Nano-scaled MTCA-KKV: for targeting thrombus, releasing pharmacophores, inhibiting thrombosis and dissolving blood clots in vivo

Abstract

Shurui Zhao,1 Ze Li,1 Fei Huang,2 Jianhui Wu,1 Lin Gui,1 Xiaoyi Zhang,1 Yaonan Wang,1 Xiaozhen Wang,1 Shiqi Peng,1 Ming Zhao11Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, People’s Republic of China; 2Institute of Cancer, Xinqiao Hospital, Third Military Medical University, Chongqing, People’s Republic of ChinaBackground: In vitro (1R,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val (MTCA-KKV) adheres activated platelets, targets P-selectin and GPIIb/IIIa. This led to the development of MTCA-KKV as thrombus targeting nano-medicine.Methods: MTCA-KKV was characterized by nano-feature, anti-thrombotic activity, thrombolytic activity, thrombus target and targeting release.Results: In vivo 0.01 μmol/kg of MTCA-KKV formed nano-particles less than 100 nm in diameter, targeted thrombus, released anti-thrombotic and thrombolytic pharmacophores, prevented thrombosis and dissolved blood clots.Conclusion: Based on the profiles of targeting thrombus, targeting release, inhibiting thrombosis and dissolving blood clots MTCA-KKV is a promising nano-medicine.Keywords: nano-particles, anti-thrombotic, thrombolytic, targeting, release

Keywords

• nano-particles
• anti-thrombotic
• thrombolytic
• targeting
• release