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Updated: Nov 9, 2025

Surface Functionalization of Hepatitis E Virus Nanoparticles Using Chemical Conjugation Methods

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Published on: May 11, 2018

Virus-Derived Peptides for Hepatic Enzyme Delivery.

Anna Pratsinis¹, Philipp Uhl², Jan Stephan Bolten¹

¹Department of Pharmaceutical Sciences, University of Basel, Basel 4056, Switzerland.

Molecular Pharmaceutics

|April 12, 2021

Summary

Hepatitis B virus (HBV) entry inhibitor MyrcludexB (MyrB) was conjugated to horseradish peroxidase (HRP) for targeted enzyme delivery. While in vitro studies confirmed NTCP-specific targeting, in vivo studies showed reduced specificity due to scavenger cell interactions.

Keywords:

bioconjugation enzyme targeting hepatic drug delivery hepatitis B virus zebrafish screening

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Published on: March 25, 2015

Area of Science:

Hepatology
Bioconjugation Chemistry
Drug Delivery Systems

Background:

Hepatitis B virus (HBV) entry is mediated by the sodium taurocholate cotransporting polypeptide (NTCP) receptor.
MyrcludexB (MyrB), an HBV-derived lipopeptide, selectively targets NTCP on hepatocytes.
Targeted enzyme delivery holds promise for prodrug therapies and detoxification.

Purpose of the Study:

To investigate the feasibility of conjugating therapeutic enzymes to MyrB for targeted delivery.
To develop enzyme delivery strategies for hepatotropic targeting.
To evaluate the NTCP-specific targeting of enzyme-MyrB conjugates.

Main Methods:

Horseradish peroxidase (HRP) was conjugated to MyrB using maleimide chemistry.
Coupling was validated using SDS-PAGE and reversed-phase HPLC.
NTCP-mediated targeting was assessed in vitro using cell lines and in vivo using zebrafish embryos and mice models.

Main Results:

HRP-MyrB conjugate demonstrated specific NTCP targeting in vitro, with concentration-dependent binding.
In vivo studies in zebrafish embryos showed interactions with scavenger endothelial cells.
In mice, both MyrB-conjugated and control constructs exhibited liver accumulation, with MyrB conjugation enhancing NTCP-mediated hepatotropism.
Zebrafish studies suggested involvement of stabilin receptors in scavenging processes.

Conclusions:

MyrcludexB (MyrB) can be successfully conjugated to enzymes like HRP for potential ex vivo diagnostic applications.
In vitro, HRP-MyrB achieves NTCP-specific targeting.
In vivo, non-NTCP-mediated interactions with scavenger cells reduce target specificity, necessitating further investigation into targeting mechanisms.