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Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery
Purpose: The goal of the present study is to develop polymeric matrix films loaded with a combination of free diclofenac sodium (DFS(free)) and DFS:Ion exchange resin complexes (DFS:IR) for immediate and sustained release profiles, respectively. Methods: Effect of ratio of DFS and IR on the DFS:IR c...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8253122/ https://www.ncbi.nlm.nih.gov/pubmed/28165833 http://dx.doi.org/10.1080/10717544.2016.1256000 |
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author | Adelli, Goutham R. Balguri, Sai Prachetan Bhagav, Prakash Raman, Vijayasankar Majumdar, Soumyajit |
author_facet | Adelli, Goutham R. Balguri, Sai Prachetan Bhagav, Prakash Raman, Vijayasankar Majumdar, Soumyajit |
author_sort | Adelli, Goutham R. |
collection | PubMed |
description | Purpose: The goal of the present study is to develop polymeric matrix films loaded with a combination of free diclofenac sodium (DFS(free)) and DFS:Ion exchange resin complexes (DFS:IR) for immediate and sustained release profiles, respectively. Methods: Effect of ratio of DFS and IR on the DFS:IR complexation efficiency was studied using batch processing. DFS:IR complex, DFS(free), or a combination of DFS(free )+( )DFS:IR loaded matrix films were prepared by melt-cast technology. DFS content was 20% w/w in these matrix films. In vitro transcorneal permeability from the film formulations were compared against DFS solution, using a side-by-side diffusion apparatus, over a 6 h period. Ocular disposition of DFS from the solution, films and corresponding suspensions were evaluated in conscious New Zealand albino rabbits, 4 h and 8 h post-topical administration. All in vivo studies were carried out as per the University of Mississippi IACUC approved protocol. Results: Complexation efficiency of DFS:IR was found to be 99% with a 1:1 ratio of DFS:IR. DFS release from DFS:IR suspension and the film were best-fit to a Higuchi model. In vitro transcorneal flux with the DFS(free )+( )DFS:IR((1:1))(1 + 1) was twice that of only DFS:IR((1:1)) film. In vivo, DFS solution and DFS:IR((1:1)) suspension formulations were not able to maintain therapeutic DFS levels in the aqueous humor (AH). Both DFS(free) and DFS(free )+( )DFS:IR((1:1))(3 + 1) loaded matrix films were able to achieve and maintain high DFS concentrations in the AH, but elimination of DFS from the ocular tissues was much faster with the DFS(free) formulation. Conclusion: DFS(free )+( )DFS:IR combination loaded matrix films were able to deliver and maintain therapeutic DFS concentrations in the anterior ocular chamber for up to 8 h. Thus, free drug/IR complex loaded matrix films could be a potential topical ocular delivery platform for achieving immediate and sustained release characteristics. |
format | Online Article Text |
id | pubmed-8253122 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-82531222021-07-13 Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery Adelli, Goutham R. Balguri, Sai Prachetan Bhagav, Prakash Raman, Vijayasankar Majumdar, Soumyajit Drug Deliv Research Article Purpose: The goal of the present study is to develop polymeric matrix films loaded with a combination of free diclofenac sodium (DFS(free)) and DFS:Ion exchange resin complexes (DFS:IR) for immediate and sustained release profiles, respectively. Methods: Effect of ratio of DFS and IR on the DFS:IR complexation efficiency was studied using batch processing. DFS:IR complex, DFS(free), or a combination of DFS(free )+( )DFS:IR loaded matrix films were prepared by melt-cast technology. DFS content was 20% w/w in these matrix films. In vitro transcorneal permeability from the film formulations were compared against DFS solution, using a side-by-side diffusion apparatus, over a 6 h period. Ocular disposition of DFS from the solution, films and corresponding suspensions were evaluated in conscious New Zealand albino rabbits, 4 h and 8 h post-topical administration. All in vivo studies were carried out as per the University of Mississippi IACUC approved protocol. Results: Complexation efficiency of DFS:IR was found to be 99% with a 1:1 ratio of DFS:IR. DFS release from DFS:IR suspension and the film were best-fit to a Higuchi model. In vitro transcorneal flux with the DFS(free )+( )DFS:IR((1:1))(1 + 1) was twice that of only DFS:IR((1:1)) film. In vivo, DFS solution and DFS:IR((1:1)) suspension formulations were not able to maintain therapeutic DFS levels in the aqueous humor (AH). Both DFS(free) and DFS(free )+( )DFS:IR((1:1))(3 + 1) loaded matrix films were able to achieve and maintain high DFS concentrations in the AH, but elimination of DFS from the ocular tissues was much faster with the DFS(free) formulation. Conclusion: DFS(free )+( )DFS:IR combination loaded matrix films were able to deliver and maintain therapeutic DFS concentrations in the anterior ocular chamber for up to 8 h. Thus, free drug/IR complex loaded matrix films could be a potential topical ocular delivery platform for achieving immediate and sustained release characteristics. Taylor & Francis 2017-02-06 /pmc/articles/PMC8253122/ /pubmed/28165833 http://dx.doi.org/10.1080/10717544.2016.1256000 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Adelli, Goutham R. Balguri, Sai Prachetan Bhagav, Prakash Raman, Vijayasankar Majumdar, Soumyajit Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery |
title | Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery |
title_full | Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery |
title_fullStr | Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery |
title_full_unstemmed | Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery |
title_short | Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery |
title_sort | diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8253122/ https://www.ncbi.nlm.nih.gov/pubmed/28165833 http://dx.doi.org/10.1080/10717544.2016.1256000 |
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