Melt-electrospinning: a novel method for formulating and improving the solubility of poorly water-soluble drugs

摘要

BACKGROUND: Solution or melt electrospinning (MES) are effective methods for fabricating nano-or micro-scale drug delivery systems (DDSs), or scaffolds for biomedical applications. Formulation of melt electrospun fibrous solid dispersions is a novel approach to improve the solubility of poorly water-soluble drugsl. The combination of several factors related to the process (amorphization, stabilization and void of any solvents) makes MES an attracking tool to be investigated to address poorly soluble drugs.AIMS: The objective of this study was to prepare and characterize DDSs fabricated by MES using in-domethacin (IND) as a model drug, and polyvinylpyrrolidone (PVP)/Soluplus (SOL)/xylitol (XYL) as carriers. Moreover, the effects of formulation on the dissolution behavior of IND was investigated.RESULTS: Melt spun fibers (MSFs) were successfully prepared and analyzed using XRPD, FTIR, DSC and SEM. The dissolution studies were carrier out at pH 6.8. Solid-state characterization confirmed the presence of amorphous IND. The dissolution (drug release) from MSFs was superior compared to that obtained with pure crystalline IND alone, or with the corresponding physical mixtures (PMs).CONCLUSIONS: The results demonstrate that MES can be used as an effective tool for fabricating micro-scale fibers (fibrous solid dispersions) for poorly-water soluble drugs. The dissolution rate of IND can be significantly improved compared to that of pure drug and PMs.