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Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles

The nose-to-brain delivery route is used to bypass the blood–brain barrier and deliver drugs directly into the brain. Over the years, significant signs of progress have been made in developing nano-drug delivery systems to address the very low drug transfer levels seen with conventional formulations...

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Autores principales: Perteghella, Sara, Rassu, Giovanna, Gavini, Elisabetta, Obinu, Antonella, Bari, Elia, Mandracchia, Delia, Bonferoni, Maria Cristina, Giunchedi, Paolo, Torre, Maria Luisa
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8150760/
https://www.ncbi.nlm.nih.gov/pubmed/34065101
http://dx.doi.org/10.3390/pharmaceutics13050680
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author Perteghella, Sara
Rassu, Giovanna
Gavini, Elisabetta
Obinu, Antonella
Bari, Elia
Mandracchia, Delia
Bonferoni, Maria Cristina
Giunchedi, Paolo
Torre, Maria Luisa
author_facet Perteghella, Sara
Rassu, Giovanna
Gavini, Elisabetta
Obinu, Antonella
Bari, Elia
Mandracchia, Delia
Bonferoni, Maria Cristina
Giunchedi, Paolo
Torre, Maria Luisa
author_sort Perteghella, Sara
collection PubMed
description The nose-to-brain delivery route is used to bypass the blood–brain barrier and deliver drugs directly into the brain. Over the years, significant signs of progress have been made in developing nano-drug delivery systems to address the very low drug transfer levels seen with conventional formulations (e.g., nasal solutions). In this paper, sericin nanoparticles were prepared using crocetin as a new bioactive natural cross-linker (NPc) and compared to sericin nanoparticles prepared with glutaraldehyde (NPg). The mean diameter of NPc and NPg was about 248 and 225 nm, respectively, and suitable for nose-to-brain delivery. The morphological investigation revealed that NPc are spherical-like particles with a smooth surface, whereas NPg seem small and rough. NPc remained stable at 4 °C for 28 days, and when freeze-dried with 0.1% w/v of trehalose, the aggregation was prevented. The use of crocetin as a natural cross-linker significantly improved the in vitro ROS-scavenging ability of NPc with respect to NPg. Both formulations were cytocompatible at all the concentrations tested on human fibroblasts and Caco-2 cells and protected them against oxidative stress damage. In detail, for NPc, the concentration of 400 µg/mL resulted in the most promising to maintain the cell metabolic activity of fibroblasts higher than 90%. Overall, the results reported in this paper support the employment of NPc as a nose-to-brain drug delivery system, as the brain targeting of antioxidants is a potential tool for the therapy of neurological diseases.
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spelling pubmed-81507602021-05-27 Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles Perteghella, Sara Rassu, Giovanna Gavini, Elisabetta Obinu, Antonella Bari, Elia Mandracchia, Delia Bonferoni, Maria Cristina Giunchedi, Paolo Torre, Maria Luisa Pharmaceutics Article The nose-to-brain delivery route is used to bypass the blood–brain barrier and deliver drugs directly into the brain. Over the years, significant signs of progress have been made in developing nano-drug delivery systems to address the very low drug transfer levels seen with conventional formulations (e.g., nasal solutions). In this paper, sericin nanoparticles were prepared using crocetin as a new bioactive natural cross-linker (NPc) and compared to sericin nanoparticles prepared with glutaraldehyde (NPg). The mean diameter of NPc and NPg was about 248 and 225 nm, respectively, and suitable for nose-to-brain delivery. The morphological investigation revealed that NPc are spherical-like particles with a smooth surface, whereas NPg seem small and rough. NPc remained stable at 4 °C for 28 days, and when freeze-dried with 0.1% w/v of trehalose, the aggregation was prevented. The use of crocetin as a natural cross-linker significantly improved the in vitro ROS-scavenging ability of NPc with respect to NPg. Both formulations were cytocompatible at all the concentrations tested on human fibroblasts and Caco-2 cells and protected them against oxidative stress damage. In detail, for NPc, the concentration of 400 µg/mL resulted in the most promising to maintain the cell metabolic activity of fibroblasts higher than 90%. Overall, the results reported in this paper support the employment of NPc as a nose-to-brain drug delivery system, as the brain targeting of antioxidants is a potential tool for the therapy of neurological diseases. MDPI 2021-05-09 /pmc/articles/PMC8150760/ /pubmed/34065101 http://dx.doi.org/10.3390/pharmaceutics13050680 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Perteghella, Sara
Rassu, Giovanna
Gavini, Elisabetta
Obinu, Antonella
Bari, Elia
Mandracchia, Delia
Bonferoni, Maria Cristina
Giunchedi, Paolo
Torre, Maria Luisa
Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles
title Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles
title_full Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles
title_fullStr Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles
title_full_unstemmed Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles
title_short Crocetin as New Cross-Linker for Bioactive Sericin Nanoparticles
title_sort crocetin as new cross-linker for bioactive sericin nanoparticles
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8150760/
https://www.ncbi.nlm.nih.gov/pubmed/34065101
http://dx.doi.org/10.3390/pharmaceutics13050680
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