Development of a solid dispersion system for polyvinyl alcohol nanofibers embedded with silicon dioxide particles via emulsion electrospinning for improved solubility of poorly water-soluble drugs

聚乙烯醇 乳状液 静电纺丝 纳米纤维 材料科学 溶解度 二氧化硅 色散(光学) 化学工程 复合材料 聚合物 有机化学 化学 物理 光学 工程类
作者
Ayaka Miki,Kouji Hara,Takato Shibata,T. Morioka,Ayaka Kobayashi,Nobuyoshi Yoshimura,Eriko Yamazoe,Takaaki Ito,Kohei Tahara
出处
期刊:Journal of Drug Delivery Science and Technology [Elsevier]
卷期号:99: 105915-105915
标识
DOI:10.1016/j.jddst.2024.105915
摘要

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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