Lipid Composition Modulates Organ-Specific Reactogenicity of Lipid Nanoparticles After Two Administrations
Mikhail Bespalov, Lilia Shirokova, Elena Mazunina, Sofia Kozlova, Evgeniia Bykonia, Olga Vasileva, Sophia Konovalova, Yulia Venediktova, Maria Vorontsova, Vladimir Gushchin, Denis Logunov, Roman Ivanov, Vasiliy Reshetnikov, Darya TeleginaBackground: Lipid nanoparticles (LNPs) can activate innate immunity, but the factors shaping repeat-dose reactogenicity remain unclear. We compared systemic, local, and organ-specific reactions after intramuscular administrations of empty LNPs containing ionizable lipids used in mRNA vaccines. Methods: Female BALB/c mice received two intramuscular injections, 2 weeks apart, of LNP-4 (four components, ALC-0315 as the sole ionizable lipid; 59 nm) or LNP-5 (five components, equimolar ALC-0315/SM-102 at the same total ionizable lipid content; 86 nm). Body weight was monitored for 15 days. Blood biochemical parameters, injection-site histology, and morphological and molecular markers in the hypothalamus, liver, lungs, and spleen were assessed 24 h after the second injection by histology, immunohistochemistry (IHC), immunofluorescence (IF), Western blotting, and quantitative PCR (qPCR). Results: Both LNPs were followed by transient body-weight loss, moderate biochemical changes, and local reactogenicity. The strongest organ-specific responses occurred in the liver and hypothalamus. Both LNPs induced hepatic sinusoidal dilation and leukocyte infiltration, but LNP-4 was associated with more myeloid cell numbers and higher inflammatory marker expression. In the hypothalamus, LNP-4 produced broader changes in inflammatory and myeloid marker expression than LNP-5. No marked structural damage was observed in the examined organs. Conclusions: Repeated LNP administration was followed by systemic and local reactogenicity, and organ-specific changes differed between the formulations, possibly reflecting lipid composition, particle size, and lipid dose. Carrier composition should be considered in the design and safety evaluation of LNP-based vaccine delivery systems.