Impact of Liposomal Drug Formulations on the RBCs Shape, Transmembrane Potential, and Mechanical Properties.

Sylwia Cyboran-Mikołajczyk,Marta Kopaczyńska,Michał Płóciennik,Przemysław Sareło,Magdalena Wawrzyńska,Magdalena Przybyło,Robert Pasławski,Urszula Pasławska,Kacper Nowak,Halina Podbielska

doi:10.3390/ijms22041710

Abstract

Liposomal technologies are used in order to improve the effectiveness of current therapies or to reduce their negative side effects. However, the liposome–erythrocyte interaction during the intravenous administration of liposomal drug formulations may result in changes within the red blood cells (RBCs). In this study, it was shown that phosphatidylcholine-composed liposomal formulations of Photolon, used as a drug model, significantly influences the transmembrane potential, stiffness, as well as the shape of RBCs. These changes caused decreasing the number of stomatocytes and irregular shapes proportion within the cells exposed to liposomes. Thus, the reduction of anisocytosis was observed. Therefore, some nanodrugs in phosphatidylcholine liposomal formulation may have a beneficial effect on the survival time of erythrocytes.

Highlights

All the analyzed liposome formulations are characterized by an average size in the range of 113–139 nm, which is consistent with the measurements carried out by means of transmission electron microscopy
The impact of liposome formulations composed of phosphatidylcholine (P1), phosphatidylcholine and cholesterol (P2), and phosphatidylcholine, cholesterol, and polymer polyethylene glycol (PEG) (P3) on shape, transmembrane potential, biomechanical parameters and osmotic resistance of erythrocytes, were assessed
It was shown that erythrocytes treated with P1 and P2 formulation are characterized by a lower value of transmembrane potential and stiffness, which correlates with higher hemolytic resistance and a reduced number of stomatocytes and cells with irregular shapes

Summary

Introduction

This could become possible by liposome enrichment of particular molecules to immobilize the desired drug in the carrier, more efficiently [5] or to enable liposomal formulation of drug to cross the body’s natural barriers, which is impossible for the drug itself [6], as well as simultaneous packaging and delivery to the target site of two or more drugs to enhance the therapeutic effect of co-therapy [7] These facts influenced the emergence of a new group of drugs, so-called super generic drugs, i.e., drugs that differ from the original drugs in their pharmaceutical formulation. The adjuvant properties of liposomal formulations have been used and were exploited for liposome-formulated RNA vaccines development for preventing infectious diseases or treating some cancers, which in the clinical trials have been showed to be safe and well-tolerated [8,9,10]

Objectives

Methods

Results

Conclusion