Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition

Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition

Haroon Rahim,1 Abdul Sadiq,2 Shahzeb Khan,2–4 Fazli Amin,1 Riaz Ullah,5 Abdelaaty A Shahat,5,6 Hafiz Majid Mahmood71Department of Pharmacy, Sarhad University of Science and Information Technology, Peshawar, Khyber Pakhtunkhwa, 25000, Pakistan; 2Department of Pharmacy, University of Malakan...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Rahim H, Sadiq A, Khan S, Amin F, Ullah R, Shahat AA, Mahmood HM
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2019
Materias:
Glimepiride nanosuspension
Precipitation-ultrasonication approach
boosted bioavailability.
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/2bc51dd8c8224c1b92b4e1c82a92c6a2
Etiquetas: Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
id oai:doaj.org-article:2bc51dd8c8224c1b92b4e1c82a92c6a2
record_format dspace
spelling oai:doaj.org-article:2bc51dd8c8224c1b92b4e1c82a92c6a22021-12-02T11:05:08ZFabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition1178-2013https://doaj.org/article/2bc51dd8c8224c1b92b4e1c82a92c6a22019-08-01T00:00:00Zhttps://www.dovepress.com/fabrication-and-characterization-of-glimepiride-nanosuspension-by-ultr-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Haroon Rahim,1 Abdul Sadiq,2 Shahzeb Khan,2–4 Fazli Amin,1 Riaz Ullah,5 Abdelaaty A Shahat,5,6 Hafiz Majid Mahmood71Department of Pharmacy, Sarhad University of Science and Information Technology, Peshawar, Khyber Pakhtunkhwa, 25000, Pakistan; 2Department of Pharmacy, University of Malakand, Chakdara, Khyber Pakhtunkhwa, 18800, Pakistan; 3Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Durban, 4000, South Africa; 4Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA; 5Department of Pharmacognosy (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 6Phytochemistry Department, National Research Centre, Giza, Egypt; 7Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaPurpose: We aimed to enhance the solubility, dissolution rate, oral bioavailability, and α-glucosidase inhibition of glimepiride (Glm) by fabricating its nanosuspension using a precipitation–ultrasonication approach.Methods: Glm nanosuspensions were fabricated using optimized processing conditions. Characterization of Glm was performed using Malvern Zetasizer, scanning electron microscopy, transmission electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. Minimum particle size and polydispersity index (PDI) values were found to be 152.4±2.42 nm and 0.23±0.01, respectively, using hydroxypropyl methylcellulose: 6 cPs, 1% w/v, polyvinylpyrrolidone K30 1% w/v, and sodium lauryl sulfate 0.12% w/v, keeping ultrasonication power input at 400 W, with 15 minutes’ processing at 3-second pauses. In vivo oral bioavailability was assessed using rabbits as a model.Results: The saturation solubility of the Glm nanosuspensions was substantially enhanced 3.14-fold and 5.77-fold compared to unprocessed drug in stabilizer solution and unprocessed active pharmaceutical ingredient. Also, the dissolution rate of the nanosuspensions ws substantially boosted when compared to the marketed formulation and unprocessed drug candidate. The results showed that >85% of Glm nanosuspensions dissolved in the first 10 minutes compared to 10.17% of unprocessed Glm), 42.19% of microsuspensions, and 19.94% of marketed tablets. In-vivo studies conducted in animals, i.e. rabbits, demonstrated that maximum concentration and AUC0–24 with oral dosing were twofold (5 mg/kg) and 1.74-fold (2.5 mg/kg) and 1.80-fold (5 mg/kg) and 1.63-fold (2.5 mg/kg), respectively, and compared with the unprocessed drug formulation. In-vitro α-glucosidase inhibition results showed that fabricated nanosuspensions had a pronounced effect compared to unprocessed drug.Conclusion: The optimized batch fabricated by ultrasonication-assisted precipitation can be useful in boosting oral bioavailability, which may be accredited to enhanced solubility and dissolution rate of Glm, ultimately resulting in its faster rate of absorption due to nanonization.Keywords: glimepiride nanosuspension, precipitation–ultrasonication approach, boosted bioavailabilityRahim HSadiq AKhan SAmin FUllah RShahat AAMahmood HMDove Medical PressarticleGlimepiride nanosuspensionPrecipitation-ultrasonication approachboosted bioavailability.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 6287-6296 (2019)
institution DOAJ
collection DOAJ
language EN
topic Glimepiride nanosuspension
Precipitation-ultrasonication approach
boosted bioavailability.
Medicine (General)
R5-920
spellingShingle Glimepiride nanosuspension
Precipitation-ultrasonication approach
boosted bioavailability.
Medicine (General)
R5-920
Rahim H
Sadiq A
Khan S
Amin F
Ullah R
Shahat AA
Mahmood HM
Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition
