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  • 1
    ISSN: 1573-904X
    Keywords: lipid emulsion ; flocculation ; coalescence ; DLVO theory ; phosphatidylcholine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. 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, Vt max, and the energy barrier for coalescence, W. Methods. The Vt max and W were calculated from the ζ potential and the rate of increase in LE particle size, respectively. Results. The Vt max and W of LE containing the oleic acid were 0.598 × 10−19 J and 3.03 × 10−19 J, respectively, while those of LE without the cosurfactant were 0.141 × 10−19 J and 1.36 × 10−19 J. Conclusions. These findings suggest that oleic acid prevents the flocculation and coalescence of LE. The Vt max and W of LE containing the cholesterol were 0.435 × 10−19 J and 0.63 × 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.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-904X
    Keywords: in vivo ESR ; spin-label ; lipid emulsion ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. We applied non-invasive and real-time method with in vivo ESR spectroscopy to determining pharmacokinetics and metabolism of lipid emulsion as a drug carrier in living mice. Methods. A spin-labeled triglyceride (SL-TG) was newly synthesized and lipid emulsion containing SL-TG was prepared. In vivo ESR spectra in mice were observed after intravenous administration of the lipid emulsion. Results. In vivo ESR spectra consisted of three components, coinciding with the in vitro spectra of SL-TG particles, free and immobilized fatty acids. The amount of the components depended on both the observing domain and the period after administration. In the chest, all three components were observed, while SL-TG particle was lacking in the abdomen. The half-life of the lipid particles in the chest was 2 hr. Conclusions. Non-invasive and real-time analysis of drug carriers in living animal is successfully accomplished using an in vivo ESR method.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1573-904X
    Keywords: emulsion ; flocculation ; coalescence ; DLVO theory ; phosphatidylcholine ; Hamaker constant
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The particle size of lipid emulsion (LE) is changed by flocculation and coalescence. This change in particle size was studied using values obtained for maximum total interaction energy (Vtmax) for flocculation and activation energy for coalescence (E). Vtmax was calculated using DLVO theory, and E was calculated from the rate of increase in particle size in LE. Two LEs (PC99LE and PC70LE) were prepared from lecithins containing 99% and 70% phosphatidylcholine, respectively. The Hamaker constants for PC99LE and PC70LE were found to be 1.4 × 10−22 J and 3.1 × 10−21 J, respectively. Vtmax for PC99LE was 4.7 kT at 121°C, and E was 1.5 × 10−19 J, while Vtmax for PC70LE at 121°C was 151 kT and E was 3.2 ×10 −19 J. These findings suggest that PC99LE readily underwent flocculation and coalescence with increase in particle size, but that the particle size of PC70LE changed little. The degrees of flocculation and coalescence of LE were determined separately using values of Vtmax and E. These parameters are thus quite useful in predicting the stability of LE.
    Type of Medium: Electronic Resource
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