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Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability
The majority of drugs have a low dissolution rate, which is a limiting step for their absorption. In this manuscript, solid dispersions (SD), solid self-microemulsifying drug delivery systems (S-SMEDDS) and solid self-nanoemulsifying drug delivery systems (S-SNEDDS) were evaluated as potential formu...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6331904/ https://www.ncbi.nlm.nih.gov/pubmed/26287134 http://dx.doi.org/10.3390/molecules200814684 |
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author | Krstić, Marko Popović, Miljana Dobričić, Vladimir Ibrić, Svetlana |
author_facet | Krstić, Marko Popović, Miljana Dobričić, Vladimir Ibrić, Svetlana |
author_sort | Krstić, Marko |
collection | PubMed |
description | The majority of drugs have a low dissolution rate, which is a limiting step for their absorption. In this manuscript, solid dispersions (SD), solid self-microemulsifying drug delivery systems (S-SMEDDS) and solid self-nanoemulsifying drug delivery systems (S-SNEDDS) were evaluated as potential formulation strategies to increase the dissolution rate of carbamazepine. Influence of increased dissolution rate on permeability of carbamazepine was evaluated using PAMPA test. In S-SMEDDS and S-SNEDDS formulations, the ratio of liquid SMEDDS/SNEDDS and solid carrier (Neusilin(®) UFL2) was varied, and carbamazepine content was constant. In SD formulations, the ratio of carbamazepine and Neusilin(®) UFL2, was varied. Formulations that showed the best dissolution rate of carbamazepine (SD_1:6, SMEDDS_1:1, SNEDDS_1:6) were mutually compared, characterization of these formulations was performed by DSC, PXRD and FT-IR analyses, and a PAMPA test was done. All formulations have shown a significant increase in dissolution rate compared to pure carbamazepine and immediate-release carbamazepine tablets. Formulation S-SMEDDS_1:1 showed the fastest release rate and permeability of carbamazepine. DSC, PXRD and FT-IR analyses confirmed that in S-SMEDDS and S-SNEDDS carbamazepine remained in polymorph form III, and that it was converted to an amorphous state in SD formulations. All formulations showed increased permeability of carbamazepine, compared to pure carbamazepine. |
format | Online Article Text |
id | pubmed-6331904 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-63319042019-01-24 Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability Krstić, Marko Popović, Miljana Dobričić, Vladimir Ibrić, Svetlana Molecules Article The majority of drugs have a low dissolution rate, which is a limiting step for their absorption. In this manuscript, solid dispersions (SD), solid self-microemulsifying drug delivery systems (S-SMEDDS) and solid self-nanoemulsifying drug delivery systems (S-SNEDDS) were evaluated as potential formulation strategies to increase the dissolution rate of carbamazepine. Influence of increased dissolution rate on permeability of carbamazepine was evaluated using PAMPA test. In S-SMEDDS and S-SNEDDS formulations, the ratio of liquid SMEDDS/SNEDDS and solid carrier (Neusilin(®) UFL2) was varied, and carbamazepine content was constant. In SD formulations, the ratio of carbamazepine and Neusilin(®) UFL2, was varied. Formulations that showed the best dissolution rate of carbamazepine (SD_1:6, SMEDDS_1:1, SNEDDS_1:6) were mutually compared, characterization of these formulations was performed by DSC, PXRD and FT-IR analyses, and a PAMPA test was done. All formulations have shown a significant increase in dissolution rate compared to pure carbamazepine and immediate-release carbamazepine tablets. Formulation S-SMEDDS_1:1 showed the fastest release rate and permeability of carbamazepine. DSC, PXRD and FT-IR analyses confirmed that in S-SMEDDS and S-SNEDDS carbamazepine remained in polymorph form III, and that it was converted to an amorphous state in SD formulations. All formulations showed increased permeability of carbamazepine, compared to pure carbamazepine. MDPI 2015-08-13 /pmc/articles/PMC6331904/ /pubmed/26287134 http://dx.doi.org/10.3390/molecules200814684 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Krstić, Marko Popović, Miljana Dobričić, Vladimir Ibrić, Svetlana Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability |
title | Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability |
title_full | Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability |
title_fullStr | Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability |
title_full_unstemmed | Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability |
title_short | Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability |
title_sort | influence of solid drug delivery system formulation on poorly water-soluble drug dissolution and permeability |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6331904/ https://www.ncbi.nlm.nih.gov/pubmed/26287134 http://dx.doi.org/10.3390/molecules200814684 |
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