Preparation, characterization and pharmacokinetics of cyadox nanosuspension
Abstract An increase in number of newly developed synthetic drugs displays bioavailability constraints because of poor water solubility. Nanosuspensions formulation may help to overwhelm these problems by increasing dissolution velocity and saturation solubility. In the present study, cyadox (Cyx) n...
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2017
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oai:doaj.org-article:8dfee1f051bd47a78c45c6d9720458752021-12-02T16:06:44ZPreparation, characterization and pharmacokinetics of cyadox nanosuspension10.1038/s41598-017-02523-42045-2322https://doaj.org/article/8dfee1f051bd47a78c45c6d9720458752017-05-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-02523-4https://doaj.org/toc/2045-2322Abstract An increase in number of newly developed synthetic drugs displays bioavailability constraints because of poor water solubility. Nanosuspensions formulation may help to overwhelm these problems by increasing dissolution velocity and saturation solubility. In the present study, cyadox (Cyx) nanosuspension was successfully prepared by recrystallization based on acid–base neutralization combined with high pressure homogenization method using Polyvinylpyrrolidone K30 (PVP) as stabilizer. The nanosuspension had uniform particle distribution, excellent sedimentation rate and redispersibility. The nanosuspension significantly improved the solubility, dissolution and bioavailability. The saturation solubility of Cyx nanocrystal was higher than that of bulk Cyx and released the total drug in very short time. Further, pharmacokinetics of Cyx nanosuspension and normal suspension following oral administration was investigated in beagle dogs. Nanosuspension improved the bioavailability of Cyx which could be beneficial for intestinal bacterial infection in animals. Maximum concentration and area under concentration time curve were increased with particles size reduction which might give rise to pronounce fluctuations in plasma concentration and more intensified antibacterial effects. The terminal half-life and mean resident time of Cyx nanosuspension had also increased compared to normal Cyx suspension. In conclusion, nanosuspensions may be a suitable delivery approach to increase the bioavailability of poorly soluble drugs.Adeel SattarDongmei ChenLishun JiangYuanhu PanYanfei TaoLingli HuangZhenli LiuShuyu XieZonghui YuanNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-9 (2017) |
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Medicine R Science Q Adeel Sattar Dongmei Chen Lishun Jiang Yuanhu Pan Yanfei Tao Lingli Huang Zhenli Liu Shuyu Xie Zonghui Yuan Preparation, characterization and pharmacokinetics of cyadox nanosuspension |
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Abstract An increase in number of newly developed synthetic drugs displays bioavailability constraints because of poor water solubility. Nanosuspensions formulation may help to overwhelm these problems by increasing dissolution velocity and saturation solubility. In the present study, cyadox (Cyx) nanosuspension was successfully prepared by recrystallization based on acid–base neutralization combined with high pressure homogenization method using Polyvinylpyrrolidone K30 (PVP) as stabilizer. The nanosuspension had uniform particle distribution, excellent sedimentation rate and redispersibility. The nanosuspension significantly improved the solubility, dissolution and bioavailability. The saturation solubility of Cyx nanocrystal was higher than that of bulk Cyx and released the total drug in very short time. Further, pharmacokinetics of Cyx nanosuspension and normal suspension following oral administration was investigated in beagle dogs. Nanosuspension improved the bioavailability of Cyx which could be beneficial for intestinal bacterial infection in animals. Maximum concentration and area under concentration time curve were increased with particles size reduction which might give rise to pronounce fluctuations in plasma concentration and more intensified antibacterial effects. The terminal half-life and mean resident time of Cyx nanosuspension had also increased compared to normal Cyx suspension. In conclusion, nanosuspensions may be a suitable delivery approach to increase the bioavailability of poorly soluble drugs. |
format |
article |
author |
Adeel Sattar Dongmei Chen Lishun Jiang Yuanhu Pan Yanfei Tao Lingli Huang Zhenli Liu Shuyu Xie Zonghui Yuan |
author_facet |
Adeel Sattar Dongmei Chen Lishun Jiang Yuanhu Pan Yanfei Tao Lingli Huang Zhenli Liu Shuyu Xie Zonghui Yuan |
author_sort |
Adeel Sattar |
title |
Preparation, characterization and pharmacokinetics of cyadox nanosuspension |
title_short |
Preparation, characterization and pharmacokinetics of cyadox nanosuspension |
title_full |
Preparation, characterization and pharmacokinetics of cyadox nanosuspension |
title_fullStr |
Preparation, characterization and pharmacokinetics of cyadox nanosuspension |
title_full_unstemmed |
Preparation, characterization and pharmacokinetics of cyadox nanosuspension |
title_sort |
preparation, characterization and pharmacokinetics of cyadox nanosuspension |
publisher |
Nature Portfolio |
publishDate |
2017 |
url |
https://doaj.org/article/8dfee1f051bd47a78c45c6d972045875 |
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