Phosphatidylserine (PS) and phosphatidylglycerol (PG) nanodispersions as potential anti-inflammatory therapeutics: Comparison of in vitro activity and impact of pegylation

Nanomedicine. 2020 Jan:23:102096. doi: 10.1016/j.nano.2019.102096. Epub 2019 Oct 25.


Phosphatidylserine (PS) and phosphatidylglycerol (PG) are endogenous phospholipids with putative anti-inflammatory potential. However, studies comparing PS and PG are rare and were mainly conducted with phospholipid-dispersions of large size and broad distributions. Thus, we prepared small-sized PS- and PG-loaded liposomes exhibiting narrow distribution, and additionally studied the impact of liposome-pegylation on the reduction of the TNFα-production caused by the PS- and PG-liposomes. These PS- and PG-containing nanodispersions had a small size around 100nm and a narrow distribution (PDI<0.1). The liposome-dispersions showed no toxicity in NHDF- and 3T3-cells and virtually no hemolytic activity. They decreased the TNFα-production of LPS-(lipopolysaccharide)-stimulated mouse peritoneal macrophages in vitro. PG-liposomes always decreased the TNFα-levels more potently than PS-liposomes. Pegylation of PS- and PG-liposomes caused different Zeta potentials, but did not change biological activity. The results of the current study indicate a high potential of the tested formulations for phospholipid-based anti-inflammatory therapies.

Keywords: Inflammation; Liposomes; Nanomedicine; Pegylation; Phosphatidylglycerol; Phosphatidylserine.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3 Cells
  • Animals
  • Humans
  • Inflammation / chemically induced
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Inflammation / pathology
  • Liposomes
  • Macrophages, Peritoneal / metabolism*
  • Macrophages, Peritoneal / pathology
  • Mice
  • Nanoparticles* / chemistry
  • Nanoparticles* / therapeutic use
  • Phosphatidylglycerols* / chemistry
  • Phosphatidylglycerols* / pharmacology
  • Phosphatidylserines* / chemistry
  • Phosphatidylserines* / pharmacology


  • Liposomes
  • Phosphatidylglycerols
  • Phosphatidylserines