Kotowska Anna M, Fay Michael, Watts Julie A, Gilmore Ian S, Scurr David J, Howe Alaina, Capka Vladimir, Perez Corey E, Doud Devin, Patel Siddharth, Umbarger Mark, Langer Robert, Alexander Morgan R
School of Pharmacy, University of Nottingham, Nottingham, UK.
Nanoscale and Microscale Research Centre, University of Nottingham, Nottingham, UK.
Commun Chem. 2025 May 22;8(1):160. doi: 10.1038/s42004-025-01526-x.
Lipid nanoparticle RNA (LNP-RNA) formulations are used for the delivery of vaccines and other therapies. RNA molecules are encapsulated within their interior through electrostatic interactions with positively charged lipids. The identity of the lipids that present at their surface play a role in how they interact with and are perceived by the body and their resultant potency. Here, we use a model formulation to develop cryogenic sample preparation for molecular depth profiling Orbitrap secondary ion mass spectrometry (Cryo-OrbiSIMS) preceded by morphological characterisation using cryogenic transmission electron microscopy (Cryo-TEM). It is found that the depth distribution of individual lipid components is revealed relative to the surface and the RNA cargo defining the core. A preferential lipid orientation can be determined for the 1,2-Dimyristoyl-glycero-3-methox-polyethylene glycol 2000 (DMG-PEG2k) molecule, by comparing the profiles of PEG to DMG fragments. PEG fragments are found immediately during analysis of the LNP surface, while the DMG fragments are deeper, coincident with RNA ions located in the core, in agreement with established models of LNPs. This laboratory-based de novo analysis technique requires no labelling, providing advantages over large facility neutron scattering characterisation.
脂质纳米颗粒RNA(LNP-RNA)制剂用于疫苗和其他疗法的递送。RNA分子通过与带正电的脂质的静电相互作用被包裹在其内部。存在于其表面的脂质的特性在它们与身体的相互作用方式、被身体感知的方式以及它们的最终效力方面发挥着作用。在这里,我们使用一种模型制剂来开发用于分子深度剖析轨道阱二次离子质谱(低温轨道阱二次离子质谱,Cryo-OrbiSIMS)的低温样品制备方法,在此之前使用低温透射电子显微镜(Cryo-TEM)进行形态表征。结果发现,相对于定义核心的表面和RNA负载,揭示了各个脂质成分的深度分布。通过比较聚乙二醇(PEG)与二肉豆蔻酰甘油-3-甲氧基-聚乙二醇2000(DMG-PEG2k)片段的谱图,可以确定DMG-PEG2k分子的优先脂质取向。在分析LNP表面时立即发现PEG片段,而DMG片段更深,与位于核心的RNA离子一致,这与已建立的LNP模型相符。这种基于实验室的从头分析技术无需标记,与大型设施的中子散射表征相比具有优势。