Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles

Cationic solid-lipid nanoparticles (cSLNs) have become a promising tool for gene and RNA therapies. PEGylation (PEG) is crucial in enhancing particle stability and protection. We evaluated the impact of PEG on the physicochemical and biological characteristics of cholesteryl-oleate cSLNs (CO-cSLNs)....

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Main Authors: David A. Narváez-Narváez, María Duarte-Ruiz, Sandra Jiménez-Lozano, Cristina Moreno-Castro, Ronny Vargas, Anna Nardi-Ricart, Encarna García-Montoya, Pilar Pérez-Lozano, Josep Mª Suñé-Negre, Cristina Hernández-Munain, Carlos Suñé, Marc Suñé-Pou
Format: Article
Language:English
Published: MDPI AG 2023-11-01
Series:Pharmaceuticals
Subjects:
Online Access:https://www.mdpi.com/1424-8247/16/11/1583
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author David A. Narváez-Narváez
María Duarte-Ruiz
Sandra Jiménez-Lozano
Cristina Moreno-Castro
Ronny Vargas
Anna Nardi-Ricart
Encarna García-Montoya
Pilar Pérez-Lozano
Josep Mª Suñé-Negre
Cristina Hernández-Munain
Carlos Suñé
Marc Suñé-Pou
author_facet David A. Narváez-Narváez
María Duarte-Ruiz
Sandra Jiménez-Lozano
Cristina Moreno-Castro
Ronny Vargas
Anna Nardi-Ricart
Encarna García-Montoya
Pilar Pérez-Lozano
Josep Mª Suñé-Negre
Cristina Hernández-Munain
Carlos Suñé
Marc Suñé-Pou
author_sort David A. Narváez-Narváez
collection DOAJ
description Cationic solid-lipid nanoparticles (cSLNs) have become a promising tool for gene and RNA therapies. PEGylation (PEG) is crucial in enhancing particle stability and protection. We evaluated the impact of PEG on the physicochemical and biological characteristics of cholesteryl-oleate cSLNs (CO-cSLNs). Several parameters were analyzed, including the particle size, polydispersity index, zeta potential, shape, stability, cytotoxicity, and loading efficiency. Five different formulations with specific PEGs were developed and compared in both suspended and freeze-dried states. Small, homogeneous, and cationic suspended nanoparticles were obtained, with the Gelucire 50/13 (PEG-32 hydrogenated palm glycerides; Gelucire) and DSPE-mPEG2000 (1,2-distearoyl-phosphatidylethanolamine-methyl-polyethyleneglycol conjungate-2000; DSPE) formulations exhibiting the smallest particle size (~170 nm). Monodisperse populations of freeze-dried nanoparticles were also achieved, with particle sizes ranging from 200 to 300 nm and Z potential values of 30–35 mV. Notably, Gelucire again produced the smallest particle size (211.1 ± 22.4), while the DSPE and Myrj S100 (polyoxyethylene (100) stearate; PEG-100 Stearate) formulations had similar particle sizes to CO-cSLNs (~235 nm). The obtained PEGylated nanoparticles showed suitable properties: they were nontoxic, had acceptable morphology, were capable of forming SLNplexes, and were stable in both suspended and lyophilized states. These PEG-cSLNs are a potential resource for in vivo assays and have the advantage of employing cost-effective PEGs. Optimizing the lyophilization process and standardizing parameters are also recommended to maintain nanoparticle integrity.
