Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA Delivery

Abstract Intranasal delivery of mRNA vaccines offers promising opportunities to combat airborne viruses like SARS‐CoV‐2 by provoking mucosal immunity, which not only defends against respiratory infection but also prevents contagious transmission. However, the development of nasal mRNA vaccines has b...

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Main Authors: Nipuni Maniyamgama, Ki Hyun Bae, Zi Wei Chang, Jialing Lee, Melgious J. Y. Ang, Yong Jie Tan, Lisa F. P. Ng, Laurent Renia, Kevin P. White, Yi Yan Yang
Format: Article
Language:English
Published: Wiley 2025-03-01
Series:Advanced Science
Subjects:
Online Access:https://doi.org/10.1002/advs.202407383
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author Nipuni Maniyamgama
Ki Hyun Bae
Zi Wei Chang
Jialing Lee
Melgious J. Y. Ang
Yong Jie Tan
Lisa F. P. Ng
Laurent Renia
Kevin P. White
Yi Yan Yang
author_facet Nipuni Maniyamgama
Ki Hyun Bae
Zi Wei Chang
Jialing Lee
Melgious J. Y. Ang
Yong Jie Tan
Lisa F. P. Ng
Laurent Renia
Kevin P. White
Yi Yan Yang
author_sort Nipuni Maniyamgama
collection DOAJ
description Abstract Intranasal delivery of mRNA vaccines offers promising opportunities to combat airborne viruses like SARS‐CoV‐2 by provoking mucosal immunity, which not only defends against respiratory infection but also prevents contagious transmission. However, the development of nasal mRNA vaccines has been hampered by the lack of effective means to overcome the mucus barrier. Herein, ionizable lipid‐incorporated liquid lipid nanoparticles (iLLNs) capable of delivering mRNA cargo across airway mucosa are designed. Adjusting the ratios of ionizable and cationic lipids allows fine‐tuning of the pKa of iLLNs to the range of nasal mucosal pH (5.5–6.5), thus facilitating mucus penetration via the formation of near‐neutral, PEGylated muco‐inert surfaces. When nasally administered to mice, the top candidate iLLN‐2/mRNA complexes enable about 60‐fold greater reporter gene expression in the nasal cavity, compared to the benchmark mRNA‐lipid nanoparticles (ALC‐LNP) having the same lipid composition as that of BNT162b2 vaccine. Moreover, a prime‐boost intranasal immunization of iLLN‐2/mRNA complexes elicits a greater magnitude of SARS‐CoV‐2 spike‐specific mucosal IgA and IgG response than ALC‐LNP, without triggering any noticeable inflammatory reactions. Taken together, these results provide useful insights for the design of nasally deliverable mRNA formulations for prophylactic applications.
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spelling doaj-art-e00b030ed4844ce7accceab01aa92e062025-08-20T02:24:47ZengWileyAdvanced Science2198-38442025-03-011211n/an/a10.1002/advs.202407383Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA DeliveryNipuni Maniyamgama0Ki Hyun Bae1Zi Wei Chang2Jialing Lee3Melgious J. Y. Ang4Yong Jie Tan5Lisa F. P. Ng6Laurent Renia7Kevin P. White8Yi Yan Yang9Bioprocessing Technology Institute (BTI) Agency for Science, Technology and Research (A*STAR) 20 Biopolis Way, Centros #06‐01 Singapore 138668 Republic of SingaporeBioprocessing Technology Institute (BTI) Agency for Science, Technology and Research (A*STAR) 20 Biopolis Way, Centros #06‐01 Singapore 138668 Republic of SingaporeA*STAR Infectious Diseases Labs (A*STAR ID Labs) Agency for Science, Technology and Research (A*STAR) 8A Biomedical Grove, Immunos #05‐13 Singapore 138648 Republic of SingaporeBioprocessing Technology Institute (BTI) Agency for Science, Technology and Research (A*STAR) 20 Biopolis Way, Centros #06‐01 Singapore 138668 Republic of SingaporeBioprocessing Technology Institute (BTI) Agency for Science, Technology and Research (A*STAR) 20 Biopolis Way, Centros #06‐01 Singapore 138668 Republic of SingaporeA*STAR Infectious Diseases Labs (A*STAR ID Labs) Agency for Science, Technology and Research (A*STAR) 8A Biomedical Grove, Immunos #05‐13 Singapore 138648 Republic of SingaporeA*STAR Infectious Diseases Labs (A*STAR ID Labs) Agency for Science, Technology and Research (A*STAR) 8A Biomedical Grove, Immunos #05‐13 Singapore 138648 Republic of SingaporeA*STAR Infectious Diseases Labs (A*STAR ID Labs) Agency for Science, Technology and Research (A*STAR) 8A Biomedical Grove, Immunos #05‐13 Singapore 138648 Republic of SingaporeDepartment of Biochemistry and Precision Medicine Translational Research Program Yong Loo Lin School of Medicine National University of Singapore Singapore 119228 Republic of SingaporeBioprocessing Technology Institute (BTI) Agency for Science, Technology and Research (A*STAR) 20 Biopolis Way, Centros #06‐01 Singapore 138668 Republic of SingaporeAbstract Intranasal delivery of mRNA vaccines offers promising opportunities to combat airborne viruses like SARS‐CoV‐2 by provoking mucosal immunity, which not only defends against respiratory infection but also prevents contagious transmission. However, the development of nasal mRNA vaccines has been hampered by the lack of effective means to overcome the mucus barrier. Herein, ionizable lipid‐incorporated liquid lipid nanoparticles (iLLNs) capable of delivering mRNA cargo across airway mucosa are designed. Adjusting the ratios of ionizable and cationic lipids allows fine‐tuning of the pKa of iLLNs to the range of nasal mucosal pH (5.5–6.5), thus facilitating mucus penetration via the formation of near‐neutral, PEGylated muco‐inert surfaces. When nasally administered to mice, the top candidate iLLN‐2/mRNA complexes enable about 60‐fold greater reporter gene expression in the nasal cavity, compared to the benchmark mRNA‐lipid nanoparticles (ALC‐LNP) having the same lipid composition as that of BNT162b2 vaccine. Moreover, a prime‐boost intranasal immunization of iLLN‐2/mRNA complexes elicits a greater magnitude of SARS‐CoV‐2 spike‐specific mucosal IgA and IgG response than ALC‐LNP, without triggering any noticeable inflammatory reactions. Taken together, these results provide useful insights for the design of nasally deliverable mRNA formulations for prophylactic applications.https://doi.org/10.1002/advs.202407383intranasalionizableliquid lipid nanoparticlesmRNAmuco‐penetrating
spellingShingle Nipuni Maniyamgama
Ki Hyun Bae
Zi Wei Chang
Jialing Lee
Melgious J. Y. Ang
Yong Jie Tan
Lisa F. P. Ng
Laurent Renia
Kevin P. White
Yi Yan Yang
Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA Delivery
Advanced Science
intranasal
ionizable
liquid lipid nanoparticles
mRNA
muco‐penetrating
title Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA Delivery
title_full Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA Delivery
title_fullStr Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA Delivery
title_full_unstemmed Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA Delivery
title_short Muco‐Penetrating Lipid Nanoparticles Having a Liquid Core for Enhanced Intranasal mRNA Delivery
title_sort muco penetrating lipid nanoparticles having a liquid core for enhanced intranasal mrna delivery
topic intranasal
ionizable
liquid lipid nanoparticles
mRNA
muco‐penetrating
url https://doi.org/10.1002/advs.202407383
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