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SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs

(1) Background: Numerous oral drugs exhibit limited bioavailability due to their poor solubility and poor intestinal permeability. The smartFilm technology is an innovative approach that improves the drug aqueous solubility via incorporating the drug in an amorphous state into a cellulose-based matr...

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Autores principales: Abdelkader, Ayat, Preis, Eduard, Keck, Cornelia M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9500710/
https://www.ncbi.nlm.nih.gov/pubmed/36145666
http://dx.doi.org/10.3390/pharmaceutics14091918
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author Abdelkader, Ayat
Preis, Eduard
Keck, Cornelia M.
author_facet Abdelkader, Ayat
Preis, Eduard
Keck, Cornelia M.
author_sort Abdelkader, Ayat
collection PubMed
description (1) Background: Numerous oral drugs exhibit limited bioavailability due to their poor solubility and poor intestinal permeability. The smartFilm technology is an innovative approach that improves the drug aqueous solubility via incorporating the drug in an amorphous state into a cellulose-based matrix, i.e., paper. smartFilms can be transformed into a free-flowing physical form (i.e., paper granules) that can be compressed into tablets with optimum physico-chemical and pharmaceutical properties. The aim of this study was to investigate if smartFilm tablets are suitable for improved oral delivery of poorly water-soluble drugs. (2) Methods: Curcumin is a poorly soluble drug with low intestinal permeability and was used for the production of curcumin-loaded smartFilms. The curcumin-loaded smartFilms were transferred into smartFilm granules which were then compressed into curcumin-loaded smartFilm tablets. The tablets were characterized regarding their physico-chemical and pharmaceutical properties, and the intestinal permeability of curcumin was determined with the ex vivo porcine intestinal model. The ex vivo intestinal permeability of curcumin from the smartFilm tablets was compared to a physical mixture of curcumin and paper and to a classical and to an innovative commercial product, respectively. (3) Results: The produced curcumin-loaded smartFilm tablets fulfilled the European Pharmacopoeia requirements, incorporated curcumin in amorphous state within the cellulose matrix and exhibited an enhanced dissolution rate. The ex vivo intestinal permeation data were shown to correlate to the in vitro dissolution data. The ex vivo intestinal permeation of curcumin from the smartFilm tablets was about two-fold higher when compared to the physical mixture and the classical commercial product. No differences in the ex vivo bioavailability were found between the smartFilm tablets and the innovative commercial product. (4) Conclusions: smartFilm tablets are a cost-effective and industrially feasible formulation approach for the formulation of poorly water-soluble drugs, i.e., BCS class II and IV drugs.
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spelling pubmed-95007102022-09-24 SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs Abdelkader, Ayat Preis, Eduard Keck, Cornelia M. Pharmaceutics Article (1) Background: Numerous oral drugs exhibit limited bioavailability due to their poor solubility and poor intestinal permeability. The smartFilm technology is an innovative approach that improves the drug aqueous solubility via incorporating the drug in an amorphous state into a cellulose-based matrix, i.e., paper. smartFilms can be transformed into a free-flowing physical form (i.e., paper granules) that can be compressed into tablets with optimum physico-chemical and pharmaceutical properties. The aim of this study was to investigate if smartFilm tablets are suitable for improved oral delivery of poorly water-soluble drugs. (2) Methods: Curcumin is a poorly soluble drug with low intestinal permeability and was used for the production of curcumin-loaded smartFilms. The curcumin-loaded smartFilms were transferred into smartFilm granules which were then compressed into curcumin-loaded smartFilm tablets. The tablets were characterized regarding their physico-chemical and pharmaceutical properties, and the intestinal permeability of curcumin was determined with the ex vivo porcine intestinal model. The ex vivo intestinal permeability of curcumin from the smartFilm tablets was compared to a physical mixture of curcumin and paper and to a classical and to an innovative commercial product, respectively. (3) Results: The produced curcumin-loaded smartFilm tablets fulfilled the European Pharmacopoeia requirements, incorporated curcumin in amorphous state within the cellulose matrix and exhibited an enhanced dissolution rate. The ex vivo intestinal permeation data were shown to correlate to the in vitro dissolution data. The ex vivo intestinal permeation of curcumin from the smartFilm tablets was about two-fold higher when compared to the physical mixture and the classical commercial product. No differences in the ex vivo bioavailability were found between the smartFilm tablets and the innovative commercial product. (4) Conclusions: smartFilm tablets are a cost-effective and industrially feasible formulation approach for the formulation of poorly water-soluble drugs, i.e., BCS class II and IV drugs. MDPI 2022-09-10 /pmc/articles/PMC9500710/ /pubmed/36145666 http://dx.doi.org/10.3390/pharmaceutics14091918 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
Abdelkader, Ayat
Preis, Eduard
Keck, Cornelia M.
SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs
title SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs
title_full SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs
title_fullStr SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs
title_full_unstemmed SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs
title_short SmartFilm Tablets for Improved Oral Delivery of Poorly Soluble Drugs
title_sort smartfilm tablets for improved oral delivery of poorly soluble drugs
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9500710/
https://www.ncbi.nlm.nih.gov/pubmed/36145666
http://dx.doi.org/10.3390/pharmaceutics14091918
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