Prolonged systemic delivery of streptokinase using liposome.
To prolong the biological half-life of streptokinase, a thrombolytic agent, streptokinase-bearing liposome with and distearolyphosphatidyl ethanolamine-N-poly (ethylene glycol) 2000 (DSPE-PEG 2000) was prepared and evaluated. Streptokinase-bearing liposomes composed of distearolyphosphatidylcholine (DSPC), cholesterol and cholesterol-3-sulfate with DSPE-PEG 2000 was prepared by the freeze-thawing method and administered via femoral vein to rats (15,000 IU/kg). The activity of streptokinase in plasma was determined by the method based on the amidolytic activity of streptokinase-plasminogen complex. Pharmacokinetic parameters of streptokinase incorporated in liposomes were compared with those of streptokinase alone. The T1/2 and AUCinfinity of streptokinase incorporated in DSPC-PEG liposome increased 16.3- and 6.1-fold, respectively, compared with those of streptokinase alone. Streptokinase-bearing long-circulating liposome could increase the circulation time of streptokinase in blood and expect longer thrombolytic activity compared with streptokinase alone.
Kim
I S
IS
College of Pharmacy, Seoul National University, Korea.
Choi
H G
HG
Choi
H S
HS
Kim
B K
BK
Kim
C K
CK
D000818:Animals; D019540:Area Under Curve; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005343:Fibrinolytic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D008081:Liposomes; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013300:Streptokinase / Q000008:administration & dosage* / Q000493:pharmacokinetics
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005343:Fibrinolytic Agents; D008081:Liposomes; D013300:Streptokinase