Introduction: Hemostasis is a complex physiological mechanism that maintains normal
blood flow and prevents excessive bleeding after vascular injury. Anticoagulant drugs are
widely used to prevent systemic embolism, stroke, and recurrent venous thromboembolism
(VTE). Conventional therapies such as heparins and vitamin K antagonists (VKAs) face challenges
including parenteral administration, toxicity, and poor patient compliance, leading to an
increased need for innovative delivery systems and reversal strategies.
Methods: This review synthesises current evidence on nanotechnology-driven drug delivery systems
(DDS) and antidote development for anticoagulants, drawing from recent preclinical and
clinical studies. The focus is on liposomes, ethosomes, cubosomes, hydrogels, solid lipid nanoparticles
(SLnPs), self-nanoemulsifying drug delivery systems (SNEDDS), and emerging antidotes
such as idarucizumab, andexanet alfa, and ciraparantag.
Results: Nanocarrier systems enhance anticoagulant therapy by improving solubility, stability,
targeted delivery, and sustained release. Oral DDS approaches, including solid dispersions, fastdissolving
platforms, and SNEDDS, show potential to replace invasive parenteral regimens. Antidote
development has advanced rapidly, with idarucizumab approved for dabigatran reversal,
andexanet alfa for factor Xa inhibitors, and ciraparantag demonstrating broad-spectrum activity
in development.
Discussion: Nanotechnology-based DDS address long-standing limitations of conventional anticoagulants,
improving patient compliance and therapeutic safety. However, cost, immunogenicity,
clearance pathways, and regulatory challenges remain barriers to widespread adoption. Antidotes,
while effective, raise concerns about accessibility and affordability in low-resource settings.
Conclusion: This review highlights the novelty of integrating nanotechnology-based delivery
systems with targeted antidote strategies. Such convergence offers a patient-centred, safer, and
more effective framework for anticoagulant therapy, while underscoring the need for future research
in clinical translation, cost-effectiveness, and long-term safety.