Melt-Blown and Electrospun Drug-Loaded Polymer Fiber Mats for Dissolution Enhancement: A Comparative Study

被引:60
作者
Balogh, Attila [1 ]
Farkas, Balazs [1 ]
Farago, Kornel [1 ]
Farkas, Attila [1 ]
Wagner, Istvan [1 ]
Van Assche, Ivo [2 ]
Verreck, Geert [2 ]
Nagy, Zsombor K. [1 ]
Marosi, Gyoergy [1 ]
机构
[1] Budapest Univ Technol & Econ, Organ Chem & Technol Dept, H-1111 Budapest, Hungary
[2] Janssen Pharmaceut, Chem & Pharmaceut Dev, Johnson & Johnson Pharmaceut Res & Dev, B-2340 Beerse, Belgium
关键词
electrospinning; melt electrospinning; melt blowing; extrusion; oral drug delivery; solid dispersion; enhanced dissolution rate; continuous pharmaceutical manufacturing; viscosity; HPLC; RELEASE; DEGRADATION; NANOFIBERS; CARVEDILOL; STABILITY; SECRETION; MEMBRANES; DELIVERY; BEHAVIOR;
D O I
10.1002/jps.24399
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (c) 2015 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:1767-1776, 2015
引用
收藏
页码:1767 / 1776
页数:10
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