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...

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Autores principales: Nakarani, M., Misra, A.K., Patel, J.K., Vaghani, S.S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Tehran University of Medical Sciences 2010
Materias:
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.
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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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