Future Science Group
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Efficacy increase of lipid nanoparticles in vivo by inclusion of bis(monoacylglycerol)phosphate - Supplementary data

posted on 2022-10-18, 11:39 authored by Amit Sagi, Rajesh Mukthavaram, River Recatto, Michael DavisMichael Davis, Hyojung Hong, Ramon Diaz Trelles, Nadja El-Mecharrafie, Grishma Acharya, Abraham Gomez, Angel Leu, Kiyoshi Tachikawa, Cristiano Sacchetti, Benchawanna Soontornniyomkij, Kumar Rajappan, Priya Karmali, Padmanabh Chivakula

Aim: To investigate the effect of incorporating bis(monoacylglycerol)phosphate (BMP) lipid into a

lipid nanoparticle and the functional transport of mRNA by the formulated nanoparticles in vivo.

Materials & methods: The nanoparticles were prepared from ionizable lipid, 1,2-distearoyl-sn-glycerol-3-

phosphocholine, cholesterol, 1,2-dimyristoyl-sn-glycerol PEG 2000, BMP and formulated mRNA encoding

human erythropoietin. We measured the effect of BMP on physicochemical properties and impact on

functional efficacy to transport mRNA to its target cells/tissue as measured by protein expression both in

vitro and in vivo. Results: Lipid nanoparticles composed of BMP displayed increased endosomalmembrane

fusion and improved mRNA delivery to the cytosol. Conclusion: The results establish the foundation for

future development of these nanoparticulated entities by designing new BMP derivatives and correlating

structures to enhanced pharmacokinetic profiles.


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