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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MDPI AG
2023-11-01
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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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issn | 1424-8247 |
language | English |
last_indexed | 2024-03-09T16:32:19Z |
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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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