Small-Angle X-ray Scattering Unveils the Internal Structure of Lipid Nanoparticles

Fuente: arXiv
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Hauptverfasser: Spinozzi, Francesco, Moretti, Paolo, Perinelli, Diego Romano, Corucci, Giacomo, Piergiovanni, Paolo, Amenitsch, Heinz, Sancini, Giulio Alfredo, Franzese, Giancarlo, Blasi, Paolo
Format: Preprint
Veröffentlicht: 2023
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author Spinozzi, Francesco
Moretti, Paolo
Perinelli, Diego Romano
Corucci, Giacomo
Piergiovanni, Paolo
Amenitsch, Heinz
Sancini, Giulio Alfredo
Franzese, Giancarlo
Blasi, Paolo
author_facet Spinozzi, Francesco
Moretti, Paolo
Perinelli, Diego Romano
Corucci, Giacomo
Piergiovanni, Paolo
Amenitsch, Heinz
Sancini, Giulio Alfredo
Franzese, Giancarlo
Blasi, Paolo
contents Lipid nanoparticles own a remarkable potential in nanomedicine, only partially disclosed. While the clinical use of liposomes and cationic lipid-nucleic acid complexes is well-established, liquid lipid nanoparticles (nanoemulsions), solid lipid nanoparticles, and nanostructured lipid carriers have even greater potential. However, they face obstacles in being used in clinics due to a lack of understanding about the molecular mechanisms controlling their drug loading and release, interactions with the biological environment (such as the protein corona), and shelf-life stability. To create effective drug delivery carriers and successfully translate bench research to clinical settings, it is crucial to have a thorough understanding of the internal structure of lipid nanoparticles. Through synchrotron small-angle X-ray scattering experiments, we determined the spatial distribution and internal structure of the nanoparticles' lipid, surfactant, and the water in them. The nanoparticles themselves have a barrel-like shape that consists of coplanar lipid platelets (specifically cetyl palmitate) that are partially covered by polysorbate 80 surfactant and retain a small amount of hydration water. Although the platelet structure was expected, the presence of surfactant molecules forming sticky patches between adjacent platelets challenges the classical core-shell model used to describe solid lipid nanoparticles. Additionally, the surfactant partially covers the water-nanoparticle interface, allowing certain lipid regions to come into direct contact with surrounding water. These structural features play a significant role in drug loading and release, biological fluid interaction, and nanoparticle stability, making these findings valuable for the rational design of lipid-based nanoparticles.
format Preprint
id arxiv_https___arxiv_org_abs_2309_12679
institution arXiv
publishDate 2023
record_format arxiv
spellingShingle Small-Angle X-ray Scattering Unveils the Internal Structure of Lipid Nanoparticles
Spinozzi, Francesco
Moretti, Paolo
Perinelli, Diego Romano
Corucci, Giacomo
Piergiovanni, Paolo
Amenitsch, Heinz
Sancini, Giulio Alfredo
Franzese, Giancarlo
Blasi, Paolo
Soft Condensed Matter
Lipid nanoparticles own a remarkable potential in nanomedicine, only partially disclosed. While the clinical use of liposomes and cationic lipid-nucleic acid complexes is well-established, liquid lipid nanoparticles (nanoemulsions), solid lipid nanoparticles, and nanostructured lipid carriers have even greater potential. However, they face obstacles in being used in clinics due to a lack of understanding about the molecular mechanisms controlling their drug loading and release, interactions with the biological environment (such as the protein corona), and shelf-life stability. To create effective drug delivery carriers and successfully translate bench research to clinical settings, it is crucial to have a thorough understanding of the internal structure of lipid nanoparticles. Through synchrotron small-angle X-ray scattering experiments, we determined the spatial distribution and internal structure of the nanoparticles' lipid, surfactant, and the water in them. The nanoparticles themselves have a barrel-like shape that consists of coplanar lipid platelets (specifically cetyl palmitate) that are partially covered by polysorbate 80 surfactant and retain a small amount of hydration water. Although the platelet structure was expected, the presence of surfactant molecules forming sticky patches between adjacent platelets challenges the classical core-shell model used to describe solid lipid nanoparticles. Additionally, the surfactant partially covers the water-nanoparticle interface, allowing certain lipid regions to come into direct contact with surrounding water. These structural features play a significant role in drug loading and release, biological fluid interaction, and nanoparticle stability, making these findings valuable for the rational design of lipid-based nanoparticles.
title Small-Angle X-ray Scattering Unveils the Internal Structure of Lipid Nanoparticles
topic Soft Condensed Matter
url https://arxiv.org/abs/2309.12679