Article (Scientific journals)
Effect of PEG Anchor and Serum on Lipid Nanoparticles: Development of a Nanoparticles Tracking Method
Berger, Manon; Degey, Manon; Leblond Chain, Jeanne et al.
2023In Pharmaceutics, 15 (2)
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Keywords :
NTA analysis; LNP; protein corona; lipid-PEG
Abstract :
[en] Polyethylene glycol (PEG) is used in Lipid Nanoparticles (LNPs) formulations to confer stealth properties and is traditionally anchored in membranes by a lipid moiety whose length significantly impacts the LNPs fate in vivo. C18 acyl chains are efficiently anchored in the membrane, while shorter C14 lipids are quickly desorbed and replaced by a protein corona responsible for the completely different fate of LNPs. In this context, a method to predict the biological behavior of LNPs depending on the lipid-PEG dissociation was developed using the Nanoparticle Tracking Analysis (NTA) method in serum. Two formulations of siRNA-containing LNPs were prepared including CSL3 or SM-102 lipids and were grafted with different lipids-PEG (C18, C14 lipids-PEG, and Ceramide-PEG). The impact of the lipid-PEG on the interactions between LNPs and serum components was demonstrated by monitoring the mean particle size and the concentration over time. In vitro, these formulations demonstrated low toxicity and efficient gene knockdown on tumor MDA-MB-231 cells, but serum was found to significantly impact the efficiency of C18-PEG-based LNPs, while it did not impact the efficiency of C14-PEG-based LNPs. The NTA method demonstrated the ability to discriminate between the behaviors of LNPs according to serum proteins’ interactions. CSL3 lipid and Cer-PEG were confirmed to have promise for LNP formulation.
Research center :
CIRM - Centre Interdisciplinaire de Recherche sur le Médicament - ULiège
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Berger, Manon  ;  Université de Liège - ULiège > Département de pharmacie > Développement de nanomédicaments
Degey, Manon ;  Université de Liège - ULiège > Faculté de Médecine > Master sc. pharma., à fin.
Leblond Chain, Jeanne;  Université de Bordeaux [FR] > CNRS, INSERM, ARNA, UMR 5320, U1212
Maquoi, Erik  ;  Université de Liège - ULiège > GIGA > GIGA Cancer - Tumours and development biology
Evrard, Brigitte  ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Lechanteur, Anna  ;  Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique
Piel, Géraldine ;  Université de Liège - ULiège > Département de pharmacie > Développement de nanomédicaments
Language :
English
Title :
Effect of PEG Anchor and Serum on Lipid Nanoparticles: Development of a Nanoparticles Tracking Method
Publication date :
10 February 2023
Journal title :
Pharmaceutics
ISSN :
1999-4923
Publisher :
MDPI AG
Special issue title :
Special Issue Therapeutic RNA Delivery Systems for Treatment of Cancer
Volume :
15
Issue :
2
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 13 February 2023

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