scholarly journals Low-Molecular-Weight Heparins: Reduced Size Particulate Systems for Improved Therapeutic Outcomes

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1757 ◽  
Author(s):  
Fahad Akhtar ◽  
Xinyu Wan ◽  
Gang Wu ◽  
Samuel Kesse ◽  
Shaoda Wang ◽  
...  

A wide range of diseases have been treated using low-molecular-weight heparins (LMWHs), the drug of choice for anticoagulation. Owing to their better pharmacokinetic features compared to those of unfractionated heparin (uFH), several systems incorporating LMWHs have been investigated to deliver and improve their therapeutic outcomes, especially through development of their micro- and nano-particles. This review article describes current perspectives on the fabrication, characterization, and application of LMWHs-loaded micro- and nano-particles to achieve ameliorated bioavailability. The valuable applications of LMWH will continue to encourage researchers to identify efficient delivery systems that have specific release characteristics and ameliorated bioavailability, overcoming the challenges presented by biological obstructions and the physicochemical properties of LMWHs.

2003 ◽  
Vol 18 (3) ◽  
pp. 106-109
Author(s):  
D Bergqvist

This review article provides an update on risk factors of venous thromboembolism and methods for preventing its occurrence following surgery. A summary of the prophylactic methods that are currently available is provided, with particular attention given to low molecular weight heparins, which are the most popular. The new methods of Xa inhibition and oral thrombin inhibition are also mentioned. Finally, the most appropriate times to start prophylaxis and the necessary duration are discussed, along with some of the risks of prophylaxis.


Author(s):  
Courtney J. Mycroft-West ◽  
Dunhao Su ◽  
Yong Li ◽  
Scott E. Guimond ◽  
Timothy R. Rudd ◽  
...  

AbstractThe dependence of the host on the interaction of hundreds of extracellular proteins with the cell surface glycosaminoglycan heparan sulphate (HS) for the regulation of homeostasis is exploited by many microbial pathogens as a means of adherence and invasion. The closely related polysaccharide heparin, the widely used anticoagulant drug, which is structurally similar to HS and is a common experimental proxy, can be expected to mimic the properties of HS. Heparin prevents infection by a range of viruses when added exogenously, including S-associated coronavirus strain HSR1 and inhibits cellular invasion by SARS-CoV-2. We have previously demonstrated that unfractionated heparin binds to the Spike (S1) protein receptor binding domain, induces a conformational change and have reported the structural features of heparin on which this interaction depends. Furthermore, we have demonstrated that enoxaparin, a low molecular weight clinical anticoagulant, also binds the S1 RBD protein and induces conformational change. Here we expand upon these studies, to a wide range of low molecular weight heparins and demonstrate that they induce a variety of conformational changes in the SARS-CoV-2 RBD. These findings may have further implications for the rapid development of a first-line therapeutic by repurposing low molecular weight heparins, as well as for next-generation, tailor-made, GAG-based antiviral agents, against SARS-CoV-2 and other members of the Coronaviridae.


1993 ◽  
Vol 13 (S 01) ◽  
pp. S5-S11 ◽  
Author(s):  
Debra Hoppensteadt ◽  
Jeanine Walenga ◽  
A Ahsan ◽  
O Iqbal ◽  
W Jeske ◽  
...  

SummaryThe introduction of low molecular weight heparins has added a new dimension to the pharmacological management of thrombotic disorders. Because of different chemical and pharmacological characteristics, due to the manufacturing process, each LMWH should be considered as a distinct entitity and only be used for its given indication. A list of commercially available LMWHs is included. The mechanism of action of the LMWHs and their use in various disorders are discussed. Available laboratory tests for monitoring LMWHs are presented and their limitations pointed out.


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