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Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats
Candesartan cilexetil (CC) is an antihypertensive drug. It has low solubility and faces hepatic first-pass metabolism after oral ingestion. We formulated bioadhesive buccal films and studied the respective drug pharmacokinetics. Different bioadhesive films were prepared (40, 80, 120, 160, 200, and 2...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8471814/ https://www.ncbi.nlm.nih.gov/pubmed/34564476 http://dx.doi.org/10.3390/membranes11090659 |
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author | Mady, Omar Y. Abulmeaty, Mahmoud M. A. Donia, Ahmed A. Al-Khureif, Abdulaziz A. Al-Shoubki, Adam A. Abudawood, Manal Abdel Moety, Doaa A. |
author_facet | Mady, Omar Y. Abulmeaty, Mahmoud M. A. Donia, Ahmed A. Al-Khureif, Abdulaziz A. Al-Shoubki, Adam A. Abudawood, Manal Abdel Moety, Doaa A. |
author_sort | Mady, Omar Y. |
collection | PubMed |
description | Candesartan cilexetil (CC) is an antihypertensive drug. It has low solubility and faces hepatic first-pass metabolism after oral ingestion. We formulated bioadhesive buccal films and studied the respective drug pharmacokinetics. Different bioadhesive films were prepared (40, 80, 120, 160, 200, and 240 mg CC per film) by using the solvent casting method. The drug concentrations used affect the drug entrapment mechanism, which was reflected in the film physicochemical properties like thickness, weight, drug content, bioadhesion, and drug release. Low drug concentration (F2, 40 mg per film) led to minute drug crystal dispersion while increasing the drug concentration (F7, 240 mg per film) showed drug crystal encapsulation, which affects the drug release. The drug pharmacokinetic from the prepared films was studied compared to the oral form by serial blood sampling via an inserted catheter in the carotid of rats. High-Performance Liquid Chromatography assay was used to measure the plasma concentration of CC in different forms. Compared to other films, the F2 showed the highest maximal concentration (Cmax) and the lowest elimination half-life (t(1/2)). Bioadhesion buccal film of CC has better bioavailability, especially at low concentrations. The ease, robustness, and ruggedness of the preparation suggests the same procedure for drugs like CC. |
format | Online Article Text |
id | pubmed-8471814 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-84718142021-09-28 Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats Mady, Omar Y. Abulmeaty, Mahmoud M. A. Donia, Ahmed A. Al-Khureif, Abdulaziz A. Al-Shoubki, Adam A. Abudawood, Manal Abdel Moety, Doaa A. Membranes (Basel) Article Candesartan cilexetil (CC) is an antihypertensive drug. It has low solubility and faces hepatic first-pass metabolism after oral ingestion. We formulated bioadhesive buccal films and studied the respective drug pharmacokinetics. Different bioadhesive films were prepared (40, 80, 120, 160, 200, and 240 mg CC per film) by using the solvent casting method. The drug concentrations used affect the drug entrapment mechanism, which was reflected in the film physicochemical properties like thickness, weight, drug content, bioadhesion, and drug release. Low drug concentration (F2, 40 mg per film) led to minute drug crystal dispersion while increasing the drug concentration (F7, 240 mg per film) showed drug crystal encapsulation, which affects the drug release. The drug pharmacokinetic from the prepared films was studied compared to the oral form by serial blood sampling via an inserted catheter in the carotid of rats. High-Performance Liquid Chromatography assay was used to measure the plasma concentration of CC in different forms. Compared to other films, the F2 showed the highest maximal concentration (Cmax) and the lowest elimination half-life (t(1/2)). Bioadhesion buccal film of CC has better bioavailability, especially at low concentrations. The ease, robustness, and ruggedness of the preparation suggests the same procedure for drugs like CC. MDPI 2021-08-26 /pmc/articles/PMC8471814/ /pubmed/34564476 http://dx.doi.org/10.3390/membranes11090659 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 Mady, Omar Y. Abulmeaty, Mahmoud M. A. Donia, Ahmed A. Al-Khureif, Abdulaziz A. Al-Shoubki, Adam A. Abudawood, Manal Abdel Moety, Doaa A. Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats |
title | Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats |
title_full | Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats |
title_fullStr | Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats |
title_full_unstemmed | Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats |
title_short | Formulation and Bioavailability of Novel Mucoadhesive Buccal Films for Candesartan Cilexetil in Rats |
title_sort | formulation and bioavailability of novel mucoadhesive buccal films for candesartan cilexetil in rats |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8471814/ https://www.ncbi.nlm.nih.gov/pubmed/34564476 http://dx.doi.org/10.3390/membranes11090659 |
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