RGD-Modified Nano-Liposomes Encapsulated Eptifibatide with Proper Hemocompatibility and Cytotoxicity Effect

Iranian Journal of Biotechnology

Shojaosadati, Seyed Abbas¹  Bardania, Hassan²  Aliakbari, Farhang³  Kobarfard, Farzad⁴  Tahoori, Mohammad Taher⁵  Morshedi, Dina⁶ 

[1] Biotechnology Group, Department of Chemical Engineering, Tarbiat Modares University, Tehran, Iran;Cellular and Molecular Research Center, Yasuj University of Medical Sciences, Yasuj, Iran;Department of Immunology, Faculty of Medicine, Shahid Sadoughi University of Medical Sciences, Yazd, Iran;Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran;Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran;Industrial and Environmental Biotechnology, National Inst. of Genetic Engineering and Biotechnology, Tehran, Iran

关键词: Liposomes;    Cytotoxicity;    Materials Testing;    Eptifibatide;   

DOI  :  10.21859/ijb.2008

学科分类：生物技术

来源: National Institute for Genetic Engineering and Biotechnology

【 摘 要 】

Background: Eptifibatide (Integrilin®) is a hepta-peptide drug which specifically prevents the aggregation of activated platelets. The peptide drugs are encapsulated into nanolipisomes in order to decreasing their side effects and improving their half-life and bioavailability. Objectives: In this study, the in vitro cytotoxicity and hemocompatibility of RGD-modified nano-liposomes (RGD-MNL) encapsulated a highly potent antiplatelet drug (eptifibatide) was investigated. Material and Methods: RGD-MNL encapsulated eptifibatide was prepared using lipid film hydration and freeze/thawing method. The morphology and size distribution (about 90 nm) of RGD-MNL were characterized using transmission electron microscopy (TEM). The in-vitro cytotoxicity of nano-liposomes was examined using the MTT, LDH release and reactive oxygen species (ROS) generation assays. The effect of RGD-MNL on red blood cells (RBC) was investigated using hemolysis and LDH release assays. Results: The results revealed that RGD-MNL had no significant cytotoxic effect on HeLa and HUVEC cell lines, and also no ROS generation increase in the cells. In addition, the adverse effect of RGD-MNL on LDH release and membrane integrity of RBC was not observed. Conclusions: In conclusion, the recommended RGD-MNL formulations have not any significant cytotoxicity on normal cells or RBC and have potential for protecting and enhancing the activity of antiplatelet drugs.

【 授权许可】

Unknown