(5):1767-76. doi: 10.1002/jps.24399. Epub 2015 Mar 11.

Abstract

Melt blowing (MB) was investigated to prepare a fast dissolving fibrous drug-loaded solid dispersion and compared with solvent-based electrospinning (SES) and melt electrospinning (MES). As a conventional solvent-free technique coupled with melt extrusion and using a high-speed gas stream, MB can provide high-quality micro- and nanofibers at industrial throughput levels. Carvedilol, a weak-base model drug with poor water solubility, was processed using a common composition optimized for the fiber spinning and blowing methods based on a hydrophilic vinylpyrrolidone-vinyl acetate copolymer (PVPVA64) and PEG 3000 plasticizer. Scanning electron microscopy combined with fiber diameter analysis showed diameter distributions characteristic to each prepared fibrous fabrics (the mean value increased toward SES<MB<MES). Differential scanning calorimetry and X-ray diffraction studies revealed that the incorporated drug was in amorphous form regardless the preparation method. The HPLC studies demonstrated that all of the materials produced by the different techniques passed the regulatory purity requirements. The fibers exhibited ultrafast drug release tested under neutral pH conditions; the melt-blown sample dissolved within 2 min owing to its large specific surface area. The presented results confirm the applicability of MB as a novel formulation technique for polymer-based drug delivery systems.

摘要

研究了熔喷法(MB)制备快速溶解的载药纤维状固体分散体,并与溶剂型电纺丝(SES)和熔体电纺丝(MES)进行了比较。作为一种与熔融挤出相结合的传统无溶剂技术,并使用高速气流,MB可以在工业生产水平上提供高质量的微纤维和纳米纤维。卡维地洛是一种水溶性差的弱碱性模型药物,使用基于亲水性乙烯基吡咯烷酮-醋酸乙烯酯共聚物(PVPVA64)和PEG 3000增塑剂的、针对纤维纺丝和吹塑方法优化的常见组合物进行加工。扫描电子显微镜结合纤维直径分析显示了每种制备的纤维织物的直径分布特征(平均值向SES<MB<MES方向增加)。差示扫描量热法和X射线衍射研究表明,无论制备方法如何,掺入的药物均为无定形形式。HPLC研究表明,不同技术制备的所有材料均符合监管纯度要求。在中性pH条件下测试,纤维表现出超快的药物释放;熔喷样品由于其大的比表面积在2分钟内溶解。所呈现的结果证实了MB作为基于聚合物的药物递送系统的新型制剂技术的适用性。

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