Cargando…
Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy
The present study aimed to develop a novel formulation containing glutathione (GSH) as an oral antioxidant therapy for the treatment of oxidative stress-related intestinal diseases. To this purpose, solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan 114 and Dynasan 118 were...
Autores principales: | , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2019
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6723327/ https://www.ncbi.nlm.nih.gov/pubmed/31357663 http://dx.doi.org/10.3390/pharmaceutics11080364 |
_version_ | 1783448742249103360 |
---|---|
author | Bertoni, Serena Albertini, Beatrice Facchini, Carlotta Prata, Cecilia Passerini, Nadia |
author_facet | Bertoni, Serena Albertini, Beatrice Facchini, Carlotta Prata, Cecilia Passerini, Nadia |
author_sort | Bertoni, Serena |
collection | PubMed |
description | The present study aimed to develop a novel formulation containing glutathione (GSH) as an oral antioxidant therapy for the treatment of oxidative stress-related intestinal diseases. To this purpose, solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan 114 and Dynasan 118 were produced by spray congealing technology. The obtained SLMs had main particle sizes ranging from 250 to 355 µm, suitable for oral administration. GSH was efficiently loaded into the SLMs at 5% or 20% w/w and the encapsulation process did not modify its chemico-physical properties, as demonstrated by FT-IR, DSC and HSM analysis. Moreover, in vitro release studies using biorelevant media showed that Dynasan 114-based SLMs could efficiently release GSH in various intestinal fluids, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay demonstrated the good radical scavenging activity of this formulation. Dynasan 114-based SLMs exhibited an excellent biocompatibility on intestinal HT-29 cells at concentrations up to 2000 μg/mL. SLMs containing GSH alone or together with another antioxidant agent (catalase) were effective in reducing intracellular reactive oxygen species (ROS) levels. Overall, this study indicated that spray congealed SLMs are a promising oral drug delivery system for the encapsulation of one or more biological antioxidant agents for local intestinal treatment. |
format | Online Article Text |
id | pubmed-6723327 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-67233272019-09-10 Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy Bertoni, Serena Albertini, Beatrice Facchini, Carlotta Prata, Cecilia Passerini, Nadia Pharmaceutics Article The present study aimed to develop a novel formulation containing glutathione (GSH) as an oral antioxidant therapy for the treatment of oxidative stress-related intestinal diseases. To this purpose, solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan 114 and Dynasan 118 were produced by spray congealing technology. The obtained SLMs had main particle sizes ranging from 250 to 355 µm, suitable for oral administration. GSH was efficiently loaded into the SLMs at 5% or 20% w/w and the encapsulation process did not modify its chemico-physical properties, as demonstrated by FT-IR, DSC and HSM analysis. Moreover, in vitro release studies using biorelevant media showed that Dynasan 114-based SLMs could efficiently release GSH in various intestinal fluids, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay demonstrated the good radical scavenging activity of this formulation. Dynasan 114-based SLMs exhibited an excellent biocompatibility on intestinal HT-29 cells at concentrations up to 2000 μg/mL. SLMs containing GSH alone or together with another antioxidant agent (catalase) were effective in reducing intracellular reactive oxygen species (ROS) levels. Overall, this study indicated that spray congealed SLMs are a promising oral drug delivery system for the encapsulation of one or more biological antioxidant agents for local intestinal treatment. MDPI 2019-07-27 /pmc/articles/PMC6723327/ /pubmed/31357663 http://dx.doi.org/10.3390/pharmaceutics11080364 Text en © 2019 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Bertoni, Serena Albertini, Beatrice Facchini, Carlotta Prata, Cecilia Passerini, Nadia Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy |
title | Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy |
title_full | Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy |
title_fullStr | Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy |
title_full_unstemmed | Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy |
title_short | Glutathione-Loaded Solid Lipid Microparticles as Innovative Delivery System for Oral Antioxidant Therapy |
title_sort | glutathione-loaded solid lipid microparticles as innovative delivery system for oral antioxidant therapy |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6723327/ https://www.ncbi.nlm.nih.gov/pubmed/31357663 http://dx.doi.org/10.3390/pharmaceutics11080364 |
work_keys_str_mv | AT bertoniserena glutathioneloadedsolidlipidmicroparticlesasinnovativedeliverysystemfororalantioxidanttherapy AT albertinibeatrice glutathioneloadedsolidlipidmicroparticlesasinnovativedeliverysystemfororalantioxidanttherapy AT facchinicarlotta glutathioneloadedsolidlipidmicroparticlesasinnovativedeliverysystemfororalantioxidanttherapy AT pratacecilia glutathioneloadedsolidlipidmicroparticlesasinnovativedeliverysystemfororalantioxidanttherapy AT passerininadia glutathioneloadedsolidlipidmicroparticlesasinnovativedeliverysystemfororalantioxidanttherapy |