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Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Apigenin (APG) is a poorly soluble bioactive compound/nutraceutical which shows poor bioavailability upon oral administration. Hence, the objective of this research work was to develop APG solid dispersions (SDs) using different techniques with the expectation to obtain improvement in its in vitro d...

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Autores principales: Alshehri, Sultan M., Shakeel, Faiyaz, Ibrahim, Mohamed A., Elzayat, Ehab M., Altamimi, Mohammad, Mohsin, Kazi, Almeanazel, Osaid T., Alkholief, Musaed, Alshetaili, Abdullah, Alsulays, Bader, Alanazi, Fars K., Alsarra, Ibrahim A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6362180/
https://www.ncbi.nlm.nih.gov/pubmed/30766439
http://dx.doi.org/10.1016/j.jsps.2018.11.008
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author Alshehri, Sultan M.
Shakeel, Faiyaz
Ibrahim, Mohamed A.
Elzayat, Ehab M.
Altamimi, Mohammad
Mohsin, Kazi
Almeanazel, Osaid T.
Alkholief, Musaed
Alshetaili, Abdullah
Alsulays, Bader
Alanazi, Fars K.
Alsarra, Ibrahim A.
author_facet Alshehri, Sultan M.
Shakeel, Faiyaz
Ibrahim, Mohamed A.
Elzayat, Ehab M.
Altamimi, Mohammad
Mohsin, Kazi
Almeanazel, Osaid T.
Alkholief, Musaed
Alshetaili, Abdullah
Alsulays, Bader
Alanazi, Fars K.
Alsarra, Ibrahim A.
author_sort Alshehri, Sultan M.
collection PubMed
description Apigenin (APG) is a poorly soluble bioactive compound/nutraceutical which shows poor bioavailability upon oral administration. Hence, the objective of this research work was to develop APG solid dispersions (SDs) using different techniques with the expectation to obtain improvement in its in vitro dissolution rate and in vivo bioavailability upon oral administration. Different SDs of APG were prepared by microwave, melted and kneaded technology using pluronic-F127 (PL) as a carrier. Prepared SDs were characterized using “thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infra-red (FTIR) spectrometer, powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM)”. After characterization, prepared SDs of APG were studied for in vitro drug release/dissolution profile and in vivo pharmacokinetic studies. The results of TGA, DSC, FTIR, PXRD and SEM indicated successful formation of APG SDs. In vitro dissolution experiments suggested significant release of APG from all SDs (67.39–84.13%) in comparison with control (32.74%). Optimized SD of APG from each technology was subjected to in vivo pharmacokinetic study in rats. The results indicated significant improvement in oral absorption of APG from SD prepared using microwave and melted technology in comparison with pure drug and commercial capsule. The enhancement in oral bioavailability of APG from microwave SD (319.19%) was 3.19 fold as compared with marketed capsule (100.00%). Significant enhancement in the dissolution rate and oral absorption of APG from SD suggested that developed SD systems can be successfully used for oral drug delivery system of APG.
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spelling pubmed-63621802019-02-14 Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques Alshehri, Sultan M. Shakeel, Faiyaz Ibrahim, Mohamed A. Elzayat, Ehab M. Altamimi, Mohammad Mohsin, Kazi Almeanazel, Osaid T. Alkholief, Musaed Alshetaili, Abdullah Alsulays, Bader Alanazi, Fars K. Alsarra, Ibrahim A. Saudi Pharm J Original Article Apigenin (APG) is a poorly soluble bioactive compound/nutraceutical which shows poor bioavailability upon oral administration. Hence, the objective of this research work was to develop APG solid dispersions (SDs) using different techniques with the expectation to obtain improvement in its in vitro dissolution rate and in vivo bioavailability upon oral administration. Different SDs of APG were prepared by microwave, melted and kneaded technology using pluronic-F127 (PL) as a carrier. Prepared SDs were characterized using “thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infra-red (FTIR) spectrometer, powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM)”. After characterization, prepared SDs of APG were studied for in vitro drug release/dissolution profile and in vivo pharmacokinetic studies. The results of TGA, DSC, FTIR, PXRD and SEM indicated successful formation of APG SDs. In vitro dissolution experiments suggested significant release of APG from all SDs (67.39–84.13%) in comparison with control (32.74%). Optimized SD of APG from each technology was subjected to in vivo pharmacokinetic study in rats. The results indicated significant improvement in oral absorption of APG from SD prepared using microwave and melted technology in comparison with pure drug and commercial capsule. The enhancement in oral bioavailability of APG from microwave SD (319.19%) was 3.19 fold as compared with marketed capsule (100.00%). Significant enhancement in the dissolution rate and oral absorption of APG from SD suggested that developed SD systems can be successfully used for oral drug delivery system of APG. Elsevier 2019-02 2018-11-14 /pmc/articles/PMC6362180/ /pubmed/30766439 http://dx.doi.org/10.1016/j.jsps.2018.11.008 Text en © 2018 The Authors https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Alshehri, Sultan M.
Shakeel, Faiyaz
Ibrahim, Mohamed A.
Elzayat, Ehab M.
Altamimi, Mohammad
Mohsin, Kazi
Almeanazel, Osaid T.
Alkholief, Musaed
Alshetaili, Abdullah
Alsulays, Bader
Alanazi, Fars K.
Alsarra, Ibrahim A.
Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques
title Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques
title_full Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques
title_fullStr Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques
title_full_unstemmed Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques
title_short Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques
title_sort dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6362180/
https://www.ncbi.nlm.nih.gov/pubmed/30766439
http://dx.doi.org/10.1016/j.jsps.2018.11.008
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