Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation
BACKGROUND AND THE PURPOSE OF THE STUDY: Itraconazole is a poorly water soluble drug which results in its insufficient bioavailability. The purpose of the present study was to formulate Itraconazole in a nanosuspension to increase the aqueous solubility and to improve its formulation related paramet...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Tehran University of Medical Sciences
2010
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3304368/ https://www.ncbi.nlm.nih.gov/pubmed/22615599 |
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author | Nakarani, M. Misra, A.K. Patel, J.K. Vaghani, S.S. |
author_facet | Nakarani, M. Misra, A.K. Patel, J.K. Vaghani, S.S. |
author_sort | Nakarani, M. |
collection | PubMed |
description | BACKGROUND AND THE PURPOSE OF THE STUDY: Itraconazole is a poorly water soluble drug which results in its insufficient bioavailability. The purpose of the present study was to formulate Itraconazole in a nanosuspension to increase the aqueous solubility and to improve its formulation related parameters, dissolution and hence oral bioavailability. METHODS: Itraconazole nanosuspension was prepared by pearl milling technique using zirconium oxide beads as a milling media, Poloxamer 407 as a stabilizer and glycerol as a wetting agent. Effects of various process parameters like, stirring time and the ratio of the beads were optimized by keeping drug:surfactant:milling media (1:3.0:50) as a constant initially and then optimized process parameters were used to optimize formulation parameters by 32 factorial designs. The optimized nanosuspension was lyophilized using mannitol (1:1 ratio) as a cryoprotectant. Nanosuspension was characterized by particle size and size distribution, drug content, scanning electron microscopy, differential scanning colorimetry and X-ray diffraction techniques. RESULTS: Optimized nanosuspension showed spherical shape with surface oriented surfactant molecules and a mean particle diameter of 294 nm. There was no significant change in crystalline nature after formulation and it was found to be chemically stable with high drug content. CONCLUSION: The in vitro dissolution profile of the optimized formulation compared to the pure drug and marketed formulation (Canditral Capsule) by using 0.1N Hydrochloric acid as release medium showed higher drug release. |
format | Online Article Text |
id | pubmed-3304368 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2010 |
publisher | Tehran University of Medical Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-33043682012-05-21 Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation Nakarani, M. Misra, A.K. Patel, J.K. Vaghani, S.S. Daru Original Article BACKGROUND AND THE PURPOSE OF THE STUDY: Itraconazole is a poorly water soluble drug which results in its insufficient bioavailability. The purpose of the present study was to formulate Itraconazole in a nanosuspension to increase the aqueous solubility and to improve its formulation related parameters, dissolution and hence oral bioavailability. METHODS: Itraconazole nanosuspension was prepared by pearl milling technique using zirconium oxide beads as a milling media, Poloxamer 407 as a stabilizer and glycerol as a wetting agent. Effects of various process parameters like, stirring time and the ratio of the beads were optimized by keeping drug:surfactant:milling media (1:3.0:50) as a constant initially and then optimized process parameters were used to optimize formulation parameters by 32 factorial designs. The optimized nanosuspension was lyophilized using mannitol (1:1 ratio) as a cryoprotectant. Nanosuspension was characterized by particle size and size distribution, drug content, scanning electron microscopy, differential scanning colorimetry and X-ray diffraction techniques. RESULTS: Optimized nanosuspension showed spherical shape with surface oriented surfactant molecules and a mean particle diameter of 294 nm. There was no significant change in crystalline nature after formulation and it was found to be chemically stable with high drug content. CONCLUSION: The in vitro dissolution profile of the optimized formulation compared to the pure drug and marketed formulation (Canditral Capsule) by using 0.1N Hydrochloric acid as release medium showed higher drug release. Tehran University of Medical Sciences 2010 /pmc/articles/PMC3304368/ /pubmed/22615599 Text en © 2010 Tehran University of Medical Sciences http://creativecommons.org/licenses/by/3.0/ This work is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License which allows users to read, copy, distribute and make derivative works for non-commercial purposes from the material, as long as the author of the original work is cited properly. |
spellingShingle | Original Article Nakarani, M. Misra, A.K. Patel, J.K. Vaghani, S.S. Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation |
title | Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation |
title_full | Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation |
title_fullStr | Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation |
title_full_unstemmed | Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation |
title_short | Itraconazole nanosuspension for oral delivery: Formulation, characterization and in vitro comparison with marketed formulation |
title_sort | itraconazole nanosuspension for oral delivery: formulation, characterization and in vitro comparison with marketed formulation |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3304368/ https://www.ncbi.nlm.nih.gov/pubmed/22615599 |
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