[The resistance of liposomes as potential drug carriers to the action of phospholipase A2].
Stability of liposomes with varied phospholipid (PL) content towards the action of phospholipase A2 (PLA2) was studied in vitro. Liposomes were prepared of phosphatidylcholine (PC), phosphatidylglycerol (PG), phosphatidylethanolamine (PE), and phosphatidylinositol (PI) and their mixtures with sphingomyelin (SM). PC and PG liposomes were also treated with PLA2 in the presence of a number of proteins such as cytochrome c, cytochrome b5, cytochrome P-450, polylysine, and histone H1. Among all the liposomes studied PG-containing ones were found to be most stable towards PLA2. In SM-containing liposomes, the levels of PG, PI, PE and PC after 20 min of hydrolysis were 65, 62, 55 and 50%, respectively. In PC + PG liposomes, the PC content after treatment with PLA2 was by about 15-20% higher than in control PC liposomes. The addition of all the proteins studied influenced significantly stability of both PC and PG in two-component PL liposomes, but had no effect on liposomes consisting only of PC. The incorporation of the integral membrane protein cytochrome P-450 into PC and PG liposomes caused a decrease in their stability towards PLA2, the decrease depending on the lipid/protein molar ratio.
N M
NM
Litvinko
T A
TA
Shumilina
M K
MK
Naubatova
A A
AA
Akhrem
D004337:Drug Carriers; D004347:Drug Interactions; D004355:Drug Stability; D006868:Hydrolysis; D008081:Liposomes / Q000494:pharmacology*; D010741:Phospholipases A / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D054467:Phospholipases A2; D010743:Phospholipids / Q000494:pharmacology; D011506:Proteins / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013997:Time Factors
D004337:Drug Carriers; D008081:Liposomes; D010743:Phospholipids; D011506:Proteins; D010741:Phospholipases A; D054467:Phospholipases A2
Izuchenie ustoĭchivosti liposom kak potentsial'nykh perenoschikov lekarstvennykh veshchestv k deĭstviiu fosfolipazy A2.