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spelling doaj.art-6d61431077e54d538826a4b5650aea072023-11-24T15:00:23ZengMDPI AGPharmaceuticals1424-82472023-11-011611158310.3390/ph16111583Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid NanoparticlesDavid A. Narváez-Narváez0María Duarte-Ruiz1Sandra Jiménez-Lozano2Cristina Moreno-Castro3Ronny Vargas4Anna Nardi-Ricart5Encarna García-Montoya6Pilar Pérez-Lozano7Josep Mª Suñé-Negre8Cristina Hernández-Munain9Carlos Suñé10Marc Suñé-Pou11Department of Pharmacy and Pharmaceutical Technology, and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, SpainDepartment of Molecular Biology, Institute of Parasitology and Biomedicine “López-Neyra” (IPBLN-CSIC), 18016 Granada, SpainDepartment of Molecular Biology, Institute of Parasitology and Biomedicine “López-Neyra” (IPBLN-CSIC), 18016 Granada, SpainDepartment of Molecular Biology, Institute of Parasitology and Biomedicine “López-Neyra” (IPBLN-CSIC), 18016 Granada, SpainDepartment of Pharmacy and Pharmaceutical Technology, and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology, and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology, and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology, and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology, and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, SpainDepartment of Cell Biology and Immunology, Institute of Parasitology and Biomedicine “López-Neyra” (IPBLN-CSIC), 18016 Granada, SpainDepartment of Molecular Biology, Institute of Parasitology and Biomedicine “López-Neyra” (IPBLN-CSIC), 18016 Granada, SpainDepartment of Pharmacy and Pharmaceutical Technology, and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, SpainCationic solid-lipid nanoparticles (cSLNs) have become a promising tool for gene and RNA therapies. PEGylation (PEG) is crucial in enhancing particle stability and protection. We evaluated the impact of PEG on the physicochemical and biological characteristics of cholesteryl-oleate cSLNs (CO-cSLNs). Several parameters were analyzed, including the particle size, polydispersity index, zeta potential, shape, stability, cytotoxicity, and loading efficiency. Five different formulations with specific PEGs were developed and compared in both suspended and freeze-dried states. Small, homogeneous, and cationic suspended nanoparticles were obtained, with the Gelucire 50/13 (PEG-32 hydrogenated palm glycerides; Gelucire) and DSPE-mPEG2000 (1,2-distearoyl-phosphatidylethanolamine-methyl-polyethyleneglycol conjungate-2000; DSPE) formulations exhibiting the smallest particle size (~170 nm). Monodisperse populations of freeze-dried nanoparticles were also achieved, with particle sizes ranging from 200 to 300 nm and Z potential values of 30–35 mV. Notably, Gelucire again produced the smallest particle size (211.1 ± 22.4), while the DSPE and Myrj S100 (polyoxyethylene (100) stearate; PEG-100 Stearate) formulations had similar particle sizes to CO-cSLNs (~235 nm). The obtained PEGylated nanoparticles showed suitable properties: they were nontoxic, had acceptable morphology, were capable of forming SLNplexes, and were stable in both suspended and lyophilized states. These PEG-cSLNs are a potential resource for in vivo assays and have the advantage of employing cost-effective PEGs. Optimizing the lyophilization process and standardizing parameters are also recommended to maintain nanoparticle integrity.https://www.mdpi.com/1424-8247/16/11/1583cationic solid lipid nanoparticlescSLNspoly(ethylene glycol)PEGfreeze-dryinglyophilization
spellingShingle David A. Narváez-Narváez
María Duarte-Ruiz
Sandra Jiménez-Lozano
Cristina Moreno-Castro
Ronny Vargas
Anna Nardi-Ricart
Encarna García-Montoya
Pilar Pérez-Lozano
Josep Mª Suñé-Negre
Cristina Hernández-Munain
Carlos Suñé
Marc Suñé-Pou
Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles
Pharmaceuticals
cationic solid lipid nanoparticles
cSLNs
poly(ethylene glycol)
PEG
freeze-drying
lyophilization
title Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles
title_full Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles
title_fullStr Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles
title_full_unstemmed Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles
title_short Comparative Analysis of the Physicochemical and Biological Characteristics of Freeze-Dried PEGylated Cationic Solid Lipid Nanoparticles
title_sort comparative analysis of the physicochemical and biological characteristics of freeze dried pegylated cationic solid lipid nanoparticles
topic cationic solid lipid nanoparticles
cSLNs
poly(ethylene glycol)
PEG
freeze-drying
lyophilization
url https://www.mdpi.com/1424-8247/16/11/1583
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