Polyglycerol fatty acid esters as alternatives to PEGylated lipids for liposome coating

Abstract

Background: Polyglycerol (PG) is a type of biocompatible hydrophilic polyether polyol, and it is considered as a potential alternative to polyethylene glycol (PEG) in modifying nanomedicines. Materials & methods: Polyglycerol fatty acid esters (PGFEs) were modified onto liposomes and their serum stability, pharmacokinetics, in vivo distribution and the capacity to induce anti-PEG IgM were compared with PEGylated liposomes (PEG-Lips). Results: Polyglycerol 10-monostearate (PG-10-MS) displayed considerable serum stability and compatibility with mice red blood cells, and it significantly prolonged the blood circulation of liposomes in the pharmacokinetics study compared with the unmodified liposomes, with a similar biodistribution pattern to that of the PEG-Lips. Moreover, PGFE-modified liposomes were less likely to induce the production of anti-PEG IgM. Conclusion: PGFEs could be considered as good candidates to replace PEG lipids for the preparation of liposomes.