PEGylated nanoemulsions containing 1,2-distearoyl-sn-glycero-3-phosphoglycerol induced weakened accelerated blood clearance phenomenon

Drug Deliv Transl Res. 2022 Oct;12(10):2569-2579. doi: 10.1007/s13346-021-01111-4. Epub 2022 Jan 29.

Abstract

Injections of polyethylene glycol (PEG)-modified nanomedicines can lead to an accelerated clearance of the next dose of PEGylated nanomedicines, which is referred to as the accelerated blood clearance (ABC) phenomenon. It has been reported that anti-PEG IgM plays an important role in the induction of the ABC phenomenon, identifying the interface between the main chain of PEG and the hydrophobic segment of the repeated injections of the PEGylated nanocarriers, resulting in increased liver uptake and loss of long-cycle characteristics. In this study, we demonstrated that the 1,2-distearoyl-sn-glycero-3-phosphoglycerol (DSPG) in PEGylated nanoemulsions (PEs) may mask this interface between the main chain of PEG and the hydrophobic segment, inhibiting the recognition and binding of anti-PEG IgM to PEs, and evidently weakening the ABC phenomenon of PEs. This will provide a novel strategy to improve the curative effect of PEGylated nanocarriers. PEGylated nanoemulsions (PEs) with 1,2-distearoyl-sn-glycero-3-phosphoglycerol (DSPG) induced weakened the accelerated blood clearance (ABC) phenomenon in Wistar rats during repeated injection of PEs.

Keywords: 1,2-Distearoyl-sn-glycero-3-phosphoglycerol; Accelerated blood clearance phenomenon; PEGylated emulsions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Immunoglobulin M
  • Liposomes* / chemistry
  • Liver / metabolism
  • Polyethylene Glycols* / chemistry
  • Rats
  • Rats, Wistar

Substances

  • Immunoglobulin M
  • Liposomes
  • Polyethylene Glycols