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Surprising lack of liposome-induced complement activation by artificial 1,3-diamidophospholipids in vitro

Type of publication Peer-reviewed
Publikationsform Original article (peer-reviewed)
Author Bugna Simon, Buscema Marzia, Matviykiv Sofiya, Urbanics Rudolf, Weinberger Andreas, Meszaros Tamas, Szebeni Janos, Zumbuehl Andreas, Saxer Till, Müller Bert,
Project Exploring Stable Phospholipid Membranes
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Original article (peer-reviewed)

Journal Nanomedicine: Nanotechnology, Biology, and Medicine
Volume (Issue) 12(3)
Page(s) 845 - 849
Title of proceedings Nanomedicine: Nanotechnology, Biology, and Medicine
DOI 10.1016/j.nano.2015.12.364


© 2015 Elsevier Inc. Cardio-vascular diseases are the main cause of death, emphasizing the need to improve patient treatment and survival. One therapeutic approach is a liposome-based drug carrier system specifically targeting constricted arteries. The recently discovered mechano-sensitive liposomes use hemodynamic shear-stress differences between healthy and constricted blood vessels as trigger for drug release. Liposomes are promising delivery containers but are being recognized as foreign by the immune system. Complement activation as essential factor of the recognition leads to adverse effects. Here, we tested complement activation by liposomes formulated from the artificial phospholipid Pad-PC-Pad in vitro. Surprisingly no complement activation was detected in human sera and porcine plasma. In in vivo experiments with three pigs, neither anaphylactic reactions nor other significant hemodynamic changes were observed even at comparably high liposome doses. The pilot study holds promise for an absence of complement-mediated adverse effects of Pad-PC-Pad liposomes in human. From the Clinical Editor: A lot of research has been done on new treatment for cardiovascular diseases. Liposome-based carrier systems have also shown promises. In this article, the authors studied the potential risks of complement activation by liposomes in in-vivo experiments. The absence of complement activation by Pad-PC-Pad liposomes may indicate its use in humans.