Physicochemical characterization of parenteral lipid emulsion: influence of cosurfactants on flocculation and coalescence.
OBJECTIVE
The stability of lipid emulsions (LE) containing various cosurfactants (oleic acid, cholesterol, Tween 80, or HCO-60) was evaluated using the maximum total interaction energy, Vtmax and the energy barrier for coalescence, W.


METHODS
The Vtmax and W were calculated from the zeta potential and the rate of increase in LE particle size, respectively.


RESULTS
The Vtmax and W of LE containing the oleic acid were 0.598 x 10(-19) J and 3.03 x 10(-19) J, respectively, while those of LE without the cosurfactant were 0.141 x 10(-19) J and 1.36 x 10(-19) J.


CONCLUSIONS
These findings suggest that oleic acid prevents the flocculation and coalescence of LE. The Vtmax and W of LE containing the cholesterol were 0.435 x 10(-19) J and 0.63 x 10(-19) J, respectively, suggesting that the cholesterol prevents the flocculation of LE but does not affect the coalescence. Analysis of the stability of LE was performed by the separate considerations of the flocculation and coalescence.
Yamaguchi
T
T
Pharmaceutics Laboratory, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
Nishizaki
K
K
Itai
S
S
Hayashi
H
H
Ohshima
H
H
D002368:Castor Oil / Q000737:chemistry; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002784:Cholesterol / Q000737:chemistry; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004355:Drug Stability; D004655:Emulsions; D005079:Excipients; D005217:Fat Emulsions, Intravenous / Q000737:chemistry*; D005427:Flocculation; D019301:Oleic Acid; D009829:Oleic Acids / Q000737:chemistry; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D013501:Surface-Active Agents; D013678:Technology, Pharmaceutical; D013816:Thermodynamics
D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D005217:Fat Emulsions, Intravenous; D009829:Oleic Acids; D011136:Polysorbates; D013501:Surface-Active Agents; D019301:Oleic Acid; D002368:Castor Oil; D002784:Cholesterol