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.
Vyas
Suresh P
SP
Department of Pharmaceutical Sciences, Dr H. S. Gour University, Sagar 470003 (MP), India. vyas_sp@rediffmail.com
Vaidya
Bhuvaneshwar
B
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