Targeted delivery of thrombolytic agents: role of integrin receptors.
Blood clotting (formation of thrombus) plays a critical role in the evolution of a number of cardiovascular diseases. Targeted delivery of thrombolytic agents reduces the risks of hemorrhage and toxicity associated with systemic drug administration, thus offering a promising, minimally invasive approach to controlling and treating thrombosis. Platelets play a major role in the progression of thrombosis on vascular injury. Platelet integrin alphaIIbbeta3 (GP IIb/IIIa) serves as a receptor for various proteins such as fibrinogen, vWF, fibronectin and vitronectin, as well as contributing to the adhesion and aggregation of platelets in a variety of conditions. These receptor-based targeted therapies are currently under clinical studies. Integrins and RGD-based ligands for integrins are currently being investigated in imaging and drug delivery related areas of research. RGD-targeted drugs and imaging agents have been developed either by direct conjugation of the homing peptide to the drug or by conjugation of the RGD-peptide to a carrier device containing drug molecules. This review describes the role of integrin receptors in the pathophysiology of thrombosis and its use in the targeted delivery of thrombolytic agents.
Department of Pharmaceutical Sciences, Dr H. S. Gour University, Sagar 470003 (MP), India. vyas_sp@rediffmail.com
Suresh P
SP
Vyas
Bhuvaneshwar
B
Vaidya
D000818:Animals; D001792:Blood Platelets / Q000187:drug effects / Q000473:pathology; D016503:Drug Delivery Systems / Q000379:methods*; D005343:Fibrinolytic Agents / Q000008:administration & dosage*; D006801:Humans; D008954:Models, Biological; D009842:Oligopeptides / Q000008:administration & dosage; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors / Q000502:physiology; D010980:Platelet Membrane Glycoproteins / Q000037:antagonists & inhibitors* / Q000502:physiology*; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors; D018000:Receptors, Peptide / Q000037:antagonists & inhibitors; D013927:Thrombosis / Q000188:drug therapy / Q000503:physiopathology
D005343:Fibrinolytic Agents; D009842:Oligopeptides; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D010980:Platelet Membrane Glycoproteins; D011971:Receptors, Immunologic; D018000:Receptors, Peptide; C051382:arginyl-glycyl-aspartic acid directed cell adhesion receptor; C047981:arginyl-glycyl-aspartic acid