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In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome

Chronic use of antihistamines can induce abnormalities in lipid absorption with potential excessive accumulation of lipids in the mesentery that can lead to the development of obesity and a metabolic syndrome. The focus of the present work was to develop a transdermal gel formulation of desloratadin...

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Autores principales: Mohamed, Eman M., Dharani, Sathish, Khuroo, Tahir, Hamed, Rania, Khan, Mansoor A., Rahman, Ziyaur
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10144708/
https://www.ncbi.nlm.nih.gov/pubmed/37111335
http://dx.doi.org/10.3390/ph16040578
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author Mohamed, Eman M.
Dharani, Sathish
Khuroo, Tahir
Hamed, Rania
Khan, Mansoor A.
Rahman, Ziyaur
author_facet Mohamed, Eman M.
Dharani, Sathish
Khuroo, Tahir
Hamed, Rania
Khan, Mansoor A.
Rahman, Ziyaur
author_sort Mohamed, Eman M.
collection PubMed
description Chronic use of antihistamines can induce abnormalities in lipid absorption with potential excessive accumulation of lipids in the mesentery that can lead to the development of obesity and a metabolic syndrome. The focus of the present work was to develop a transdermal gel formulation of desloratadine (DES) to prevent/reduce obesity and metabolic syndromes. Nine formulations were prepared to contain hydroxypropyl methylcellulose (2–3%), DES (2.5–5.0%), and Transcutol(®) (15–20%). The formulations were evaluated for cohesive and adhesive properties, viscosity, drug diffusion through synthetic and pig ear skin, and pharmacokinetics in New Zealand white rabbits. Drug permeation was faster through the skin compared to synthetic membranes. The drug had good permeation, as indicated by very short lag time (0.08–0.47 h) and high flux (59.3–230.7 μg/cm(2).h). The maximum plasma concentration (C(max)) and area under the curve (AUC) of transdermal gel formulations were 2.4 and 3.2 fold that of the Clarinex tablet formulation. In conclusion, as indicated by the higher bioavailability, transdermal gel formulation of DES may decrease the dose of the drug, compared to commercial formulation. It has the potential to reduce or eliminate metabolic syndromes associated with oral antihistamine therapy.
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spelling pubmed-101447082023-04-29 In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome Mohamed, Eman M. Dharani, Sathish Khuroo, Tahir Hamed, Rania Khan, Mansoor A. Rahman, Ziyaur Pharmaceuticals (Basel) Article Chronic use of antihistamines can induce abnormalities in lipid absorption with potential excessive accumulation of lipids in the mesentery that can lead to the development of obesity and a metabolic syndrome. The focus of the present work was to develop a transdermal gel formulation of desloratadine (DES) to prevent/reduce obesity and metabolic syndromes. Nine formulations were prepared to contain hydroxypropyl methylcellulose (2–3%), DES (2.5–5.0%), and Transcutol(®) (15–20%). The formulations were evaluated for cohesive and adhesive properties, viscosity, drug diffusion through synthetic and pig ear skin, and pharmacokinetics in New Zealand white rabbits. Drug permeation was faster through the skin compared to synthetic membranes. The drug had good permeation, as indicated by very short lag time (0.08–0.47 h) and high flux (59.3–230.7 μg/cm(2).h). The maximum plasma concentration (C(max)) and area under the curve (AUC) of transdermal gel formulations were 2.4 and 3.2 fold that of the Clarinex tablet formulation. In conclusion, as indicated by the higher bioavailability, transdermal gel formulation of DES may decrease the dose of the drug, compared to commercial formulation. It has the potential to reduce or eliminate metabolic syndromes associated with oral antihistamine therapy. MDPI 2023-04-12 /pmc/articles/PMC10144708/ /pubmed/37111335 http://dx.doi.org/10.3390/ph16040578 Text en © 2023 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
Mohamed, Eman M.
Dharani, Sathish
Khuroo, Tahir
Hamed, Rania
Khan, Mansoor A.
Rahman, Ziyaur
In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome
title In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome
title_full In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome
title_fullStr In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome
title_full_unstemmed In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome
title_short In Vitro and In Vivo Characterization of the Transdermal Gel Formulation of Desloratadine for Prevention of Obesity and Metabolic Syndrome
title_sort in vitro and in vivo characterization of the transdermal gel formulation of desloratadine for prevention of obesity and metabolic syndrome
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10144708/
https://www.ncbi.nlm.nih.gov/pubmed/37111335
http://dx.doi.org/10.3390/ph16040578
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