PS and PG enriched extrudates and nanofibers for local anti-inflammatory therapies
The aim of the project is to develop and to characterize anti-inflammatory phospholipid depot formulations for local therapy in the brain, ear and eye. The preparations will include (I) preformed implants and (II) electrospun nonwovens. The project is based on the encouraging results1) obtained with phosphatidylcholine extrudates for controlled release2) and the biological activity of phosphatidylserine (PS) and phosphatidylglycerol (PG) containing phospholipid nanodispersions (PRC project: Phosphatidyl-serine enriched phospholipids as anti-inflammatory agents). PS3) or PG4)5) containing phospholipid depot systems have a high potential for the local treatment of inflammations.
To gain detailed insights into the drug delivery mechanism, we will use electron spin resonance (ESR) spectroscopy and multispectral optical imaging to characterize micro-mobility, micro-polarity, and pH value. The released material will be characterized with respect to the amount, size, and structures (e.g., by light, fluorescence, and electron microscopy).
Finally, such systems could also be used as drug delivery systems. Both the controlled release and the anti-inflammatory properties are attractive aspects with high potential for clinical applications.
Benefit for the community
The project will enlarge the applications of phospholipids. The anti-inflammatory properties of PS and PG enriched phospholipids combined with the advantages of parenteral controlled local drug delivery is very attractive for clinical applications. Because phospholipids are highly biocompatible, such systems have great promise especially within a very sensitive biological environment (e.g., brain, ear, and eyes). Currently there are many unmet needs for the local treatment in these organs. We are confident, that PS and PG enriched phospholipid depot formulations have high potential for clinical applications and we would be happy to contribute in the exploration of properties.
Phosphatidylserine (PS) and Phosphatidylglycerol (PG) Nanodispersions as potential anti-inflammatory therapeutics: Comparison of In Vitro activity and impact of Pegylation
Nanomedicine 23, 102096
Nicardipine loaded solid phospholipid extrudates for the prevention of cerebral vasospasms: in vitro characterization
Pharmaceutics, 12, 817
Apoptotic mimicry: Phosphatidylserine liposomes reduce inflammation through activation of peroxisome proliferator-activated receptors (PPARs) in vivo
Br. J. Pharmacol. 151, 844–850
Soy phosphatidylglycerol reduces inflammation in a contact irritant ear edema mouse model in vivo
J. Pharmacol. Exp. Ther. 366, 1–8
Phosphatidylserine inhibits inflammatory responses in interleukin-1β-stimulated fibroblast-like synoviocytes and alleviates carrageenan-induced arthritis in rat
Nutr. Res. 33, 242–250