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Review
. 2024 Oct 12;17(10):1362.
doi: 10.3390/ph17101362.

Multifaceted Heparin: Diverse Applications beyond Anticoagulant Therapy

Razia Sultana  1   2 , Masamichi Kamihira  1
Affiliations
Review

Multifaceted Heparin: Diverse Applications beyond Anticoagulant Therapy

Razia Sultana et al. Pharmaceuticals (Basel). .

Abstract

Heparin, a naturally occurring polysaccharide, has fascinated researchers and clinicians for nearly a century due to its versatile biological properties and has been used for various therapeutic purposes. Discovered in the early 20th century, heparin has been a key therapeutic anticoagulant ever since, and its use is now implemented as a life-saving pharmacological intervention in the management of thrombotic disorders and beyond. In addition to its known anticoagulant properties, heparin has been found to exhibit anti-inflammatory, antiviral, and anti-tumorigenic activities, which may lead to its widespread use in the future as an essential drug against infectious diseases such as COVID-19 and in various medical treatments. Furthermore, recent advancements in nanotechnology, including nano-drug delivery systems and nanomaterials, have significantly enhanced the intrinsic biofunctionalities of heparin. These breakthroughs have paved the way for innovative applications in medicine and therapy, expanding the potential of heparin research. Therefore, this review aims to provide a creation profile of heparin, space for its utilities in therapeutic complications, and future characteristics such as bioengineering and nanotechnology. It also discusses the challenges and opportunities in realizing the full potential of heparin to improve patient outcomes and elevate therapeutic interventions.

Keywords: anticoagulant; bioengineering; glycosaminoglycan; heparin; nano-drug delivery systems; nanotechnology.

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Conflict of interest statement

The authors declare that they have no known competing financial interests.

Figures

Figure 1
Figure 1
A timeline of the historical development of therapeutic heparin. USP: United States Pharmacopeia; BSE: bovine spongiform encephalopathy; FDA: Food and Drug Administration.
Figure 2
Figure 2
Structural characterization of unfractionated heparin (UFH) and ultra-low molecular weight heparin (ULMWH), Fondaparinux. (A) The generalized chemical structure of UFH includes major domains, typically consisting of twenty to fifty copies each of trisulfated and disulfated units. (B) Fondaparinux, a synthetic ULMWH, features a specialized antithrombin III (AT) binding site.
Figure 3
Figure 3
Mechanism of heparin action on blood clotting factors in anti-coagulation. The figure illustrates the structure of the AT-binding pentasaccharide, which is crucial for the inactivation of FXa and factor IIa (FIIa). Longer heparin sequences can further enhance this inactivation.
Figure 4
Figure 4
Overview of advanced bioengineering processes in eukaryotic and prokaryotic expression systems, followed by modifications to generate heparin/HS.
Figure 5
Figure 5
Nanotechnology-driven innovations in heparin-based therapeutics.
See this image and copyright information in PMC

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