Resorcinolic lipids improve the properties of sphingomyelin–cholesterol liposomes

Alkylresorcinolic lipids isolated from cereal grains and their semi-synthetic myristoyl-sulphonyl derivatives (MSAR) were used to modify small long-circulating sphingomyelin–cholesterol liposomes. Those SM:Chol vesicles modified with 10–30 mol% resorcinolic lipids had stable size and low membrane pe...

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Bibliographic Details
Published in:Chemistry and physics of lipids 2010-09, Vol.163 (7), p.648-654
Main Authors: Zant-Przeworska, E., Stasiuk, M., Gubernator, J., Kozubek, A.
Format: Article
Language:English
Subjects:
Alkylresorcinol derivative
Alkylresorcinols
Animals
Cholesterol - chemistry
Drug Stability
Fluoresceins - chemistry
Humans
Liposomes
Liposomes - blood
Liposomes - pharmacokinetics
Male
Rats
Resorcinolic lipids
Resorcinols - pharmacology
Serum stability
Sphingomyelin
Sphingomyelins - chemistry
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Summary:Alkylresorcinolic lipids isolated from cereal grains and their semi-synthetic myristoyl-sulphonyl derivatives (MSAR) were used to modify small long-circulating sphingomyelin–cholesterol liposomes. Those SM:Chol vesicles modified with 10–30 mol% resorcinolic lipids had stable size and low membrane permeability in vitro at 4 °C and 37 °C. Liposomes containing 30 mol% MSAR showed very fast solute release in the presence of human plasma at 37 °C, which was drastically diminished in heat-inactivated plasma. In vivo studies showed that unmodified SM:Chol liposomes and those modified with alkylresorcinols were eliminated from the circulation more slowly than liposomes with the highest concentration of MSAR in membrane and were located mostly in the liver and spleen.
ISSN:0009-3084
1873-2941
DOI:10.1016/j.chemphyslip.2010.05.202