Enhanced solubility and controlled release of probucol using electrospun nanofibers prepared with different pharmaceutical polymers.

Abstract

We aimed to improve the water solubility and control the release of probucol using electrospinning technology. The effects of multiple polymer matrices and surfactants on the water solubility of probucol were evaluated. Probucol-loaded nanofibers were prepared using four polymers: polyvinylacetal diethylaminoacetate (AEA), methacrylic acid/ethyl acrylate (1/1) copolymer (Kollicoat MAE), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG, Soluplus), and polyvinylpyrrolidone (PVP). Each polymer exhibited different solubility characteristics, and optimal manufacturing conditions were determined. Probucol was in an amorphous state within the nanofibers. The pH-sensitive polymers, including AEA and MAE, enhanced probucol solubility, enabling controlled release in response to pH changes. Additionally, incorporating the surfactants, Tween 80 and Span 20, improved the wettability of Soluplus nanofibers, further enhancing probucol solubility. The addition of surfactants reduced the fiber diameter of the nanofibers, increased the initial dissolution rate, and approximately doubled the drug release rate after 24 h. These findings indicate that the choice of polymer matrix and surfactant is critical for improving solubility and controlling the release of drugs with poor water solubility in electrospun nanofiber solid dispersions. These results provide valuable insights for the development of nanofiber formulations.