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Authors Wu J, Zhu H, Yang G, He J, Wang Y, Zhao S, Zhang X, Gui L, Zhao M, Peng S
Received 28 August 2017
Accepted for publication 22 November 2017
Published 26 February 2018 Volume 2018:13 Pages 1139—1158
DOI https://doi.org/10.2147/IJN.S150205
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Akshita Wason
Peer reviewer comments 2
Editor who approved publication: Dr Linlin Sun
Background: Arterial thrombosis has
been associated with a series of pathological conditions, and the discovery of
arterial thrombosis inhibitor is of clinical importance.
Methods: By analyzing the pharmacophores of anti-platelet
agents, thrombus targeting peptide and anti-thrombotic nano-systems
3S-1,2,3,4-tetrahydroisoquino- line-3-carbonyl-Thr-Ala-Arg-Gly-Asp(Val)-Val
(IQCA-TAVV) was designed and prepared as a nano-scaled arterial thrombosis
inhibitor.
Results: In vitro the nanoparticles of IQCA-TAVV were
able to adhere onto the surface of activated platelets, attenuate activated
platelets to extend pseudopodia and inhibit activated platelets to form
aggregators. In vivo IQCA-TAVV targeted arterial thrombus, dose dependently
inhibited arterial thrombosis with a 1 nmol/kg of minimal effective dose, and
the activity was ~1670 folds of that of aspirin.
Conclusion: IQCA-TAVV represented the design, preparation
and application of nanomedicine capable of adhering on the surface of activated
platelets, attenuating platelet activation, targeting arterial thrombus and
inhibiting arterial thrombosis.
Keywords: arterial
thrombosis, thrombus targeting, nanodelivery, antithrombosis