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Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies

The purpose of the present work was to prepare buccal adhesive tablets of miconazole nitrate. The simplex centroid experimental design was used to arrive at optimum ratio of carbopol 934P, hydroxypropylmethylcellulose K4M and polyvinylpyrollidone, which will provide desired drug release and mucoadhe...

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Autores principales: Madgulkar, A., Kadam, S., Pokharkar, V.
Formato: Texto
Lenguaje:English
Publicado: Medknow Publications 2009
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2865788/
https://www.ncbi.nlm.nih.gov/pubmed/20490296
http://dx.doi.org/10.4103/0250-474X.56032
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author Madgulkar, A.
Kadam, S.
Pokharkar, V.
author_facet Madgulkar, A.
Kadam, S.
Pokharkar, V.
author_sort Madgulkar, A.
collection PubMed
description The purpose of the present work was to prepare buccal adhesive tablets of miconazole nitrate. The simplex centroid experimental design was used to arrive at optimum ratio of carbopol 934P, hydroxypropylmethylcellulose K4M and polyvinylpyrollidone, which will provide desired drug release and mucoadhesion. Swelling index, mucoadhesive strength and in vitro drug release of the prepared tablet was determined. The drug release and bioadhesion was dependent on type and relative amounts of the polymers. The optimized combination was subjected to in vitro antifungal activity, transmucosal permeation, drug deposition in mucosa, residence time and bioadhesion studies. IR spectroscopy was used to investigate any interaction between drug and excipients. Dissolution of miconazole from tablets was sustained for 6 h. based on the results obtained, it can be concluded that the prepared slow release buccoadhesive tablets of miconazole would markedly prolong the duration of antifungal activity. Comparison of in vitro antifungal activity of tablet with marketed gel showed that drug concentrations above the minimum inhibitory concentration were achieved immediately from both formulations but release from tablet was sustained up to 6 h, while the gel showed initially fast drug release, which did not sustain later. Drug permeation across buccal mucosa was minimum from the tablet as well as marketed gel; the deposition of drug in mucosa was higher in case of tablet. In vitro residence time and bioadhesive strength of tablet was higher than gel. Thus the buccoadhesive tablet of miconazole nitrate may offer better control of antifungal activity as compared to the gel formulation.
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spelling pubmed-28657882010-05-20 Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies Madgulkar, A. Kadam, S. Pokharkar, V. Indian J Pharm Sci Research Paper The purpose of the present work was to prepare buccal adhesive tablets of miconazole nitrate. The simplex centroid experimental design was used to arrive at optimum ratio of carbopol 934P, hydroxypropylmethylcellulose K4M and polyvinylpyrollidone, which will provide desired drug release and mucoadhesion. Swelling index, mucoadhesive strength and in vitro drug release of the prepared tablet was determined. The drug release and bioadhesion was dependent on type and relative amounts of the polymers. The optimized combination was subjected to in vitro antifungal activity, transmucosal permeation, drug deposition in mucosa, residence time and bioadhesion studies. IR spectroscopy was used to investigate any interaction between drug and excipients. Dissolution of miconazole from tablets was sustained for 6 h. based on the results obtained, it can be concluded that the prepared slow release buccoadhesive tablets of miconazole would markedly prolong the duration of antifungal activity. Comparison of in vitro antifungal activity of tablet with marketed gel showed that drug concentrations above the minimum inhibitory concentration were achieved immediately from both formulations but release from tablet was sustained up to 6 h, while the gel showed initially fast drug release, which did not sustain later. Drug permeation across buccal mucosa was minimum from the tablet as well as marketed gel; the deposition of drug in mucosa was higher in case of tablet. In vitro residence time and bioadhesive strength of tablet was higher than gel. Thus the buccoadhesive tablet of miconazole nitrate may offer better control of antifungal activity as compared to the gel formulation. Medknow Publications 2009 /pmc/articles/PMC2865788/ /pubmed/20490296 http://dx.doi.org/10.4103/0250-474X.56032 Text en © Indian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Madgulkar, A.
Kadam, S.
Pokharkar, V.
Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies
title Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies
title_full Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies
title_fullStr Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies
title_full_unstemmed Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies
title_short Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies
title_sort development of buccal adhesive tablet with prolonged antifungal activity: optimization and ex vivo deposition studies
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2865788/
https://www.ncbi.nlm.nih.gov/pubmed/20490296
http://dx.doi.org/10.4103/0250-474X.56032
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