Mechanistic Insight into pH-Driven Phase Transition of Lipid Nanoparticles DOI Creative Commons
Marius F.W. Trollmann, Rainer A. Böckmann

bioRxiv (Cold Spring Harbor Laboratory), Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 29, 2024

Lipid nanoparticles (LNPs) are essential delivery vehicles in mRNA-based vaccines, with their functionality largely governed by aminolipids. At low pH, protonated aminolipids facilitate efficient mRNA encapsulation, while deprotonation at physiological pH drives LNP remodeling into a stable spherical structure, potentially aiding release during endosomal re-protonation and concomitant restructuring pH. Our study uncovers the pH-dependent phase transition of Comirnaty lipid formulation molecular scale, highlighting intricate interplay between reorganization aminolipid protonation. We observe substantial shift pKa, from 7-8 surface to below 4 within hydrophobic core, resulting an overall apparent pKa nanoparticle 6.3. The protonation significantly affects aminolipid's localization, enriched vicinity neutral monolayer covering LNPs comprises cholesterol (60-65%), helper phospholipids (20-25%), PEGylated lipids (5%), mix deprotonated (5-10%). These findings provide mechanistic insights behavior LNPs, offering foundation for optimizing design enhance stability, tunable responses, therapeutic efficacy.

Language: Английский

Computational Methods for Modeling Lipid-Mediated Active Pharmaceutical Ingredient Delivery DOI Creative Commons
Markéta Paloncýová, Mariana Valério, Ricardo Nascimento dos Santos

et al.

Molecular Pharmaceutics, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 29, 2025

Lipid-mediated delivery of active pharmaceutical ingredients (API) opened new possibilities in advanced therapies. By encapsulating an API into a lipid nanocarrier (LNC), one can safely deliver APIs not soluble water, those with otherwise strong adverse effects, or very fragile ones such as nucleic acids. However, for the rational design LNCs, detailed understanding composition-structure-function relationships is missing. This review presents currently available computational methods LNC investigation, screening, and design. The state-of-the-art physics-based approaches are described, focus on molecular dynamics simulations all-atom coarse-grained resolution. Their strengths weaknesses discussed, highlighting aspects necessary obtaining reliable results simulations. Furthermore, machine learning, i.e., data-based approach to lipid-mediated introduced. data produced by experimental theoretical provide valuable insights. Processing these help optimize LNCs better performance. In final section this Review, computer reviewed, specifically addressing compatibility

Language: Английский

Citations

2

Revisiting lipid nanoparticle composition and structure: A critical take on simulation approaches DOI Creative Commons
Marius F.W. Trollmann,

Paolo Rossetti,

Rainer A. Böckmann

et al.

Proceedings of the National Academy of Sciences, Journal Year: 2025, Volume and Issue: 122(9)

Published: Feb. 24, 2025

Emotions coordinate our behavior and physiological states during survival-salient events pleasurable interactions. Even though we are often consciously aware of current emotional state, such as anger or happiness, the mechanisms giving ...Emotions felt in body, somatosensory feedback has been proposed to trigger conscious experiences. Here reveal maps bodily sensations associated with different emotions using a unique topographical self-report method. In ...

Language: Английский

Citations

1

Capturing the Dynamic Integrity of Carbocyanine Fluorophores-based Lipid Nanoparticles by the FRET technique DOI Creative Commons
Siyu Long, David A. Turner, Kevin J. Hamill

et al.

Journal of Materials Chemistry B, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 1, 2025

Nanoparticles capable of dynamically reporting their structural integrity in real-time are a powerful tool to guide the design drug delivery technologies.

Language: Английский

Citations

0

Reply to Trollmann et al.: Perspective on LNP structure and simulation DOI Creative Commons
Adiran Garaizar, Christian Díaz-Oviedo,

Nina Zablowsky

et al.

Proceedings of the National Academy of Sciences, Journal Year: 2025, Volume and Issue: 122(9)

Published: Feb. 24, 2025

Emotions coordinate our behavior and physiological states during survival-salient events pleasurable interactions. Even though we are often consciously aware of current emotional state, such as anger or happiness, the mechanisms giving ...Emotions felt in body, somatosensory feedback has been proposed to trigger conscious experiences. Here reveal maps bodily sensations associated with different emotions using a unique topographical self-report method. In ...

Language: Английский

Citations

0

Recent strategies for enhanced delivery of mRNA to the lungs DOI
Brittany J. Heiser, Arian Veyssi, Debadyuti Ghosh

et al.

Nanomedicine, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 27

Published: April 7, 2025

mRNA-based therapies have emerged as a transformative tool in modern medicine, gaining significant attention following their successful use COVID-19 vaccines. Delivery to the lungs offers several compelling advantages for mRNA delivery. The are one of most vascularized organs body, which provides an extensive surface area that can facilitate efficient drug transport. Local delivery bypasses gastrointestinal degradation, potentially enhancing therapeutic efficacy. In addition, capillary network ideal target systemic However, developing effective presents challenges. complex anatomy and body's immune response foreign particles create barriers This review discusses key approaches overcoming these challenges improving lungs. It examines both local strategies aimed at lung while mitigating off-target effects. Although substantial progress has been made lung-targeted therapies, remain optimizing cellular uptake achieving efficacy within pulmonary tissues. continued refinement enhance lung-specific targeting minimizing degradation is critical clinical success therapies.

Language: Английский

Citations

0

Mechanistic Insight into pH-Driven Phase Transition of Lipid Nanoparticles DOI Creative Commons
Marius F.W. Trollmann, Rainer A. Böckmann

bioRxiv (Cold Spring Harbor Laboratory), Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 29, 2024

Lipid nanoparticles (LNPs) are essential delivery vehicles in mRNA-based vaccines, with their functionality largely governed by aminolipids. At low pH, protonated aminolipids facilitate efficient mRNA encapsulation, while deprotonation at physiological pH drives LNP remodeling into a stable spherical structure, potentially aiding release during endosomal re-protonation and concomitant restructuring pH. Our study uncovers the pH-dependent phase transition of Comirnaty lipid formulation molecular scale, highlighting intricate interplay between reorganization aminolipid protonation. We observe substantial shift pKa, from 7-8 surface to below 4 within hydrophobic core, resulting an overall apparent pKa nanoparticle 6.3. The protonation significantly affects aminolipid's localization, enriched vicinity neutral monolayer covering LNPs comprises cholesterol (60-65%), helper phospholipids (20-25%), PEGylated lipids (5%), mix deprotonated (5-10%). These findings provide mechanistic insights behavior LNPs, offering foundation for optimizing design enhance stability, tunable responses, therapeutic efficacy.

Language: Английский

Citations

1