Abstract：
:To reduce systemic bleeding risks during anticoagulant treatment, a new concept named "precise anticoagulation" was proposed to localize the effects of anticoagulants via the targeted delivery of prodrugs to the coagulation site. In this study, the fusion protein Annexin V-hirudin 3-ABD (hAvHA) was constructed to achieve the prolonged circulation and targeted delivery of hirudin to coagulation sites. hAvHA was inactive as a prodrug, and it could bind to albumin during circulation. The drug was quickly activated via factor Xa-mediated cleavage once coagulation occurred, and hirudin was efficiently released to exert antithrombin activity in vitro. The hAvHA protein could be activated in mouse blood and exert significant anticoagulation effects. The results of FITC labeling illustrated that hAvHA bound to procoagulant platelets, suggesting the Annexin V modification permits targeted delivery to sites of thrombosis. hAvHA bound to albumin in vitro with an equilibrium dissociation constant of 8 pM, suggesting the ABD modification permitted prolonged circulation in vivo. Moreover, the bleeding time was much shorter in hAvHA-treated mice than in hirudin-treated mice. Therefore, our results suggested that that hAvHA is a potential and promising anticoagulant in vivo.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Han HH,Zhang HT,Wang R,Yan Y,Liu X,Wang Y,Zhu Y,Wang JCdoi
10.1016/j.ijpharm.2020.119869subject
Has Abstractpub_date
2020-09-10 00:00:00pages
119869eissn
0378-5173issn
1873-3476pii
S0378-5173(20)30854-1journal_volume
589pub_type
杂志文章abstract：:The purpose of this work was to investigate the influence of dissolution medium composition on the in vitro release of ketoprofen from a series of ER products and the impact of the different buffer media on the in vivo-in vitro (IVIV) relationship. The products investigated were coated micro bead preparations having i...
journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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