Platelets directed liposomes for the delivery of streptokinase: development and characterization.
The present study was aimed to study the effect of RGD peptide conjugation on the bio-distribution behaviour of long circulatory liposomes in the thrombosed rat model. Further, thrombolysis study was also performed to evaluate the therapeutic activity of the prepared liposomes. Liposomes were prepared by film hydration method and peptide was subsequently conjugated on the preformed liposomes using carbodiimide chemistry. Prepared liposomes were characterized for size and size distribution, entrapment efficiency and in vitro drug release. In vitro targeting ability of the liposomes was determined by platelets binding assay. In vivo studies were performed in the rat model containing human blood clot inoculated in the carotid artery. Results of the study showed that RGD peptide conjugated liposomes significantly accumulated to the site of blood clot and higher thrombolytic activity was observed with peptide modified liposomes as compared to plain streptokinase solution and long circulatory liposomes.
Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar, Madhya Pradesh, India.
Bhuvaneshwar
B
Vaidya
G P
GP
Agrawal
Suresh P
SP
Vyas
D000818:Animals; D001792:Blood Platelets / Q000187:drug effects* / Q000378:metabolism; D002341:Carotid Artery Thrombosis / Q000188:drug therapy* / Q000378:metabolism; D005343:Fibrinolytic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008081:Liposomes; D009842:Oligopeptides / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010974:Platelet Aggregation / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D013300:Streptokinase / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution
D005343:Fibrinolytic Agents; D008081:Liposomes; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid; D013300:Streptokinase