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Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis
This research aimed to boost granisetron (GS) delivery to the brain via the intranasal route to better manage chemotherapy-induced emesis. Glycerol monooleate (GMO), Poloxamer 407 (P 407) and Tween 80 (T 80) were used to formulate GS-loaded cubosomes (GS-CBS) utilizing a melt dispersion-emulsificati...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9316995/ https://www.ncbi.nlm.nih.gov/pubmed/35890270 http://dx.doi.org/10.3390/pharmaceutics14071374 |
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author | Eissa, Essam M. Elkomy, Mohammed H. Eid, Hussein M. Ali, Adel A. Abourehab, Mohammed A. S. Alsubaiyel, Amal M. Naguib, Ibrahim A. Alsalahat, Izzeddin Hassan, Amira H. |
author_facet | Eissa, Essam M. Elkomy, Mohammed H. Eid, Hussein M. Ali, Adel A. Abourehab, Mohammed A. S. Alsubaiyel, Amal M. Naguib, Ibrahim A. Alsalahat, Izzeddin Hassan, Amira H. |
author_sort | Eissa, Essam M. |
collection | PubMed |
description | This research aimed to boost granisetron (GS) delivery to the brain via the intranasal route to better manage chemotherapy-induced emesis. Glycerol monooleate (GMO), Poloxamer 407 (P 407) and Tween 80 (T 80) were used to formulate GS-loaded cubosomes (GS-CBS) utilizing a melt dispersion-emulsification technique. GS-CBS were characterized by testing particle diameter, surface charge and entrapment efficiency. The formulations were optimized using a Box–Behnken statistical design, and the optimum formula (including GMO with a concentration of 4.9%, P 407 with a concentration of 10%, and T 80 with a concentration of 1%) was investigated for morphology, release behavior, ex vivo permeation through the nasal mucosa, and physical stability. Moreover, the optimal formula was incorporated into a thermosensitive gel and subjected to histopathological and in vivo biodistribution experiments. It demonstrated sustained release characteristics, increased ex vivo permeability and improved physical stability. Moreover, the cubosomal in situ gel was safe and biocompatible when applied to the nasal mucosa. Furthermore, compared to a drug solution, the nose-to-brain pathway enhanced bioavailability and brain distribution. Finally, the cubosomal in situ gel may be a potential nanocarrier for GS delivery to the brain through nose-to-brain pathway. |
format | Online Article Text |
id | pubmed-9316995 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-93169952022-07-27 Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis Eissa, Essam M. Elkomy, Mohammed H. Eid, Hussein M. Ali, Adel A. Abourehab, Mohammed A. S. Alsubaiyel, Amal M. Naguib, Ibrahim A. Alsalahat, Izzeddin Hassan, Amira H. Pharmaceutics Article This research aimed to boost granisetron (GS) delivery to the brain via the intranasal route to better manage chemotherapy-induced emesis. Glycerol monooleate (GMO), Poloxamer 407 (P 407) and Tween 80 (T 80) were used to formulate GS-loaded cubosomes (GS-CBS) utilizing a melt dispersion-emulsification technique. GS-CBS were characterized by testing particle diameter, surface charge and entrapment efficiency. The formulations were optimized using a Box–Behnken statistical design, and the optimum formula (including GMO with a concentration of 4.9%, P 407 with a concentration of 10%, and T 80 with a concentration of 1%) was investigated for morphology, release behavior, ex vivo permeation through the nasal mucosa, and physical stability. Moreover, the optimal formula was incorporated into a thermosensitive gel and subjected to histopathological and in vivo biodistribution experiments. It demonstrated sustained release characteristics, increased ex vivo permeability and improved physical stability. Moreover, the cubosomal in situ gel was safe and biocompatible when applied to the nasal mucosa. Furthermore, compared to a drug solution, the nose-to-brain pathway enhanced bioavailability and brain distribution. Finally, the cubosomal in situ gel may be a potential nanocarrier for GS delivery to the brain through nose-to-brain pathway. MDPI 2022-06-29 /pmc/articles/PMC9316995/ /pubmed/35890270 http://dx.doi.org/10.3390/pharmaceutics14071374 Text en © 2022 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 Eissa, Essam M. Elkomy, Mohammed H. Eid, Hussein M. Ali, Adel A. Abourehab, Mohammed A. S. Alsubaiyel, Amal M. Naguib, Ibrahim A. Alsalahat, Izzeddin Hassan, Amira H. Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis |
title | Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis |
title_full | Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis |
title_fullStr | Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis |
title_full_unstemmed | Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis |
title_short | Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis |
title_sort | intranasal delivery of granisetron to the brain via nanostructured cubosomes-based in situ gel for improved management of chemotherapy-induced emesis |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9316995/ https://www.ncbi.nlm.nih.gov/pubmed/35890270 http://dx.doi.org/10.3390/pharmaceutics14071374 |
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