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Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion

BACKGROUND: Baicalin is the main bioactive constitute of the dried roots of Scutellaria baicalensis and possesses various biological activities. However, the poor water solubility and low oral bioavailability limit its efficacy. OBJECTIVE: The present study was conducted to enhance the dissolution a...

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Autores principales: Cui, Li, Sune, E, Song, Jie, Wang, Jing, Jia, Xiao-bin, Zhang, Zhen-hai
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5096281/
https://www.ncbi.nlm.nih.gov/pubmed/27867277
http://dx.doi.org/10.4103/0973-1296.192199
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author Cui, Li
Sune, E
Song, Jie
Wang, Jing
Jia, Xiao-bin
Zhang, Zhen-hai
author_facet Cui, Li
Sune, E
Song, Jie
Wang, Jing
Jia, Xiao-bin
Zhang, Zhen-hai
author_sort Cui, Li
collection PubMed
description BACKGROUND: Baicalin is the main bioactive constitute of the dried roots of Scutellaria baicalensis and possesses various biological activities. However, the poor water solubility and low oral bioavailability limit its efficacy. OBJECTIVE: The present study was conducted to enhance the dissolution and oral bioavailability of baicalin (BA) through a novel mesoporous carbon nanopowder (MCN) drug carrier. MATERIALS AND METHODS: Solid dispersions (SDs) of BA with MCN were prepared using a solvent evaporation method. The physical state of the formulations was investigated using SEM, differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). The pharmaceutical performance of pure BA, physical mixture (PM) and SDs was evaluated by performing an in-vitro dissolution test. The pharmacokinetic studies were conducted in SD rats and the analysis of the biological samples was performed on an Acquity UPLC–MS system. The intestinal and renal toxicity test of MCN was also evaluated. RESULTS: The drug release profile indicated that the BA dissolution rate from SDs with a BA/MCN ratio of 1:6 greatly increased in comparison with that of the pure crystalline drug. Furthermore, a pharmacokinetic analysis in rats showed that the BA area under the concentration–time curve for SDs of MCN/BA was 1.83 times larger than that of pure BA. In comparison with the pure drug, the MCN–BA system significantly shortened the time to T(max) and generated higher C(max). There was no intestinal and renal toxicity of MCN. CONCLUSION: These results indicated that the oral bioavailability of BA was remarkably improved by the MCN carrier. Additionally, intestinal toxicity test showed that MCN produced no toxicity in the gastrointestinal tract. Our results show that MCN-based SDs could be used to enhance the bioavailability of drugs with poor water solubility. SUMMARY: The drug release profile indicated that the BA dissolution rate from SDs with a BA/MCN ratio of 1:6 greatly increased in comparison with that of the pure crystalline drug. Furthermore, a pharmacokinetic analysis in rats showed that the BA area under the concentration–time curve for SDs of MCN/BA was 1.83 times larger than that of pure BA. In comparison with the pure drug, the MCN–BA system significantly shortened the time to T(max) and generated higher C(max.) Abbreviations used: BA: baicalin, MCN: mesoporous carbon nanopowder, SDs: solid dispersions, SEM: scanning electron microscopy, DSC: differential scanning calorimetry, XRD: powder X-ray diffraction, HPLC: high-performance liquid chromatography, PM: physical mixture, S.D.: standard deviation, ANOVA: analysis of variance, RSD: relative standard deviation, ESI: electrospray ionization, IS: internal standard, MRM: multiple reaction monitoring
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spelling pubmed-50962812016-11-18 Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion Cui, Li Sune, E Song, Jie Wang, Jing Jia, Xiao-bin Zhang, Zhen-hai Pharmacogn Mag Original Article BACKGROUND: Baicalin is the main bioactive constitute of the dried roots of Scutellaria baicalensis and possesses various biological activities. However, the poor water solubility and low oral bioavailability limit its efficacy. OBJECTIVE: The present study was conducted to enhance the dissolution and oral bioavailability of baicalin (BA) through a novel mesoporous carbon nanopowder (MCN) drug carrier. MATERIALS AND METHODS: Solid dispersions (SDs) of BA with MCN were prepared using a solvent evaporation method. The physical state of the formulations was investigated using SEM, differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). The pharmaceutical performance of pure BA, physical mixture (PM) and SDs was evaluated by performing an in-vitro dissolution test. The pharmacokinetic studies were conducted in SD rats and the analysis of the biological samples was performed on an Acquity UPLC–MS system. The intestinal and renal toxicity test of MCN was also evaluated. RESULTS: The drug release profile indicated that the BA dissolution rate from SDs with a BA/MCN ratio of 1:6 greatly increased in comparison with that of the pure crystalline drug. Furthermore, a pharmacokinetic analysis in rats showed that the BA area under the concentration–time curve for SDs of MCN/BA was 1.83 times larger than that of pure BA. In comparison with the pure drug, the MCN–BA system significantly shortened the time to T(max) and generated higher C(max). There was no intestinal and renal toxicity of MCN. CONCLUSION: These results indicated that the oral bioavailability of BA was remarkably improved by the MCN carrier. Additionally, intestinal toxicity test showed that MCN produced no toxicity in the gastrointestinal tract. Our results show that MCN-based SDs could be used to enhance the bioavailability of drugs with poor water solubility. SUMMARY: The drug release profile indicated that the BA dissolution rate from SDs with a BA/MCN ratio of 1:6 greatly increased in comparison with that of the pure crystalline drug. Furthermore, a pharmacokinetic analysis in rats showed that the BA area under the concentration–time curve for SDs of MCN/BA was 1.83 times larger than that of pure BA. In comparison with the pure drug, the MCN–BA system significantly shortened the time to T(max) and generated higher C(max.) Abbreviations used: BA: baicalin, MCN: mesoporous carbon nanopowder, SDs: solid dispersions, SEM: scanning electron microscopy, DSC: differential scanning calorimetry, XRD: powder X-ray diffraction, HPLC: high-performance liquid chromatography, PM: physical mixture, S.D.: standard deviation, ANOVA: analysis of variance, RSD: relative standard deviation, ESI: electrospray ionization, IS: internal standard, MRM: multiple reaction monitoring Medknow Publications & Media Pvt Ltd 2016 /pmc/articles/PMC5096281/ /pubmed/27867277 http://dx.doi.org/10.4103/0973-1296.192199 Text en Copyright: © Pharmacognosy Magazine http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.
spellingShingle Original Article
Cui, Li
Sune, E
Song, Jie
Wang, Jing
Jia, Xiao-bin
Zhang, Zhen-hai
Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion
title Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion
title_full Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion
title_fullStr Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion
title_full_unstemmed Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion
title_short Characterization and Bioavailability Study of Baicalin-mesoporous Carbon Nanopowder Solid Dispersion
title_sort characterization and bioavailability study of baicalin-mesoporous carbon nanopowder solid dispersion
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5096281/
https://www.ncbi.nlm.nih.gov/pubmed/27867277
http://dx.doi.org/10.4103/0973-1296.192199
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