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The quest for targeted delivery in colon cancer: mucoadhesive valdecoxib microspheres
The aim of the present study was to prepare valdecoxib, a cyclo-oxygenase-2 enzyme inhibitor, as a loaded multiparticulate system to achieve site-specific drug delivery to colorectal tumors. Film coating was done with the pH-sensitive polymer Eudragit S100 and sodium alginate was used as mucoadhesiv...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2011
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3124854/ https://www.ncbi.nlm.nih.gov/pubmed/21720517 http://dx.doi.org/10.2147/IJN.S19561 |
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author | Thakral, Naveen K Ray, Alok R Bar-Shalom, Daniel Eriksson, André Huss Majumdar, Dipak K |
author_facet | Thakral, Naveen K Ray, Alok R Bar-Shalom, Daniel Eriksson, André Huss Majumdar, Dipak K |
author_sort | Thakral, Naveen K |
collection | PubMed |
description | The aim of the present study was to prepare valdecoxib, a cyclo-oxygenase-2 enzyme inhibitor, as a loaded multiparticulate system to achieve site-specific drug delivery to colorectal tumors. Film coating was done with the pH-sensitive polymer Eudragit S100 and sodium alginate was used as mucoadhesive polymer in the core. The microspheres were characterized by X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy and were evaluated for particle size, drug load, in vitro drug release, release kinetics, accelerated stability, and extent of mucoadhesion. The coated microspheres released the drug at pH 7.4, the putative parameter for colonic delivery. When applied to the mucosal surface of freshly excised goat colon, microspheres pretreated with phosphate buffer pH 7.4 for 30 minutes showed mucoadhesion. To ascertain the effect of valdecoxib on the viability of Caco-2 cells, the 3-(4,5-dimethylthiazol-2yl) 2,5-diphenyltetrazolium bromide) test was conducted using both valdecoxib and coated microspheres. In both cases, the percentage of dehydrogenase activity indicated a lack of toxicity against Caco-2 cells in the tested concentration range. Drug transport studies of the drug as well as the coated microspheres in buffers of pH 6 and 7.4 across Caco-2 cell monolayers were conducted. The microspheres were found to exhibit slower and delayed drug release and lower intracellular concentration of valdecoxib. |
format | Online Article Text |
id | pubmed-3124854 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-31248542011-06-29 The quest for targeted delivery in colon cancer: mucoadhesive valdecoxib microspheres Thakral, Naveen K Ray, Alok R Bar-Shalom, Daniel Eriksson, André Huss Majumdar, Dipak K Int J Nanomedicine Original Research The aim of the present study was to prepare valdecoxib, a cyclo-oxygenase-2 enzyme inhibitor, as a loaded multiparticulate system to achieve site-specific drug delivery to colorectal tumors. Film coating was done with the pH-sensitive polymer Eudragit S100 and sodium alginate was used as mucoadhesive polymer in the core. The microspheres were characterized by X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy and were evaluated for particle size, drug load, in vitro drug release, release kinetics, accelerated stability, and extent of mucoadhesion. The coated microspheres released the drug at pH 7.4, the putative parameter for colonic delivery. When applied to the mucosal surface of freshly excised goat colon, microspheres pretreated with phosphate buffer pH 7.4 for 30 minutes showed mucoadhesion. To ascertain the effect of valdecoxib on the viability of Caco-2 cells, the 3-(4,5-dimethylthiazol-2yl) 2,5-diphenyltetrazolium bromide) test was conducted using both valdecoxib and coated microspheres. In both cases, the percentage of dehydrogenase activity indicated a lack of toxicity against Caco-2 cells in the tested concentration range. Drug transport studies of the drug as well as the coated microspheres in buffers of pH 6 and 7.4 across Caco-2 cell monolayers were conducted. The microspheres were found to exhibit slower and delayed drug release and lower intracellular concentration of valdecoxib. Dove Medical Press 2011 2011-05-19 /pmc/articles/PMC3124854/ /pubmed/21720517 http://dx.doi.org/10.2147/IJN.S19561 Text en © 2011 Thakral et al, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited. |
spellingShingle | Original Research Thakral, Naveen K Ray, Alok R Bar-Shalom, Daniel Eriksson, André Huss Majumdar, Dipak K The quest for targeted delivery in colon cancer: mucoadhesive valdecoxib microspheres |
title | The quest for targeted delivery in colon cancer: mucoadhesive
valdecoxib microspheres |
title_full | The quest for targeted delivery in colon cancer: mucoadhesive
valdecoxib microspheres |
title_fullStr | The quest for targeted delivery in colon cancer: mucoadhesive
valdecoxib microspheres |
title_full_unstemmed | The quest for targeted delivery in colon cancer: mucoadhesive
valdecoxib microspheres |
title_short | The quest for targeted delivery in colon cancer: mucoadhesive
valdecoxib microspheres |
title_sort | quest for targeted delivery in colon cancer: mucoadhesive
valdecoxib microspheres |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3124854/ https://www.ncbi.nlm.nih.gov/pubmed/21720517 http://dx.doi.org/10.2147/IJN.S19561 |
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