Preparation of cupric sulfate-based self-emulsifiable nanocomposites and their application to the photothermal therapy of colon adenocarcinoma.

Abstract Nanocomposites (NCs) of cupric sulfate monohydrate (CuSO 4 ) were fabricated by hot-melt extrusion (HME) system equipped with twin screws. Micron-sized bulk powder of CuSO 4 was dispersed in the mixture of surfactants (Span 80 and Tween 80) and hydrophilic polymer (polyethylene glycol (PEG) 6000) by HME process. Reduction of surface tension by surfactants and homogeneous dispersion in hydrophilic polymer along with HME technique were introduced to prepare CuSO 4 NCs. Dispersion of CuSO 4 NCs exhibited approximately 204 nm hydrodynamic size, unimodal size distribution, and positive zeta potential values. Encapsulation of CuSO 4 in CuSO 4 NCs and the physicochemical interactions between CuSO 4 and pharmaceutical excipients were investigated by solid-state studies. Of note, CuSO 4 NCs group exhibited higher antiproliferation efficacies, compared with bulk CuSO 4 , in Caco-2 (human adenocarcinoma) cells at 75 and 100 μg/mL CuSO 4 concentrations ( p < 0.05). Also, near-infrared laser irradiation to CuSO 4 NCs group elevated the antiproliferation efficacies, compared with non-irradiation group, in Caco-2 cells. After intravenous injection in mice, CuSO 4 NCs did not show severe in vivo toxicities. Developed CuSO 4 NCs can be one of promising candidates of photothermal therapeutic agents for colon cancers. Highlights • CuSO 4 nanocomposites (NCs) were fabricated by hot-melt extrusion method. • Dispersion of CuSO 4 in NCs was identified by several solid-state studies. • CuSO 4 NCs exhibited improved photothermal therapeutic efficacies in Caco-2 cells. [ABSTRACT FROM AUTHOR]