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Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

PURPOSE: The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate. METHODS: Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyviny...

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Autores principales: Yousaf, Abid Mehmood, Mustapha, Omer, Kim, Dong Wuk, Kim, Dong Shik, Kim, Kyeong Soo, Jin, Sung Giu, Yong, Chul Soon, Youn, Yu Seok, Oh, Yu-Kyoung, Kim, Jong Oh, Choi, Han-Gon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4716746/
https://www.ncbi.nlm.nih.gov/pubmed/26834471
http://dx.doi.org/10.2147/IJN.S97496
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author Yousaf, Abid Mehmood
Mustapha, Omer
Kim, Dong Wuk
Kim, Dong Shik
Kim, Kyeong Soo
Jin, Sung Giu
Yong, Chul Soon
Youn, Yu Seok
Oh, Yu-Kyoung
Kim, Jong Oh
Choi, Han-Gon
author_facet Yousaf, Abid Mehmood
Mustapha, Omer
Kim, Dong Wuk
Kim, Dong Shik
Kim, Kyeong Soo
Jin, Sung Giu
Yong, Chul Soon
Youn, Yu Seok
Oh, Yu-Kyoung
Kim, Jong Oh
Choi, Han-Gon
author_sort Yousaf, Abid Mehmood
collection PubMed
description PURPOSE: The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate. METHODS: Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyvinylpyrrolidone (PVP) and Labrafil(®) M 2125 as carriers using the electrospray technique, and the effect of the carriers on drug solubility and solvation was assessed. The solid state characterization of an optimized formulation was conducted by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopic analyses. Oral bioavailability in rats was also evaluated for the formulation of an optimized nanospherule in comparison with free drug and a conventional fenofibrate-loaded solid dispersion. RESULTS: All of the electrosprayed nanospherule formulations had remarkably enhanced aqueous solubility and dissolution compared with free drug. Moreover, Labrafil M 2125, a surfactant, had a positive influence on the solubility and dissolution of the drug in the electrosprayed nanospherule. Increases were observed as the PVP/drug ratio increased to 4:1, but higher ratios gave no significant increases. In particular, an electrosprayed nanospherule composed of fenofibrate, PVP, and Labrafil M 2125 at the weight ratio of 1:4:0.5 resulted in a particle size of <200 nm with the drug present in the amorphous state. It demonstrated the highest solubility (32.51±2.41 μg/mL), an excellent dissolution (~85% in 10 minutes), and an oral bioavailability ~2.5-fold better than that of the free drug. It showed similar oral bioavailability compared to the conventional solid dispersion. CONCLUSION: Electrosprayed nanospherules, which provide improved solubility and bioavailability, are promising drug delivery tools for oral administration of poorly water-soluble fenofibrate.
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spelling pubmed-47167462016-02-01 Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate Yousaf, Abid Mehmood Mustapha, Omer Kim, Dong Wuk Kim, Dong Shik Kim, Kyeong Soo Jin, Sung Giu Yong, Chul Soon Youn, Yu Seok Oh, Yu-Kyoung Kim, Jong Oh Choi, Han-Gon Int J Nanomedicine Original Research PURPOSE: The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate. METHODS: Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyvinylpyrrolidone (PVP) and Labrafil(®) M 2125 as carriers using the electrospray technique, and the effect of the carriers on drug solubility and solvation was assessed. The solid state characterization of an optimized formulation was conducted by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopic analyses. Oral bioavailability in rats was also evaluated for the formulation of an optimized nanospherule in comparison with free drug and a conventional fenofibrate-loaded solid dispersion. RESULTS: All of the electrosprayed nanospherule formulations had remarkably enhanced aqueous solubility and dissolution compared with free drug. Moreover, Labrafil M 2125, a surfactant, had a positive influence on the solubility and dissolution of the drug in the electrosprayed nanospherule. Increases were observed as the PVP/drug ratio increased to 4:1, but higher ratios gave no significant increases. In particular, an electrosprayed nanospherule composed of fenofibrate, PVP, and Labrafil M 2125 at the weight ratio of 1:4:0.5 resulted in a particle size of <200 nm with the drug present in the amorphous state. It demonstrated the highest solubility (32.51±2.41 μg/mL), an excellent dissolution (~85% in 10 minutes), and an oral bioavailability ~2.5-fold better than that of the free drug. It showed similar oral bioavailability compared to the conventional solid dispersion. CONCLUSION: Electrosprayed nanospherules, which provide improved solubility and bioavailability, are promising drug delivery tools for oral administration of poorly water-soluble fenofibrate. Dove Medical Press 2016-01-12 /pmc/articles/PMC4716746/ /pubmed/26834471 http://dx.doi.org/10.2147/IJN.S97496 Text en © 2016 Yousaf et al. This work is published and licensed by Dove Medical Press Limited The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.
spellingShingle Original Research
Yousaf, Abid Mehmood
Mustapha, Omer
Kim, Dong Wuk
Kim, Dong Shik
Kim, Kyeong Soo
Jin, Sung Giu
Yong, Chul Soon
Youn, Yu Seok
Oh, Yu-Kyoung
Kim, Jong Oh
Choi, Han-Gon
Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate
title Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate
title_full Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate
title_fullStr Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate
title_full_unstemmed Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate
title_short Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate
title_sort novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4716746/
https://www.ncbi.nlm.nih.gov/pubmed/26834471
http://dx.doi.org/10.2147/IJN.S97496
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