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. 2020 Jan 25;19:1357–1367. doi: 10.1016/j.omtn.2020.01.018

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© 2020 The Authors

This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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Biodistribution of ASO/LNP Complexes in Major Organs (Brain, Heart, Lung, Liver, Spleen, and Kidney)

The three best-performing lipids, 113-O14B-3, 113-O16B-3, and 306-O12B-3, chosen from the in vitro screening studies were formulated in the following formulation: lipids/cholesterol/DOPE/DSPE-PEG2000 at the weight ratio 16/4/1/1. The Alexa 750-labeled ASOs were mixed with formulated LNPs at the weight ratio of 1/15, followed by the intravenous injection to mice. The results showed that all of the ASO-loaded LNPs exhibited most fluorescence signals in the liver, indicating the complexes mainly accumulating in this organ. Also, the ASO-Alexa 750s delivered by 306-O12B-3 exhibited the strongest fluorescence intensity in the liver.