title: Development and characterization of highly selective target-sensitive liposomes for the delivery of streptokinase: in vitro/in vivo studies.
abstract: Streptokinase is one of the most commonly used thrombolytic agents for the treatment of thromboembolism. Short half-life of the streptokinase requires administration of higher dose which results in various side effects including systemic haemorrhage due to activation of systemic plasmin. To increase the selectivity of the streptokinase and hence to reduce side effects, various novel carriers have been developed. Among these carriers, liposomes have been emerged as versatile carrier. In the present study, highly selective target-sensitive liposomes were developed and evaluated by in vitro and in vivo studies. Prepared liposomes were found to release streptokinase in vitro following binding with activated platelets. Intravital microscopy studies in thrombosed murine model revealed higher accumulation of liposomes in the thrombus area. In vivo thrombolysis study was performed in the human clot inoculated rat model. Results of the study showed that target-sensitive liposomes dissolved 28.27 ± 1.56% thrombus as compared to 17.18 ± 1.23% of non-liposomal streptokinase. Further, it was also observed that target-sensitive liposomes reduced the clot dissolution time as compared to streptokinase solution. Studies concluded that developed liposomes might be pragmatic carriers for the treatment of thromboembolism.
authors.affiliation: a Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences , Dr. H. S. Gour University , Sagar , Madhya Pradesh , India and.
authors.forename: Bhuvaneshwar
authors.initials: B
authors.lastname: Vaidya
authors.affiliation: b Department of Biochemistry, Institute of Medical Sciences , Banaras Hindu University , Varanasi , Uttar Pradesh , India.
authors.forename: Manasa K
authors.initials: MK
authors.lastname: Nayak
authors.affiliation: b Department of Biochemistry, Institute of Medical Sciences , Banaras Hindu University , Varanasi , Uttar Pradesh , India.
authors.forename: Debabrata
authors.initials: D
authors.lastname: Dash
authors.affiliation: a Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences , Dr. H. S. Gour University , Sagar , Madhya Pradesh , India and.
authors.forename: Govind P
authors.initials: GP
authors.lastname: Agrawal
authors.affiliation: a Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences , Dr. H. S. Gour University , Sagar , Madhya Pradesh , India and.
authors.forename: Suresh P
authors.initials: SP
authors.lastname: Vyas
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods; D006207:Half-Life; D006470:Hemorrhage / Q000188:drug therapy; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry*; D008297:Male; D051379:Mice; D051381:Rats; D017208:Rats, Wistar; D013300:Streptokinase / Q000008:administration & dosage* / Q000737:chemistry; D013923:Thromboembolism / Q000188:drug therapy; D013927:Thrombosis / Q000188:drug therapy
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D013300:Streptokinase
keywords: Streptokinase; target-sensitive liposomes; targeting; thrombolytic agents; thrombus