A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and Microbiome
Objective: This study aimed to develop a holobiont tablet with rapid dispersibility to provide regulation of the microbiota, virucidal activity, and skin barrier protection. Methods: A 2<sup>3</sup> factorial experiment was planned to define the best formulation for the development of th...
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MDPI AG
2023-12-01
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Series: | Pharmaceutics |
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Online Access: | https://www.mdpi.com/1999-4923/15/12/2793 |
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author | Ana Carolina Henriques Ribeiro Machado Laís Júlio Marinheiro Heather Ann Elizabeth Benson Jeffrey Ernest Grice Tereza da Silva Martins Alexandra Lan Patricia Santos Lopes Newton Andreo-Filho Vania Rodrigues Leite-Silva |
author_facet | Ana Carolina Henriques Ribeiro Machado Laís Júlio Marinheiro Heather Ann Elizabeth Benson Jeffrey Ernest Grice Tereza da Silva Martins Alexandra Lan Patricia Santos Lopes Newton Andreo-Filho Vania Rodrigues Leite-Silva |
author_sort | Ana Carolina Henriques Ribeiro Machado |
collection | DOAJ |
description | Objective: This study aimed to develop a holobiont tablet with rapid dispersibility to provide regulation of the microbiota, virucidal activity, and skin barrier protection. Methods: A 2<sup>3</sup> factorial experiment was planned to define the best formulation for the development of the base tablet, using average weight, hardness, dimensions, swelling rate, and disintegration time as parameters to be analyzed. To produce holobiont tablets, the chosen base formulation was fabricated by direct compression of prebiotics, postbiotics, and excipients. The tablets also incorporated solid lipid nanoparticles containing postbiotics that were obtained by high-pressure homogenization and freeze-drying. The in vitro virucidal activity against alpha-coronavirus particles (CCoV-VR809) was determined in VERO cell culture. In vitro analysis, using monolayer cells and human equivalent skin, was performed by rRTq-PCR to determine the expression of interleukins 1, 6, 8, and 17, aquaporin-3, involucrin, filaggrin, FoxO3, and SIRT-1. Antioxidant activity and collagen-1 synthesis were also performed in fibroblast cells. Metagenomic analysis of the skin microbiome was determined in vivo before and after application of the holobiont tablet, during one week of continuous use, and compared to the use of alcohol gel. Samples were analyzed by sequencing the V3–V4 region of the 16S rRNA gene. Results: A handrub tablet with rapid dispersibility was developed for topical use and rinse off. After being defined as safe, the virucidal activity was found to be equal to or greater than that of 70% alcohol, with a reduction in interleukins and maintenance or improvement of skin barrier gene markers, in addition to the reestablishment of the skin microbiota after use. Conclusions: The holobiont tablets were able to improve the genetic markers related to the skin barrier and also its microbiota, thereby being more favorable for use as a hand sanitizer than 70% alcohol. |
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institution | Directory Open Access Journal |
issn | 1999-4923 |
language | English |
last_indexed | 2024-03-08T20:25:40Z |
publishDate | 2023-12-01 |
publisher | MDPI AG |
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spelling | doaj.art-06ce3a6a5d874ae3badd11dffe49a8c82023-12-22T14:32:22ZengMDPI AGPharmaceutics1999-49232023-12-011512279310.3390/pharmaceutics15122793A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and MicrobiomeAna Carolina Henriques Ribeiro Machado0Laís Júlio Marinheiro1Heather Ann Elizabeth Benson2Jeffrey Ernest Grice3Tereza da Silva Martins4Alexandra Lan5Patricia Santos Lopes6Newton Andreo-Filho7Vania Rodrigues Leite-Silva8Programa de Pós-Graduação em Medicina Translacional, Universidade Federal de São Paulo, Rua Pedro de Toledo, 720, Sao Paulo 04039-002, SP, BrazilDepartamento de Ciências Farmacêuticas, Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua São Nicolau, 210, Diadema 09913-030, SP, BrazilCurtin