The influence of alkali fatty acids on the properties and the stability of parenteral O/W emulsions modified with Solutol HS 15

• Published in: European journal of pharmaceutics and biopharmaceutics 2000-03, Vol.49 (2), p.143-149
• Main Authors: Buszello, K, Harnisch, S, Müller, R.H, Müller, B.W
• Format: Article
• Language: English
• Subjects: Adsorption; Alkali fatty acid; Biological and medical sciences; Blood Proteins - chemistry; Drug Stability; Emulsions - chemistry; General pharmacology; Hydrogen-Ion Concentration; Lauric Acids - pharmacology; Medical sciences; O/W emulsion; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Phosphatidylcholines - administration & dosage; Plasma protein adsorption; Polyethylene Glycols - pharmacology; Solutol HS 15; Stearates - pharmacology; Stearic Acids - pharmacology; Surface-Active Agents - pharmacology
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/S0939-6411(99)00081-8

Arachis oil based parenteral O/W emulsions were prepared using soya bean phosphatidylcholine (SPC) and different combinations of co-emulsifiers containing polyethylene glycol fatty acid esters (Solutol HS 15 ®) and alkali fatty acids (sodium laurate, sodium stearate). The parameters measured were droplet size (both by photon correlation spectroscopy and laser diffractometry), pH and zeta potential. All emulsions were subjected to autoclaving. The addition of polyethylene glycol 12-hydroxy stearate (Solutol HS 15 ®) led to a significant decrease of mean oil droplet size. For long-term stability the amount added turned out to be the most important factor. With increased amounts of Solutol HS 15 ® the packing density of the emulsifier layer and the zeta potential decreased leading to instability. The optimum load of Solutol HS 15 ® was found to be 15 μmol/ml. Alkali fatty acids markedly improved the physical stability of the emulsions. Improved stability properties conferred to emulsions by alkali fatty acids could be attributed to the zeta potential increase even in the presence of Solutol HS 15 ®. Consequently a mixed emulsifier film was established in which the ionized fatty acids determined the interface charge. In addition to this a strengthening of the molecular interactions occurring between phospholipid and Solutol HS 15 ® emulsifier in the presence of ionized fatty acids at the O/W interface can be assumed (L. Rydhag, The importance of the phase behaviour of phospholipids for emulsion stability, Fette Seifen Anstrichm. 81 (1979) 168–173). Different co-emulsifier mixtures were shown to have a pronounced impact on the plasma protein adsorption onto emulsion droplets.