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Theranostics 2022; 12(17):7509-7531. doi:10.7150/thno.77259 This issue Cite

Review

Lipid nanoparticles for delivery of RNA therapeutics: Current status and the role of in vivo imaging

Han Na Jung^1*, Seok-Yong Lee^2,4,5*, Somin Lee³, Hyewon Youn^4,5✉, Hyung-Jun Im^1,3,4,6✉

1. Department of Applied Bioengineering, Graduate School of Convergence Science and Technology, Seoul National University, Seoul 08826, Republic of Korea.
2. Department of Biomedical Sciences, Seoul National University Graduate School, Seoul 03080, Republic of Korea.
3. Department of Molecular Medicine and Biopharmaceutical Sciences, Graduate School of Convergence Science and Technology, Seoul National University, Seoul 08826, Republic of Korea.
4. Cancer Research Institute, Seoul National University College of Medicine, Seoul 03080, Republic of Korea.
5. Department of Nuclear Medicine, Seoul National University Hospital, Seoul 03080, Republic of Korea.
6. Research Institute for Convergence Science, Seoul National University, Seoul, 08826, Republic of Korea.
* These authors contributed equally to this work.

✉ Corresponding authors: Dr. Hyung Jun Im, iiihjjjac.kr; Dr. Hyewon Youn, hwyounac.kr

Abstract

Lipid nanoparticles (LNPs) have been one of the most successful nano-delivery vehicles that enable efficient delivery of cytotoxic chemotherapy agents, antibiotics, and nucleic acid therapeutics. During the coronavirus disease (COVID-19) pandemic, LNP-based COVID-19 messenger RNA (mRNA) vaccines from Pfizer/BioNTech and Moderna have been successfully developed, resulting in global sales of $37 billion and $17.7 billion, respectively, in 2021. Based on this success, the development of multiple LNP-based RNA therapeutics is gaining momentum due to its potential in vaccines and therapeutics for various genetic diseases and cancers. Furthermore, imaging techniques can be utilized to evaluate the pharmacokinetics and pharmacodynamics (PK/PD) effects, which helps target discovery and accelerates the development of LNP-based mRNA therapies. A thorough introduction and explanation of the components of LNPs and its functions along with various production methods of formulating LNPs are provided in this review. Furthermore, recent advances in LNP-based RNA therapeutics in clinics and clinical trials are explored. Additionally, the evaluation of PK/PD of LNPs for RNA delivery and the current and potential roles in developing LNP-based mRNA pharmaceutics through imaging techniques will be discussed.

Keywords: Lipid nanoparticles, RNA therapeutics, Drug delivery system, Vaccines, In vivo imaging

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