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Profiling patent compounds in lipid nanoparticle formulations of siRNA
Han, Yunfeng1; Wang, Mengyang1; Chen, Yu1; Ouyang, Defang1,2,3; Zheng, Ying1,4; Hu, Yuanjia1,2,3
2024-12-10
Source PublicationMolecular Therapy Nucleic Acids
ISSN2162-2531
Volume35Issue:4Pages:102362
Abstract

Lipid nanoparticles (LNPs) have emerged as a prominent delivery system for nucleic acid drugs, attracting significant attention, especially through the successful development of several commercial products. As a key component in LNPs, cationic lipids have long served as a key technical barrier to block competitors by building up a complex patent thicket. However, there have been few studies as yet that have comprehensively analyzed the patented compounds in LNP formulations, despite a large number of technical reviews and original articles. In this context, this study focuses on analyzing the macroscopic landscapes and microscopic molecular characteristics of LNP patents, aiming to provide a valuable reference for researchers and developers in making informed technological and commercial decisions. By mining 2,994 patents, 265 formulas, 7,674 compounds, and 28,789 fragments, this work sketches the empirical golden ratio of lipid materials in LNP formulation, discloses the advanced technology in the formulation, characterizes high-frequency fragments of heads, linkers and tails in both novel cationic lipids as well as targeting lipids, and establishes a virtual focus library of LNP materials.

DOI10.1016/j.omtn.2024.102362
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaResearch & Experimental Medicine
WOS SubjectMedicine, Research & Experimental
WOS IDWOS:001350523400001
PublisherCELL PRESS, 50 HAMPSHIRE ST, FLOOR 5, CAMBRIDGE, MA 02139
Scopus ID2-s2.0-85207771552
Fulltext Access
Citation statistics
Document TypeJournal article
CollectionDEPARTMENT OF PHARMACEUTICAL SCIENCES
Institute of Chinese Medical Sciences
THE STATE KEY LABORATORY OF QUALITY RESEARCH IN CHINESE MEDICINE (UNIVERSITY OF MACAU)
Corresponding AuthorZheng, Ying; Hu, Yuanjia
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China
2.Centre for Pharmaceutical Regulatory Sciences, University of Macau, Macao SAR, China
3.DPM, Faculty of Health Sciences, University of Macau, Macao SAR, China
4.DPS, Faculty of Health Sciences, University of Macau, Macao SAR, China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences;  Faculty of Health Sciences;  University of Macau
Recommended Citation
GB/T 7714
Han, Yunfeng,Wang, Mengyang,Chen, Yu,et al. Profiling patent compounds in lipid nanoparticle formulations of siRNA[J]. Molecular Therapy Nucleic Acids, 2024, 35(4), 102362.
APA Han, Yunfeng., Wang, Mengyang., Chen, Yu., Ouyang, Defang., Zheng, Ying., & Hu, Yuanjia (2024). Profiling patent compounds in lipid nanoparticle formulations of siRNA. Molecular Therapy Nucleic Acids, 35(4), 102362.
MLA Han, Yunfeng,et al."Profiling patent compounds in lipid nanoparticle formulations of siRNA".Molecular Therapy Nucleic Acids 35.4(2024):102362.
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