Medical School, Curtin University, Perth, WA 6845, AustraliaFrazer Institute, Faculty of Medicine, The University of Queensland, Brisbane, QLD 4102, AustraliaLaboratório de Materiais Híbridos, Departamento de Química, Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua São Nicolau, 210, 2° Andar, Diadema 09913-030, SP, BrazilShanghai Pechoin Daily Chemical Corporation, Shanghai 200060, ChinaDepartamento de Ciências Farmacêuticas, Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua São Nicolau, 210, Diadema 09913-030, SP, BrazilDepartamento de Ciências Farmacêuticas, Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, Rua São Nicolau, 210, Diadema 09913-030, SP, BrazilPrograma de Pós-Graduação em Medicina Translacional, Universidade Federal de São Paulo, Rua Pedro de Toledo, 720, Sao Paulo 04039-002, SP, BrazilObjective: This study aimed to develop a holobiont tablet with rapid dispersibility to provide regulation of the microbiota, virucidal activity, and skin barrier protection. Methods: A 2<sup>3</sup> factorial experiment was planned to define the best formulation for the development of the base tablet, using average weight, hardness, dimensions, swelling rate, and disintegration time as parameters to be analyzed. To produce holobiont tablets, the chosen base formulation was fabricated by direct compression of prebiotics, postbiotics, and excipients. The tablets also incorporated solid lipid nanoparticles containing postbiotics that were obtained by high-pressure homogenization and freeze-drying. The in vitro virucidal activity against alpha-coronavirus particles (CCoV-VR809) was determined in VERO cell culture. In vitro analysis, using monolayer cells and human equivalent skin, was performed by rRTq-PCR to determine the expression of interleukins 1, 6, 8, and 17, aquaporin-3, involucrin, filaggrin, FoxO3, and SIRT-1. Antioxidant activity and collagen-1 synthesis were also performed in fibroblast cells. Metagenomic analysis of the skin microbiome was determined in vivo before and after application of the holobiont tablet, during one week of continuous use, and compared to the use of alcohol gel. Samples were analyzed by sequencing the V3–V4 region of the 16S rRNA gene. Results: A handrub tablet with rapid dispersibility was developed for topical use and rinse off. After being defined as safe, the virucidal activity was found to be equal to or greater than that of 70% alcohol, with a reduction in interleukins and maintenance or improvement of skin barrier gene markers, in addition to the reestablishment of the skin microbiota after use. Conclusions: The holobiont tablets were able to improve the genetic markers related to the skin barrier and also its microbiota, thereby being more favorable for use as a hand sanitizer than 70% alcohol.https://www.mdpi.com/1999-4923/15/12/2793handrub tabletsolid lipid nanoparticlesvirucideskin barriermicrobiome |
spellingShingle | Ana Carolina Henriques Ribeiro Machado Laís Júlio Marinheiro Heather Ann Elizabeth Benson Jeffrey Ernest Grice Tereza da Silva Martins Alexandra Lan Patricia Santos Lopes Newton Andreo-Filho Vania Rodrigues Leite-Silva A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and Microbiome Pharmaceutics handrub tablet solid lipid nanoparticles virucide skin barrier microbiome |
title | A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and Microbiome |
title_full | A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and Microbiome |
title_fullStr | A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and Microbiome |
title_full_unstemmed | A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and Microbiome |
title_short | A Novel Handrub Tablet Loaded with Pre- and Post-Biotic Solid Lipid Nanoparticles Combining Virucidal Activity and Maintenance of the Skin Barrier and Microbiome |
title_sort | novel handrub tablet loaded with pre and post biotic solid lipid nanoparticles combining virucidal activity and maintenance of the skin barrier and microbiome |
topic | handrub tablet solid lipid nanoparticles virucide skin barrier microbiome |
url | https://www.mdpi.com/1999-4923/15/12/2793 |
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