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KMID : 0369819900200030135
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Jorunal of Korean Pharmaceutical Sciences
1990 Volume.20 No. 3 p.135 ~ p.144
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The Solubilization Behavior of DOPE - Immunoliposomes with Immnoglobulin G ( IgG ) by Added Bile Salts
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이은옥/Lee EO
김진구/김종득/Kim JG/Kim JD
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Abstract
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The effects of bile salts (BS) on the stability of dioleoylphosphatidylethanolamine (DOPE) liposomes were investigated, observing apparent absorbance of vacant liposomes and calcein release from entrapped liposomes. Unilamellar liposomes were prepared by using a small quantity of palmitoly-immunoglobulin G(IgG) (2.5×10?4 mo1/lipid mol) to stabilize the bilayer phase of the unsaturated DOPE which by itself does not form stable liposomes. The destabilization of PE immunoliposomes by papain, clearly demonstrates that the IgG is essential for stabilization of PE bilayer. Approximately 4% of the entrapped calcein was released from the PE liposomes after 1 hr from liposome formation. Calcein release and absorbance of liposomes depended on the BS/lipid ratio because of the solubilization of lipid molecule in bilayer and the formation of mixed micelles. At very low BS concentrations, the incorporation of BS induced BS/lipid aggregates in the outer vesicles monolayer, while high BS concentrations, mixed micelles were formed. Chelate and its conjugates as 3α,7α,12α?trihydroxy BS induce the concentration of the 3α, 12α?dihydroxy BS at half-maximal solubilization of immunoliposomes to approximately 2.5-, or 5-fold. Conjugation of BS with glycine or taurine slightly enhanced their capacities to perturb membranes.
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KEYWORD
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immunoliposome, bile salt, solubilization, IgG
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