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Related Concept Videos

Anticoagulant Drugs: Low-Molecular-Weight Heparins01:30

Anticoagulant Drugs: Low-Molecular-Weight Heparins

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Hemostasis is a crucial process that prevents excessive blood loss from damaged blood vessels. It involves various mechanisms such as vasoconstriction, platelet adhesion and activation, and fibrin formation. The importance of each mechanism depends on the type of vessel injury. In contrast, thrombosis is the abnormal formation of a blood clot within the blood vessels, leading to potential complications if the clot obstructs blood flow. Thrombosis can be caused by increased coagulability of the...
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Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

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Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
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Updated: May 21, 2025

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Supramolecular Prodrug Hydrogel for One-Week Protection Against Thrombosis.

Wenjing Zhang1,2, Xue Tian1, Sheng Xu2

  • 1School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing, 211816, China.

Small (Weinheim an Der Bergstrasse, Germany)
|May 19, 2025
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Summary

A novel long-acting anticoagulant hydrogel delivers Bivalirudin (Biva) on-demand. This engineered peptide depot provides sustained antithrombotic effects with reduced bleeding risk, improving patient compliance.

Keywords:
anticoagulantbivalirudinlong‐termprodrugsupramolecular hydrogel

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Area of Science:

  • Biomaterials Science
  • Pharmacology
  • Nanotechnology

Background:

  • Bivalirudin (Biva) is an anticoagulant with advantages over heparin but has a short half-life, limiting clinical use.
  • Short drug half-life necessitates frequent administration, increasing patient burden and medical costs.

Purpose of the Study:

  • To develop a long-acting, injectable anticoagulant hydrogel for sustained Bivalirudin (Biva) delivery.
  • To create a prodrug system activated by specific proteases at the site of thrombosis.

Main Methods:

  • Engineered a fusion peptide (d-RADA)8-B integrating Biva, a self-assembly motif, and a Factor Xa (FXa)-responsive element.
  • Subcutaneous injection formed a protease-resistant hydrogel depot releasing the prodrug.
  • Assessed antithrombotic efficacy and bleeding risk in animal models of carotid artery and pulmonary embolism.

Main Results:

  • The (d-RADA)8-B hydrogel demonstrated protease-degradation resistance and slow prodrug release.
  • Subcutaneous administration achieved sustained Biva release and effective antithrombotic activity.
  • Significant suppression of embolism was observed in vivo without increased hemorrhage.

Conclusions:

  • Engineered a supramolecular anticoagulant hydrogel for long-term, high-load Bivalirudin (Biva) delivery.
  • Achieved on-demand antithrombotic activation via FXa-responsive prodrug release.
  • This strategy offers a promising approach for improved anticoagulant therapy with enhanced compliance.