[Properties of streptokinase included in polyetylenglycol microcapsules].
Thrombolytic therapy by high doses of streptokinase (SK) that are stipulated by its rapid clearance is accompanied by side effects. In this work for the purpose of lifetime prolongation in bloodstream and decrease in side effects SK was included in microcapsules from water-soluble polyethyleneglygol (PEG) using the double emulsification method. By variation of the emulsification conditions, molecular weight of PEG (20 or 40 kDa) and PEG/SK ratio (12 or 8 mg PEG/1000 IU SK) it was obtained four preparations of PEG-microcapsules with high percent of SK inclusion (approximately 90-91%), which has completely preserved its fibrinolytic activity and released from microcapsules with different rates. The time of SK full release from obtained PEG-microcapsules was varied from 45 to 90 min (pH 7.4; 37 degrees C). The comparative in vitro study ofthrombolytic and side effects of free SK and SK*PEG-microcapsules was conducted. It was found that at equal doses (500 IU/mL) the lysis rates of human plasma clots under the action of encapsulated preparations of SK (with the exception of a small lag period) were equal to the lysis rate induced by free SK. Besides, SK*PEG-microcapsules caused a less exhaustion of plasminogen and fibrinogen in plasma than free SK.
L I
LI
Mukhametova
R B
RB
Aĭsina
D V
DV
Tiupa
A S
AS
Medvedeva
K B
KB
Gershkovich
D002214:Capsules / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems; D006801:Humans; D007700:Kinetics; D008970:Molecular Weight; D010958:Plasminogen / Q000737:chemistry / Q000378:metabolism; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry; D013300:Streptokinase / Q000008:administration & dosage* / Q000737:chemistry; D015912:Thrombolytic Therapy
D002214:Capsules; D011092:Polyethylene Glycols; D010958:Plasminogen; D013300:Streptokinase