Monoacyl Phospholipids as Interfacial Stabilizers in Parenteral Protein Formulations

Richard Wibel and Peter Hölig, Lipoid GmbH, Frigenstr. 4, D-67065 Ludwigshafen, Germany (email: p.hoelig@lipoid.com)

Monoacyl phospholipids are phospholipids with one fatty acid chain in the sn-1 position, while the sn-2 position is not esterified (Figure 1). Monoacyl phospholipids (MAPL) are endogenous molecules that arise upon enzymatic cleavage of diacyl phospholipids, the main components of cell membranes. Thus, monoacyl phospholipids are also known as lyso phospholipids.

Monoacyl phospholipids are amphiphilic molecules. This allows them to migrate to interfaces where they reduce interfacial tension and can prevent protein adsorption and aggregation. In addition, monoacyl phospholipids are water-soluble and have a conical geometry such as polysorbates. These characteristics prompted investigations regarding their ability to stabilize protein formulations.

MAPLs in Research

In a PRC-funded project carried out in the research group of Prof. Dr. Wolfgang Friess, monoacyl phospholipids were tested for their safety, stability and performance as interfacial stabilizers. A first publication investigates the safety of monoacyl phospholipids in vitro and their ability to stabilize protein formulations at the air-liquid interface in comparison to the benchmark polysorbate 80.1)

A second publication investigates the performance of monoacyl phospholipids regarding chemical stability, long-term stability, and interactions at the silicone oil-liquid interface.2)

In summary, the conducted studies showed that monoacyl phospholipids are a safe, effective and stable alternative to polysorbate 80.

Interested in MAPLs?

Lipoid provides high-quality GMP phospholipids that enable an industrial use of monoacyl phospholipids in parenteral protein formulations. With its long-standing expertise in all technical, regulatory, analytical and scientific aspects of phospholipids, Lipoid can accompany product developments from early R&D stages to commercialization.

Contact info@lipoid.com if you want to learn more about our monoacyl phospholipids and their applications in parenteral protein formulations.