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  • Title: Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity?
    Author: Lam HT, Le-Vinh B, Phan TNQ, Bernkop-Schnürch A.
    Journal: J Pharm Pharmacol; 2019 Feb; 71(2):156-166. PubMed ID: 30251762.
    Abstract:
    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.
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