For Research Use Only. Not for Clinical Use.

Introduction of HEPylation

HEP, an active polymer of HEPylation is a natural polysaccharide and a biosynthetic precursor of heparin. From a chem-physical standpoint, the HEP chain is very hydrophilic due to its two hydroxyl groups on every monosaccharide unit and a negative carboxylate group on every other monosaccharide unit. Because of its relation to heparin, it is recognized as 'self' inside our body environment and doesn't have any immunogenicity issue. HEP is completely biocompatible and is predicted to serve as a conjugating vehicle to extend the plasma half-life of biologics without liabilities of polydispersity, immunogenicity, and/or unwanted accumulation in the body. The strategy of synthetically decorating or coating drugs with HEP could improve the body's acceptance of drugs, resulting in a more stable, predictable circulation time that is not subject to ABC upon repeat dosing.

Fig.1 HEP modification of drug cargo. (DeAngelis, 2015)

HEP, A Promising 'Naturally Good' Polymeric Conjugating Vehicle for Delivery of Injectable Therapeutics

HEP is stable in the extracellular spaces where many therapeutic drugs act. The molecule has a 0.5 to 8 day half-life in bloodstream depending on its molecular weight and the route of injection. The polymer chain length is stable in the plasma. No accumulation in tissues was observed. The polymer does not cross the blood-brain barrier, which may be important for ensuring the safety of some therapeutics. A variety of biologics have been modified with HEP with retention of activity and improvement of pharmacokinetics. Most of the typical chemistries used to modify molecules with PEG are amenable to use with HEP. HEP meets the criteria for a desirable drug delivery vehicle on multiple fronts. In summary, HEP has ideal intrinsic and economic characteristics for a delivery vehicle.

Custom Services of HEPylation Based Half-Life Extension

HEP and its derivatives are of interest for their potential as pharmacological agents for diversified fields. Creative Biolabs has focused on the half-life extension drug development for many years. We have a very professional technical team and rich project experience in HEPylation-based half-life extension drug development. If you have any problems with half-life extension drug development or you are interested in our services, please do not hesitate to contact us for more details.

Reference

1. DeAngelis, P.L. Heparosans, promising 'naturally good' polymeric conjugating vehicles for delivery of injectable therapeutics. Expert opinion on drug delivery. 2015, 12(3): 349-352.