Low molecular weight heparins for current and future uses: approaches for micro- and nano-particulate delivery

Abstract

Low molecular weight heparins (LMWHs), the anticoagulant drug of choice in many indications, had been suggested as novel drug treatment for a range of diseases. Their superior pharmacokinetic properties compared to unfractionated heparin (UFH), motivated scientists to explore new delivery systems for improved therapeutic outcomes. Micro-and nano-carriers, with the versatile nature and characteristics of materials used for their fabrication, are able to surmount the challenges opposed by their native structures. The present review discusses the recent perspectives on the development of micro-and nano-particulate vectors for the delivery of LMWHs through various routes. Special focus on the application of the suggested systems, their characterization and the achieved improved bioavailability will be given throughout the review.

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

“…Chemical or enzymatic depolymerization of commercial-grade heparin produces low- molecular-weight heparins, which are sulfated oligosaccharides, carry a negative charge, and are hydrophilic in nature [ 45 ]. Table 1 describes the procedures for preparing the most frequently utilized commercial LMWHs [ 46 , 47 ]. To exert an anticoagulant effect, LMWHs catalyze Xa inactivation by binding to antithrombin [ 47 ].…”

Development of Lipid–Polymer Hybrid Nanoparticles for Improving Oral Absorption of Enoxaparin

“…To translate the administration route from injection to oral delivery, it is quite crucial to increase the oral absorption of LMWH [ 7 , 8 ]. With the advances in nanotechnology, polymer- and lipid-based nanocarriers such as polymeric micelles [ 9 ], polymeric nanoparticles [ 10 ], lipid nanocapsules [ 11 ], microemulsions [ 12 ], and solid lipid nanoparticles [ 13 ] have been intensively used to facilitate the oral absorption of LMWH. Rationally designed nanocarriers are able to overcome the hurdles encountered during the absorption process through following ways, including (1) protecting drugs from acidic degradation in the stomach; (2) increasing the intestinal epithelial permeability; (3) facilitating intestinal lymphatic transport [ 13 , 14 , 15 , 16 , 17 , 18 ].…”

Production and Characterization of Melon Sulfated Pectin (Cucumis melo var. acidulus) Nanoparticles with Anticoagulant Potential

“…Studies assert that the drug can be nanoencapsulated to improve its pharmacokinetic profile, improve treatment efficacy, minimize side effects and increase its chemical and conformational stability, confirming the efficiency of the nanoencapsulation of anticoagulant drugs. 7,8 Therefore, the purpose of this paper was to evaluate the anticoagulant activity of pectin isolated and later chemically sulfated and, from these results, produce and characterize a nanocarrier system to expand its therapeutic potential.…”