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Factorial design-based development of measlamine microspheres for colonic delivery
For treating colonic diseases, conventional oral drug delivery systems are not effective, as they fail to reach the appropriate site of action. Thus, there is a need to develop effective and safe therapy for the treatment of colonic disorders. The aim of the present study was to design a colon-speci...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Landes Bioscience
2011
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3549889/ https://www.ncbi.nlm.nih.gov/pubmed/23507747 http://dx.doi.org/10.4161/biom.18461 |
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author | Jain, Vikas Prasad, Dayal Jain, Deepika Mishra, Santosh Kumar Singh, Ranjit |
author_facet | Jain, Vikas Prasad, Dayal Jain, Deepika Mishra, Santosh Kumar Singh, Ranjit |
author_sort | Jain, Vikas |
collection | PubMed |
description | For treating colonic diseases, conventional oral drug delivery systems are not effective, as they fail to reach the appropriate site of action. Thus, there is a need to develop effective and safe therapy for the treatment of colonic disorders. The aim of the present study was to design a colon-specific delivery system for an anti-inflammatory drug, mesalamine, with minimal degradation and optimum delivery of the drug with relatively higher local concentration, which may provide more effective therapy for inflammatory bowel disease including Crohn disease and ulcerative colitis. Factorial designs (four factors and two levels) for eudragit S-100 (pH-dependent polymer)-coated, pectin (natural polysaccharides)-based microspheres of mesalamine were constructed and conducted in a fully randomized manner to study all possible combinations. Based on the desirability function formulation, F14 was found to be the best formulation. The overall desirability coefficient of formulation F14 was found to be 0.825. The formulation F14 was subjected to in vitro release studies, and the results were evaluated kinetically and statistically. The microspheres started releasing the drug at the beginning of 7th hour, which corresponds to the arrival time at proximal colon. The cumulative percent drug release for formulation F14 at the end of 16 h was found to be 98%. The release kinetics showed that the release followed the Higuchi model, and the main mechanism of drug release was diffusion. The study presents a new approach for colon-specific drug delivery. |
format | Online Article Text |
id | pubmed-3549889 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | Landes Bioscience |
record_format | MEDLINE/PubMed |
spelling | pubmed-35498892013-05-22 Factorial design-based development of measlamine microspheres for colonic delivery Jain, Vikas Prasad, Dayal Jain, Deepika Mishra, Santosh Kumar Singh, Ranjit Biomatter Report For treating colonic diseases, conventional oral drug delivery systems are not effective, as they fail to reach the appropriate site of action. Thus, there is a need to develop effective and safe therapy for the treatment of colonic disorders. The aim of the present study was to design a colon-specific delivery system for an anti-inflammatory drug, mesalamine, with minimal degradation and optimum delivery of the drug with relatively higher local concentration, which may provide more effective therapy for inflammatory bowel disease including Crohn disease and ulcerative colitis. Factorial designs (four factors and two levels) for eudragit S-100 (pH-dependent polymer)-coated, pectin (natural polysaccharides)-based microspheres of mesalamine were constructed and conducted in a fully randomized manner to study all possible combinations. Based on the desirability function formulation, F14 was found to be the best formulation. The overall desirability coefficient of formulation F14 was found to be 0.825. The formulation F14 was subjected to in vitro release studies, and the results were evaluated kinetically and statistically. The microspheres started releasing the drug at the beginning of 7th hour, which corresponds to the arrival time at proximal colon. The cumulative percent drug release for formulation F14 at the end of 16 h was found to be 98%. The release kinetics showed that the release followed the Higuchi model, and the main mechanism of drug release was diffusion. The study presents a new approach for colon-specific drug delivery. Landes Bioscience 2011-10-01 /pmc/articles/PMC3549889/ /pubmed/23507747 http://dx.doi.org/10.4161/biom.18461 Text en Copyright © 2011 Landes Bioscience http://creativecommons.org/licenses/by-nc/3.0/ This is an open-access article licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. The article may be redistributed, reproduced, and reused for non-commercial purposes, provided the original source is properly cited. |
spellingShingle | Report Jain, Vikas Prasad, Dayal Jain, Deepika Mishra, Santosh Kumar Singh, Ranjit Factorial design-based development of measlamine microspheres for colonic delivery |
title | Factorial design-based development of measlamine microspheres for colonic delivery |
title_full | Factorial design-based development of measlamine microspheres for colonic delivery |
title_fullStr | Factorial design-based development of measlamine microspheres for colonic delivery |
title_full_unstemmed | Factorial design-based development of measlamine microspheres for colonic delivery |
title_short | Factorial design-based development of measlamine microspheres for colonic delivery |
title_sort | factorial design-based development of measlamine microspheres for colonic delivery |
topic | Report |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3549889/ https://www.ncbi.nlm.nih.gov/pubmed/23507747 http://dx.doi.org/10.4161/biom.18461 |
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