Stability of SUV liposomes in the presence of cholate salts and pancreatic lipases: effect of lipid composition.
The effect of bile salts (sodium cholate and sodium taurocholate), and pancreatic lipases on the structural integrity of SUV liposomes of different lipid compositions was studied. Liposomal membrane integrity was judged by bile salt or pancreatin-induced release of vesicle encapsulated 5,6-carboxyfluorescein, and vesicle size distribution before and after incubations. Bile salt concentration was 10 mM, while a saturated solution of pancreatin (mixed with equal volume of liposomes) was utilized. Results agree with earlier studies, demonstrating the instability of liposomes composed of lipids with low transition temperatures (PC and DMPC) in presence of cholates. Addition of cholesterol (1:1 lipid:chol molar ratio) does not substantially increase the encapsulated molecule retention. Nevertheless, liposomes composed of lipids with high transition temperatures (DPPC, DSPC and SM), retain significantly higher amounts of encapsulated material, under all conditions studied. Furthermore, the vesicles formed by mixing cholesterol with these lipids will possibly be sufficiently stable in the gastrointestinal tract for long periods of time. Sizing results reveal that in most cases release of encapsulated molecules is mainly caused by their leakage through holes formed on the lipid bilayer. However, in stearylamine containing DPPC and DSPC vesicles, the cholate-induced drastic decrease in vesicle size suggests total liposome disruption as the possible mechanism of encapsulated material immediate release.
Kokkona
M
M
Department of Pharmacy, School of Health Sciences, University of Patras, Rio 26500, Patras, Greece.
Kallinteri
P
P
Fatouros
D
D
Antimisiaris
S G
SG
D000818:Animals; D002784:Cholesterol; D004355:Drug Stability; D007700:Kinetics; D008049:Lipase; D008081:Liposomes / Q000737:chemistry*; D010179:Pancreas / Q000201:enzymology; D010194:Pancreatin; D010713:Phosphatidylcholines / Q000737:chemistry; D020358:Sodium Cholate; D013109:Sphingomyelins / Q000737:chemistry; D013656:Taurocholic Acid
D008081:Liposomes; D010713:Phosphatidylcholines; D013109:Sphingomyelins; D013656:Taurocholic Acid; D010194:Pancreatin; D002784:Cholesterol; D008049:Lipase; D020358:Sodium Cholate