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Objectives The aim of this study was to evaluate the cytotoxicity of self‐emulsifying drug delivery systems (SEDDS) containing five different cationic surfactants. Methods Cationic surfactants were added in a concentration of 1% and 5% (m/m) to SEDDS comprising 30% Capmul MCM, 30% Captex 355, 30% Cremophor EL and 10% propylene glycol. The resulting formulations were characterized in terms of size, zeta potential, in‐vitro haemolytic activity and toxicity on Caco‐2 via MTT assay and lactate dehydrogenase release assay. Key findings The evaluated surfactants had in both concentrations a minor impact on the size of SEDDS ranging from 30.2 ± 0.6 to 55.4 ± 1.1 nm, whereas zeta potential changed significantly from −9.0 ± 0.3 to +28.8 ± 1.6 mV. The overall cytotoxicity of cationic surfactants followed the rank order: hexadecylpyridinium chloride > benzalkonium chloride > alkyltrimethylammonium bromide > octylamine > 1‐decyl‐3‐methylimidazolium. The haemolytic activity of the combination of cationic surfactants and SEDDS on human red blood cells was synergistic. Furthermore, cationic SEDDS exhibited higher cytotoxicity of Caco‐2 cells compared to SEDDS without cationic surfactants. Conclusions According to these results, SEDDS and cationic surfactants seem to bear an additive up to synergistic toxic risk.

The results of this study suggest that the developed SEDDS could be considered for oral opioid peptide delivery.