title: Encapsulation of eptifibatide in RGD-modified nanoliposomes improves platelet aggregation inhibitory activity.
abstract: Eptifibatide is an antiplatelet drug used for the treatment of thrombosis. However, as a result of its accumulation in non-targeted tissues and short half-life, it has a limited efficacy. In this study, RGD-modified nano-liposomes (RGD-MNL) were prepared as carriers for the targeted delivery of eptifibatide to activated platelets. The nano-liposomes were about 90 ± 10 nm in size, with an encapsulation efficiency of 37 ± 5 % and a good stability during 21 days, with a negligible change in the size of nanoliosomes. The in vitro cytotoxicity of nanoliposomes was examined using MTT assay. The results obtained from the ex vivo study showed that the antiplatelet activity of eptifibatide encapsulated nanoliposomes was higher in comparison with the free drug (81.63 vs. 46.17 % for RGD-MNL) and (66.67 vs. 46.17 % for UNL), and this increase was more significant for nanoliposomes targeted with RGD peptide (81.63 %; p < 0.05). The results indicated that RGD-MNL encapsulated eptifibatide had no significant cytotoxic effect on cells. In conclusion, the present nanoliposome formulation can be regarded as a new delivery system for protection and enhancement of the antiplatelet activity of eptifibatide.
authors: Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran.|Cellular and Molecular Research Center, Yasuj University of Medical Sciences, Yasuj, Iran.
authors: Hassan
authors: H
authors: Bardania
authors: Biotechnology Group, Faculty of Chemical Engineering, Tarbiat Modares University, Ale Ahmad Highway, P.O. Box 14115-143, Tehran, Iran. shoja_sa@modares.ac.ir.
authors: Seyed Abbas
authors: SA
authors: Shojaosadati
authors: Department of Medical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Shams Alley, Vali-e-Asr Ave, Tehran, Iran. kobarfard@sbmu.ac.ir.|Phytochemistry Research Center, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Shams Alley, Vali-e-Asr Ave, Tehran, Iran. kobarfard@sbmu.ac.ir.
authors: Farzad
authors: F
authors: Kobarfard
authors: Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
authors: Farid
authors: F
authors: Dorkoosh
authors: Phytochemistry Research Center, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Shams Alley, Vali-e-Asr Ave, Tehran, Iran.
authors: Marjan Esfahani
authors: ME
authors: Zadeh
authors: Cellular and Molecular Research Center, Yasuj University of Medical Sciences, Yasuj, Iran.
authors: Mahmoud
authors: M
authors: Naraki
authors: Department of Pharmacology and Toxicology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
authors: Mehrdad
authors: M
authors: Faizi
mesh_terms: D001792:Blood Platelets / Q000166:cytology; D016923:Cell Death / Q000187:drug effects; D002478:Cells, Cultured; D004337:Drug Carriers / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D000077542:Eptifibatide; D006801:Humans; D008081:Liposomes / Q000737:chemistry / Q000627:therapeutic use*; D053758:Nanoparticles / Q000737:chemistry / Q000627:therapeutic use; D009842:Oligopeptides / Q000737:chemistry; D010455:Peptides / Q000008:administration & dosage* / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage* / Q000494:pharmacology
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D009842:Oligopeptides; D010455:Peptides; D010975:Platelet Aggregation Inhibitors; C047981:arginyl-glycyl-aspartic acid; D000077542:Eptifibatide
keywords: Antiplatelet activity; Cytotoxicity; Eptifibatide; RGD-MNL encapsulated eptifibatide; RGD-modified nanoliposomes (RGD-MNL)