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Updated: May 12, 2026

Antigenic Liposomes for Generation of Disease-specific Antibodies

Antigenic Liposomes for Generation of Disease-specific Antibodies

Published on: October 25, 2018

Complement activation by PEGylated liposomes containing prednisolone.

Jolanda M van den Hoven¹, Reka Nemes, Josbert M Metselaar

¹Dept. Pharmacy & Pharmacology, Slotervaart Hospital, Louwesweg 6, 1066 EC Amsterdam, The Netherlands. Jolanda.vandenHoven@slz.nl

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences

|March 27, 2013

Summary

Modifying the PEGylation profile of liposomes can reduce complement system activation, a cause of hypersensitivity reactions. This research explores new PEGylation strategies to improve liposome safety and efficacy.

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Area of Science:

Biotechnology
Immunology
Materials Science

Background:

PEGylated liposomes can trigger hypersensitivity reactions (HSRs) due to complement system (C) activation.
This activation is often linked to the negative charge of the PEG anchor molecule on the liposome surface.

Purpose of the Study:

To investigate if altering the PEGylation profile of liposomes can significantly reduce complement system activation.
To achieve complement activation levels comparable to nonreactive liposomal formulations.

Main Methods:

In vitro assays were used to measure complement activation markers (SC5b-9, C3a, C4d, Bb) in normal human serum.
Liposomes with varied PEG chain length, surface concentration, anchor molecule, and size were tested, including both empty and prednisolone-loaded formulations.

Main Results:

Most tested PEGylated liposomes showed minimal or no complement activation.
One formulation, CHOL-PEG2000, demonstrated significant activation of the alternative pathway, indicated by increased SC5b-9 and Bb levels.
CHOL-PEG2000 liposomes uniquely induced direct C3 conversion without charge or antibody mediation.

Conclusions:

Altering PEGylation strategies can effectively minimize complement activation by liposomes, potentially reducing HSRs.
While CHOL-PEG2000 liposomes show promise for understanding liposomal complement activation, their direct C3 conversion suggests caution for clinical development.
Further in vivo studies are needed to confirm the safety of liposomes with reduced complement activation potential.