Bitay Enikő, Gergely Attila Levente, Szabó Zoltán-István
Department of Mechanical Engineering, Faculty of Technical and Human Sciences, Sapientia Hungarian University of Transylvania, Calea Sighișoarei nr. 2., 540485 Târgu-Mureş, Romania.
Research Institute of the Transylvanian Museum Society, 2-4 Napoca, 400009 Cluj, Romania.
Pharmaceutics. 2023 Aug 31;15(9):2256. doi: 10.3390/pharmaceutics15092256.
Aceclofenac-loaded polyvinylpyrrolidone fiber-based amorphous solid dispersion was produced successfully by centrifugal spinning. The solution concentration and rotational speed were optimized to produce the fiber-based drug carrier system, with a determined production rate of 12.7 g/h dry solid fibers. The obtained fibers were bead-free and smooth-surfaced with an average diameter of 7.5 ± 2.5 μm. Gas chromatographic determinations revealed that ethanol, as a residual solvent, was well below the regulatory limit of 0.5%. Differential scanning calorimetric investigation and infrared spectroscopic measurements were used to track the physicochemical changes that intervene during fiber formation in the solid state. The results revealed that the rapid evaporation of the solvent was accompanied by a probable crystalline to amorphous transition of the active substance during centrifugal spinning. In vitro dissolution studies revealed an instantaneous disintegration of the fibrous structure and a rapid release of the active substance, with the microfibrous webs greatly outperforming the crystalline active substance, especially in the early time-points. This implies that centrifugal spinning offers a viable scale-up production process to prepare drug-loaded fiber-based solid dispersions.
通过离心纺丝成功制备了载醋氯芬酸的聚乙烯吡咯烷酮纤维基无定形固体分散体。对溶液浓度和转速进行了优化，以制备纤维基药物载体系统，确定的干固体纤维生产速率为12.7 g/h。所获得的纤维无珠且表面光滑，平均直径为7.5±2.5μm。气相色谱测定表明，作为残留溶剂的乙醇远低于0.5%的监管限度。采用差示扫描量热法研究和红外光谱测量来追踪固态纤维形成过程中发生的物理化学变化。结果表明，在离心纺丝过程中，溶剂的快速蒸发伴随着活性物质可能从结晶态向无定形态的转变。体外溶出度研究表明，纤维结构瞬间崩解，活性物质快速释放，微纤维网的性能大大优于结晶态活性物质，尤其是在早期时间点。这意味着离心纺丝为制备载药纤维基固体分散体提供了一种可行的放大生产工艺。
