Novel functionalization of liposomic nano-vehicles for strongly-enhanced drug delivery

Introduction

Delivery to diseased cells or tissues of therapeutic agents attached or encapsulated in nanoparticles – nanomedicine – presents many benefits and comprises a rapidly-growing multi-billion-euro market.

Lipid-Based Drug Delivery

Lipid-based drug-delivery nano-vehicles, where drugs (not least the recent, very widely used, mRNA-based COVID-19 vaccines) are encapsulated in lipid vesicles (liposomes) or lipid nanoparticles, form a substantial part of that market.

Current Standards and Limitations

Nearly all FDA-approved liposomic vehicles are functionalized with poly(ethylene glycol), PEG, moieties, the current gold standard. These act both to:

• Sterically stabilize the vesicles
• Increase their blood-retention time and thus their therapeutic efficiency

At the same time, such PEGylation has several drawbacks, including:

1. Reduced cellular uptake
2. Accumulation of PEG in tissues
3. Accelerated blood clearance on repeated intravenous dosage due to heightened immune response

Novel Functionalization Approaches

We use novel functionalization approaches to overcome these drawbacks. The present project explores the innovation dimension of our new approach.

Research Questions

In particular, we aim to address the following questions:

• Is it effective?
• Is it efficient?
• How widely applicable is it?
• What is the IPR position for future exploitation of this new strategy?

These questions illustrate the high-risk/high-gain nature of this proposal and are addressed here through several inter-related work packages.

Potential Impact

Success of our project in demonstrating that our novel approach is significantly superior to the current universally used PEGylation would not only have a therapeutic advantage for many diseases but also tap into a large and growing market.