Optimization of RGD-modified Nano-liposomes Encapsulating Eptifibatide

Atherosclerosis is among the major causes of the cardiovascular disease, which results from platelet aggregation, plaque formation, ending to the occlusion of the blood vessels (1). There are chemical, protein, and peptide drugs such as eptifibatide for treating the atherosclerotic plaques efficiently. Eptifibatide (Integrilin) is an intravenous (IV) drug; a cyclic heptapeptide containing 6 amino acids and 1 mercaptopropionyl (des-amino cysteinyl) residue with an interachain disulfide bridge between the cysteine amide and the mercaptopropionyl moieties that selectively inhibits ligand binding to the platelet GP IIb/IIIa receptor and rapidly dissociate from its receptor (2, 3). Eptifibatide is an efficient non immunogenic drug, however has a short half-life due to rapid inactivation and elimination by renal filtration, enzymatic degradation, and accumulation in non-targeted tissues (2). Therefore, the efficiency of the antithrombotic agents such as eptifibatide could be improved through protection and targeted delivery using nano-carriers to the site of thrombus (4). Liposomes are the most commonly used nano-carriers for drug delivery in cardiovascular diseases (5, 6). Iran J Biotech. 2016 June;14(2): e1399 DOI:10.15171/ijb.1399