Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

Abid Mehmood Yousaf,1 Dong Wuk Kim,1 Yu-Kyoung Oh,2 Chul Soon Yong,3 Jong Oh Kim,3 Han-Gon Choi11College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, 2College of Pharmacy, Seoul National University, Seoul, 3College of Pharmacy, Yeungnam University,...

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Autores principales:	Yousaf AM, Kim DW, Oh YK, Yong CS, Kim JO, Choi HG
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/5a10df4e7d544d2faedb2fe4d2b23787
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spelling	oai:doaj.org-article:5a10df4e7d544d2faedb2fe4d2b237872021-12-02T02:01:31ZEnhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation1178-2013https://doaj.org/article/5a10df4e7d544d2faedb2fe4d2b237872015-03-01T00:00:00Zhttp://www.dovepress.com/enhanced-oral-bioavailability-of-fenofibrate-using-polymeric-nanoparti-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Abid Mehmood Yousaf,1 Dong Wuk Kim,1 Yu-Kyoung Oh,2 Chul Soon Yong,3 Jong Oh Kim,3 Han-Gon Choi11College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, 2College of Pharmacy, Seoul National University, Seoul, 3College of Pharmacy, Yeungnam University, Gyongsan, South KoreaBackground: The intention of this research was to prepare and compare various solubility-enhancing nanoparticulated systems in order to select a nanoparticulated formulation with the most improved oral bioavailability of poorly water-soluble fenofibrate.Methods: The most appropriate excipients for different nanoparticulated preparations were selected by determining the drug solubility in 1% (w/v) aqueous solutions of each carrier. The polyvinylpyrrolidone (PVP) nanospheres, hydroxypropyl-β-cyclodextrin (HP-β-CD) nanocorpuscles, and gelatin nanocapsules were formulated as fenofibrate/PVP/sodium lauryl sulfate (SLS), fenofibrate/HP-β-CD, and fenofibrate/gelatin at the optimized weight ratios of 2.5:4.5:1, 1:4, and 1:8, respectively. The three solid-state products were achieved using the solvent-evaporation method through the spray-drying technique. The physicochemical characterization of these nanoparticles was accomplished by powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Their physicochemical properties, aqueous solubility, dissolution rate, and pharmacokinetics in rats were investigated in comparison with the drug powder.Results: Among the tested carriers, PVP, HP-β-CD, gelatin, and SLS showed better solubility and were selected as the most appropriate constituents for various nanoparticulated systems. All of the formulations significantly improved the aqueous solubility, dissolution rate, and oral bioavailability of fenofibrate compared to the drug powder. The drug was present in the amorphous form in HP-β-CD nanocorpuscles; however, in other formulations, it existed in the crystalline state with a reduced intensity. The aqueous solubility and dissolution rates of the nanoparticles (after 30 minutes) were not significantly different from one another. Among the nanoparticulated systems tested in this study, the initial dissolution rates (up to 10 minutes) were higher with the PVP nanospheres and HP-β-CD nanocorpuscles; however, neither of them resulted in the highest oral bioavailability. Irrespective of relatively retarded dissolution rate, gelatin nanocapsules showed the highest apparent aqueous solubility and furnished the most improved oral bioavailability of the drug (~5.5-fold), owing to better wetting and diminution in crystallinity.Conclusion: Fenofibrate-loaded gelatin nanocapsules prepared using the solvent-evaporation method through the spray-drying technique could be a potential oral pharmaceutical product for administering the poorly water-soluble fenofibrate with an enhanced bioavailability.Keywords: gelatin nanocapsules, hydrophilic polymeric matrix, crystallinity, ameliorated oral bioavailabilityYousaf AMKim DWOh YKYong CSKim JOChoi HGDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 1819-1830 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Yousaf AM Kim DW Oh YK Yong CS Kim JO Choi HG Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
description	Abid Mehmood Yousaf,1 Dong Wuk Kim,1 Yu-Kyoung Oh,2 Chul Soon Yong,3 Jong Oh Kim,3 Han-Gon Choi11College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, 2College of Pharmacy, Seoul National University, Seoul, 3College of Pharmacy, Yeungnam University, Gyongsan, South KoreaBackground: The intention of this research was to prepare and compare various solubility-enhancing nanoparticulated systems in order to select a nanoparticulated formulation with the most improved oral bioavailability of poorly water-soluble fenofibrate.Methods: The most appropriate excipients for different nanoparticulated preparations were selected by determining the drug solubility in 1% (w/v) aqueous solutions of each carrier. The polyvinylpyrrolidone (PVP) nanospheres, hydroxypropyl-β-cyclodextrin (HP-β-CD) nanocorpuscles, and gelatin nanocapsules were formulated as fenofibrate/PVP/sodium lauryl sulfate (SLS), fenofibrate/HP-β-CD, and fenofibrate/gelatin at the optimized weight ratios of 2.5:4.5:1, 1:4, and 1:8, respectively. The three solid-state products were achieved using the solvent-evaporation method through the spray-drying technique. The physicochemical characterization of these nanoparticles was accomplished by powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Their physicochemical properties, aqueous solubility, dissolution rate, and pharmacokinetics in rats were investigated in comparison with the drug powder.Results: Among the tested carriers, PVP, HP-β-CD, gelatin, and SLS showed better solubility and were selected as the most appropriate constituents for various nanoparticulated systems. All of the formulations significantly improved the aqueous solubility, dissolution rate, and oral bioavailability of fenofibrate compared to the drug powder. The drug was present in the amorphous form in HP-β-CD nanocorpuscles; however, in other formulations, it existed in the crystalline state with a reduced intensity. The aqueous solubility and dissolution rates of the nanoparticles (after 30 minutes) were not significantly different from one another. Among the nanoparticulated systems tested in this study, the initial dissolution rates (up to 10 minutes) were higher with the PVP nanospheres and HP-β-CD nanocorpuscles; however, neither of them resulted in the highest oral bioavailability. Irrespective of relatively retarded dissolution rate, gelatin nanocapsules showed the highest apparent aqueous solubility and furnished the most improved oral bioavailability of the drug (~5.5-fold), owing to better wetting and diminution in crystallinity.Conclusion: Fenofibrate-loaded gelatin nanocapsules prepared using the solvent-evaporation method through the spray-drying technique could be a potential oral pharmaceutical product for administering the poorly water-soluble fenofibrate with an enhanced bioavailability.Keywords: gelatin nanocapsules, hydrophilic polymeric matrix, crystallinity, ameliorated oral bioavailability
format	article
author	Yousaf AM Kim DW Oh YK Yong CS Kim JO Choi HG
author_facet	Yousaf AM Kim DW Oh YK Yong CS Kim JO Choi HG
author_sort	Yousaf AM
title	Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
title_short	Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
title_full	Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
title_fullStr	Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
title_full_unstemmed	Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
title_sort	enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/5a10df4e7d544d2faedb2fe4d2b23787
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Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

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