Abstract

This study explored the development of solid dispersions of probucol (PBC), a poorly water-soluble drug, embedded within polyvinyl alcohol (PVA) nanofibers at a high concentration (30 %) via emulsion electrospinning. This study addressed the issues of low solubility and dissolution rates of such drugs by examining the incorporation of various types of silica particles—Aerosil 200 (A200), Sylisia 320 (SY320), Aerosil R972, and Sylophobic 100—as additives in oil-in-water emulsions. The results revealed that regardless of their hydrophilic or hydrophobic properties, silica particles preserved the amorphous state of PBC within the nanofibers without altering its crystallinity. Notably, all nanofibers embedded with silica particles demonstrated improved drug solubility compared to those without silica. This suggests that silica plays a role in mitigating the reduced solubility of drugs associated with their higher concentrations. Stability assessments of nanofibers embedded with A200 and SY320 under accelerated conditions revealed that A200 nanofibers preserved drug crystallinity and solubility, thus exhibiting superior storage stability. In contrast, SY320 nanofibers underwent drug crystallization, leading to a decrease in solubility upon storage. In conclusion, this study highlights the potential of silica particles in enhancing the solubility and stability of PBC in PVA nanofibers, suggesting that emulsion electrospinning with suitable silica additives is an effective strategy for developing advanced drug delivery systems for poorly water-soluble drugs.

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