description Haroon Rahim,1 Abdul Sadiq,2 Shahzeb Khan,2–4 Fazli Amin,1 Riaz Ullah,5 Abdelaaty A Shahat,5,6 Hafiz Majid Mahmood71Department of Pharmacy, Sarhad University of Science and Information Technology, Peshawar, Khyber Pakhtunkhwa, 25000, Pakistan; 2Department of Pharmacy, University of Malakand, Chakdara, Khyber Pakhtunkhwa, 18800, Pakistan; 3Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Durban, 4000, South Africa; 4Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA; 5Department of Pharmacognosy (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 6Phytochemistry Department, National Research Centre, Giza, Egypt; 7Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaPurpose: We aimed to enhance the solubility, dissolution rate, oral bioavailability, and α-glucosidase inhibition of glimepiride (Glm) by fabricating its nanosuspension using a precipitation–ultrasonication approach.Methods: Glm nanosuspensions were fabricated using optimized processing conditions. Characterization of Glm was performed using Malvern Zetasizer, scanning electron microscopy, transmission electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. Minimum particle size and polydispersity index (PDI) values were found to be 152.4±2.42 nm and 0.23±0.01, respectively, using hydroxypropyl methylcellulose: 6 cPs, 1% w/v, polyvinylpyrrolidone K30 1% w/v, and sodium lauryl sulfate 0.12% w/v, keeping ultrasonication power input at 400 W, with 15 minutes’ processing at 3-second pauses. In vivo oral bioavailability was assessed using rabbits as a model.Results: The saturation solubility of the Glm nanosuspensions was substantially enhanced 3.14-fold and 5.77-fold compared to unprocessed drug in stabilizer solution and unprocessed active pharmaceutical ingredient. Also, the dissolution rate of the nanosuspensions ws substantially boosted when compared to the marketed formulation and unprocessed drug candidate. The results showed that >85% of Glm nanosuspensions dissolved in the first 10 minutes compared to 10.17% of unprocessed Glm), 42.19% of microsuspensions, and 19.94% of marketed tablets. In-vivo studies conducted in animals, i.e. rabbits, demonstrated that maximum concentration and AUC0–24 with oral dosing were twofold (5 mg/kg) and 1.74-fold (2.5 mg/kg) and 1.80-fold (5 mg/kg) and 1.63-fold (2.5 mg/kg), respectively, and compared with the unprocessed drug formulation. In-vitro α-glucosidase inhibition results showed that fabricated nanosuspensions had a pronounced effect compared to unprocessed drug.Conclusion: The optimized batch fabricated by ultrasonication-assisted precipitation can be useful in boosting oral bioavailability, which may be accredited to enhanced solubility and dissolution rate of Glm, ultimately resulting in its faster rate of absorption due to nanonization.Keywords: glimepiride nanosuspension, precipitation–ultrasonication approach, boosted bioavailability
format article
author Rahim H
Sadiq A
Khan S
Amin F
Ullah R
Shahat AA
Mahmood HM
author_facet Rahim H
Sadiq A
Khan S
Amin F
Ullah R
Shahat AA
Mahmood HM
author_sort Rahim H
title Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition
title_short Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition
title_full Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition
title_fullStr Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition
title_full_unstemmed Fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition
title_sort fabrication and characterization of glimepiride nanosuspension by ultrasonication-assisted precipitation for improvement of oral bioavailability and in vitro α-glucosidase inhibition
publisher Dove Medical Press
publishDate 2019
url https://doaj.org/article/2bc51dd8c8224c1b92b4e1c82a92c6a2
work_keys_str_mv AT rahimh fabricationandcharacterizationofglimepiridenanosuspensionbyultrasonicationassistedprecipitationforimprovementoforalbioavailabilityandinvitroalphaglucosidaseinhibition
AT sadiqa fabricationandcharacterizationofglimepiridenanosuspensionbyultrasonicationassistedprecipitationforimprovementoforalbioavailabilityandinvitroalphaglucosidaseinhibition
AT khans fabricationandcharacterizationofglimepiridenanosuspensionbyultrasonicationassistedprecipitationforimprovementoforalbioavailabilityandinvitroalphaglucosidaseinhibition
AT aminf fabricationandcharacterizationofglimepiridenanosuspensionbyultrasonicationassistedprecipitationforimprovementoforalbioavailabilityandinvitroalphaglucosidaseinhibition
AT ullahr fabricationandcharacterizationofglimepiridenanosuspensionbyultrasonicationassistedprecipitationforimprovementoforalbioavailabilityandinvitroalphaglucosidaseinhibition
AT shahataa fabricationandcharacterizationofglimepiridenanosuspensionbyultrasonicationassistedprecipitationforimprovementoforalbioavailabilityandinvitroalphaglucosidaseinhibition
AT mahmoodhm fabricationandcharacterizationofglimepiridenanosuspensionbyultrasonicationassistedprecipitationforimprovementoforalbioavailabilityandinvitroalphaglucosidaseinhibition
_version_ 1718396281264537600

Ejemplares similares