Development of iron(II) sulfate nanoparticles produced by hot-melt extrusion and their therapeutic potentials for colon cancer

• Published in: International journal of pharmaceutics 2019-03, Vol.558, p.388-395
• Main Authors: Koo, Ja Seong, Lee, Song Yi, Azad, Md Obyedul Kalam, Kim, Minju, Hwang, Sung Jun, Nam, Suyeong, Kim, Sungyun, Chae, Byung-Jo, Kang, Wie-Soo, Cho, Hyun-Jong
• Format: Article
• Language: English
• Subjects: Antiproliferation; Apoptosis; Caco-2 cell; Hot-melt extrusion; Iron(II) sulfate; Nanoparticle
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2019.01.018

[Display omitted] Particle size reduction of FeSO4 (iron(II) sulfate, IS) from micron to nano size was achieved by a combination of hot-melt extrusion (HME) processing and the input of Span 80, Tween 80, and poly(ethylene glycol) (PEG) 6000. Conveying, kneading, and extruding steps of the HME process and a decrease in the surface tension by surfactants were introduced to produce FeSO4 nanoparticles (NPs) in an aqueous environment. The FeSO4-based NPs (ISNPs) in the dispersion were composed of FeSO4, Span 80, Tween 80, and PEG 6000 and displayed a hydrodynamic size of 350–400 nm (5–50 mg/mL ISNPs concentration range) and a spherical shape. Considering the feeding ratio of FeSO4 (20%, w/w) used for preparing the ISNPs, FeSO4 appears to be wrapped by Span 80, Tween 80, and PEG 6000 according to the results of X-ray photoelectron spectroscopy (XPS) analysis. ISNPs exhibited different thermodynamic properties from those of FeSO4 itself. In colon adenocarcinoma (Caco-2) cells, the ISNPs group exhibited enhanced antiproliferation and apoptosis potentials compared to the FeSO4 group (p