Effects of buffer pH and phosphate concentration on the droplet size and EYP hydrolysis of perflubron/EYP emulsions.
Oil-in-water emulsions containing perflubron (perfluorooctyl bromide; PFOB) and stabilized with egg yolk phospholipid (EYP) have potential applications as contrast agents and oxygen carriers. In this study, the effects of buffer pH and total phosphate concentration on the emulsion droplet size and EYP hydrolysis were evaluated. 90% w/v perflubron emulsions with NaH2PO4-Na2HPO4 buffers of different pH (4.7-8.7) and phosphate concentrations (30 and 60 mM) were prepared with a high-pressure homogenizer. Emulsions were stored at 40 degrees C and tested at 0, 1, 2 and 3 months. The pH dropped quickly in emulsions with pH 8.7 buffer whereas acidic and neutral buffered emulsions exhibited minor pH drops. The concentration of free fatty acids (FFA) vs emulsion pH can be fitted to a parabolic curve with a minimum at about pH 6.0. The droplet growth rates in emulsions with the pH 4.7 buffer were about 2.5 times of those in emulsions with the pH 8.7 buffer. Total phosphate concentration had only a minor effect. This study emphasizes the importance of the careful selection of buffer pH and capacity to control EYP hydrolysis and possibly emulsion droplet size.
Alliance Pharmaceutical Corp., San Diego, California 92121.
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D002021:Buffers; D003287:Contrast Media; D004530:Egg Yolk / Q000737:chemistry*; D004655:Emulsions; D005230:Fatty Acids, Nonesterified / Q000032:analysis; D005466:Fluorocarbons / Q000737:chemistry*; D006842:Hydrocarbons, Brominated; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D010316:Particle Size; D010710:Phosphates / Q000032:analysis*; D010743:Phospholipids / Q000737:chemistry*
D002021:Buffers; D003287:Contrast Media; D004655:Emulsions; D005230:Fatty Acids, Nonesterified; D005466:Fluorocarbons; D006842:Hydrocarbons, Brominated; D010710:Phosphates; D010743:Phospholipids; C003072:perflubron