Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability

Hany SM Ali,1,2 Ahmed F Hanafy,1,3 Abdulmalik Alqurshi1 1Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Al-Madinah Al-Munawwarah, Saudi Arabia; 2Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt; 3Research and Deve...

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Autores principales:	Ali HSM, Hanafy AF, Alqurshi A
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Glyburide nanocrystals downstream tablet bioavailability. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/c2c993104e414cd9a4d875d43322b99e
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spelling	oai:doaj.org-article:c2c993104e414cd9a4d875d43322b99e2021-12-02T03:23:17ZEngineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability1178-2013https://doaj.org/article/c2c993104e414cd9a4d875d43322b99e2019-03-01T00:00:00Zhttps://www.dovepress.com/engineering-of-solidified-glyburide-nanocrystals-for-tablet-formulatio-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Hany SM Ali,1,2 Ahmed F Hanafy,1,3 Abdulmalik Alqurshi1 1Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Al-Madinah Al-Munawwarah, Saudi Arabia; 2Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt; 3Research and Development Department, Al Andalous Pharmaceutical Industries, Cairo, Egypt Introduction: Presenting poorly water-soluble drugs as nanoparticles has shown to be an effective technique in enhancing drug dissolution rate, intrinsic solubility, and thus oral bioavailability. Nevertheless, working with nanoparticles introduces many challenges, one of which is their physical instability. Formulating nanoparticles into a solid dosage form may overcome such challenges and thus unlock the potential benefits of nanosizing. Methods: The current work investigates the possibility of developing a novel solid dosage form, with enhanced dissolution rate, whereby nanocrystals (~400 nm) of the class II Biopharmaceutical Classification System drug, glyburide (GBD) were fabricated through combined precipitation and homogenization procedures. Using a novel, but scalable, spraying technique, GBD nanocrystals were loaded onto commonly used tablet fillers, water-soluble lactose monohydrate (LAC), and water insoluble microcrystalline cellulose (MCC). Conventional tableting processes were then used to convert the powders generated into a tablet dosage form. Results: Studies of redispersibility showed considerable preservation of size characteristics of GBD nanocrystals during downstream processing with redispersibility indices of 105 and 118 for GBD–LAC and GBD–MCC, respectively. Characterization by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy showed that the powders generated powders contained nanosized crystals of GBD which adhered to carrier surfaces. Powder flowability was characterized using Hausner ratio (HR) and Carr’s index (CI). GBD–LAC-loaded particles exhibited poor flowability with CI and HR of 37.5% and 1.60, respectively, whilst GBD–MCC particles showed a slightly improved flowability with CI and HR of 26.47% and 1.36, respectively. The novel tablet dosage form met US Pharmacopeia specifications, including drug content, hardness, and friability. Conclusion: Higher dissolution rates were observed from the nanocrystal-based tablets compared to the microsized and commercial drug formulations. Moreover, the novel nanocrystal tablet dosage forms showed enhanced in vivo performance with area under the plasma concentration–time curve in the first 24 hours values 1.97 and 2.24 times greater than that of marketed tablets. Keywords: glyburide, nanocrystals, downstream, tablet, bioavailability, solidification, redispersibilityAli HSMHanafy AFAlqurshi ADove Medical PressarticleGlyburidenanocrystalsdownstreamtabletbioavailability.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 1893-1906 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Glyburide nanocrystals downstream tablet bioavailability. Medicine (General) R5-920
spellingShingle	Glyburide nanocrystals downstream tablet bioavailability. Medicine (General) R5-920 Ali HSM Hanafy AF Alqurshi A Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
description	Hany SM Ali,1,2 Ahmed F Hanafy,1,3 Abdulmalik Alqurshi1 1Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taibah University, Al-Madinah Al-Munawwarah, Saudi Arabia; 2Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt; 3Research and Development Department, Al Andalous Pharmaceutical Industries, Cairo, Egypt Introduction: Presenting poorly water-soluble drugs as nanoparticles has shown to be an effective technique in enhancing drug dissolution rate, intrinsic solubility, and thus oral bioavailability. Nevertheless, working with nanoparticles introduces many challenges, one of which is their physical instability. Formulating nanoparticles into a solid dosage form may overcome such challenges and thus unlock the potential benefits of nanosizing. Methods: The current work investigates the possibility of developing a novel solid dosage form, with enhanced dissolution rate, whereby nanocrystals (~400 nm) of the class II Biopharmaceutical Classification System drug, glyburide (GBD) were fabricated through combined precipitation and homogenization procedures. Using a novel, but scalable, spraying technique, GBD nanocrystals were loaded onto commonly used tablet fillers, water-soluble lactose monohydrate (LAC), and water insoluble microcrystalline cellulose (MCC). Conventional tableting processes were then used to convert the powders generated into a tablet dosage form. Results: Studies of redispersibility showed considerable preservation of size characteristics of GBD nanocrystals during downstream processing with redispersibility indices of 105 and 118 for GBD–LAC and GBD–MCC, respectively. Characterization by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy showed that the powders generated powders contained nanosized crystals of GBD which adhered to carrier surfaces. Powder flowability was characterized using Hausner ratio (HR) and Carr’s index (CI). GBD–LAC-loaded particles exhibited poor flowability with CI and HR of 37.5% and 1.60, respectively, whilst GBD–MCC particles showed a slightly improved flowability with CI and HR of 26.47% and 1.36, respectively. The novel tablet dosage form met US Pharmacopeia specifications, including drug content, hardness, and friability. Conclusion: Higher dissolution rates were observed from the nanocrystal-based tablets compared to the microsized and commercial drug formulations. Moreover, the novel nanocrystal tablet dosage forms showed enhanced in vivo performance with area under the plasma concentration–time curve in the first 24 hours values 1.97 and 2.24 times greater than that of marketed tablets. Keywords: glyburide, nanocrystals, downstream, tablet, bioavailability, solidification, redispersibility
format	article
author	Ali HSM Hanafy AF Alqurshi A
author_facet	Ali HSM Hanafy AF Alqurshi A
author_sort	Ali HSM
title	Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
title_short	Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
title_full	Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
title_fullStr	Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
title_full_unstemmed	Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
title_sort	engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/c2c993104e414cd9a4d875d43322b99e
work_keys_str_mv	AT alihsm engineeringofsolidifiedglyburidenanocrystalsfortabletformulationvialoadingofcarriersdownstreamprocessingcharacterizationandbioavailability AT hanafyaf engineeringofsolidifiedglyburidenanocrystalsfortabletformulationvialoadingofcarriersdownstreamprocessingcharacterizationandbioavailability AT alqurshia engineeringofsolidifiedglyburidenanocrystalsfortabletformulationvialoadingofcarriersdownstreamprocessingcharacterizationandbioavailability
_version_	1718401819085897728

Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability

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