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Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System

Luteolin (LUT) is a natural pharmaceutical compound that is weakly water soluble and has low bioavailability when taken orally. As a result, the goal of this research was to create self-nanoemulsifying drug delivery systems (SNEDDS) for LUT in an attempt to improve its in vitro dissolution and hepat...

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Autores principales: Shakeel, Faiyaz, Alamer, Moad M., Alam, Prawez, Alshetaili, Abdullah, Haq, Nazrul, Alanazi, Fars K., Alshehri, Sultan, Ghoneim, Mohammed M., Alsarra, Ibrahim A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8703857/
https://www.ncbi.nlm.nih.gov/pubmed/34946581
http://dx.doi.org/10.3390/molecules26247497
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author Shakeel, Faiyaz
Alamer, Moad M.
Alam, Prawez
Alshetaili, Abdullah
Haq, Nazrul
Alanazi, Fars K.
Alshehri, Sultan
Ghoneim, Mohammed M.
Alsarra, Ibrahim A.
author_facet Shakeel, Faiyaz
Alamer, Moad M.
Alam, Prawez
Alshetaili, Abdullah
Haq, Nazrul
Alanazi, Fars K.
Alshehri, Sultan
Ghoneim, Mohammed M.
Alsarra, Ibrahim A.
author_sort Shakeel, Faiyaz
collection PubMed
description Luteolin (LUT) is a natural pharmaceutical compound that is weakly water soluble and has low bioavailability when taken orally. As a result, the goal of this research was to create self-nanoemulsifying drug delivery systems (SNEDDS) for LUT in an attempt to improve its in vitro dissolution and hepatoprotective effects, resulting in increased oral bioavailability. Using the aqueous phase titration approach and the creation of pseudo-ternary phase diagrams with Capryol-PGMC (oil phase), Tween-80 (surfactant), and Transcutol-HP (co-emulsifier), various SNEDDS of LUT were generated. SNEDDS were assessed for droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), and percent of transmittance (percent T) after undergoing several thermodynamic stability and self-nanoemulsification experiments. When compared to LUT suspension, the developed SNEDDS revealed considerable LUT release from all SNEDDS. Droplet size was 40 nm, PDI was <0.3, ZP was −30.58 mV, RI was 1.40, percent T was >98 percent, and drug release profile was >96 percent in optimized SNEDDS of LUT. For in vivo hepatoprotective testing in rats, optimized SNEDDS was chosen. When compared to LUT suspension, hepatoprotective tests showed that optimized LUT SNEDDS had a substantial hepatoprotective impact. The findings of this investigation suggested that SNEDDS could improve bioflavonoid LUT dissolution rate and therapeutic efficacy.
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spelling pubmed-87038572021-12-25 Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System Shakeel, Faiyaz Alamer, Moad M. Alam, Prawez Alshetaili, Abdullah Haq, Nazrul Alanazi, Fars K. Alshehri, Sultan Ghoneim, Mohammed M. Alsarra, Ibrahim A. Molecules Article Luteolin (LUT) is a natural pharmaceutical compound that is weakly water soluble and has low bioavailability when taken orally. As a result, the goal of this research was to create self-nanoemulsifying drug delivery systems (SNEDDS) for LUT in an attempt to improve its in vitro dissolution and hepatoprotective effects, resulting in increased oral bioavailability. Using the aqueous phase titration approach and the creation of pseudo-ternary phase diagrams with Capryol-PGMC (oil phase), Tween-80 (surfactant), and Transcutol-HP (co-emulsifier), various SNEDDS of LUT were generated. SNEDDS were assessed for droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), and percent of transmittance (percent T) after undergoing several thermodynamic stability and self-nanoemulsification experiments. When compared to LUT suspension, the developed SNEDDS revealed considerable LUT release from all SNEDDS. Droplet size was 40 nm, PDI was <0.3, ZP was −30.58 mV, RI was 1.40, percent T was >98 percent, and drug release profile was >96 percent in optimized SNEDDS of LUT. For in vivo hepatoprotective testing in rats, optimized SNEDDS was chosen. When compared to LUT suspension, hepatoprotective tests showed that optimized LUT SNEDDS had a substantial hepatoprotective impact. The findings of this investigation suggested that SNEDDS could improve bioflavonoid LUT dissolution rate and therapeutic efficacy. MDPI 2021-12-11 /pmc/articles/PMC8703857/ /pubmed/34946581 http://dx.doi.org/10.3390/molecules26247497 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Shakeel, Faiyaz
Alamer, Moad M.
Alam, Prawez
Alshetaili, Abdullah
Haq, Nazrul
Alanazi, Fars K.
Alshehri, Sultan
Ghoneim, Mohammed M.
Alsarra, Ibrahim A.
Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System
title Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System
title_full Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System
title_fullStr Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System
title_full_unstemmed Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System
title_short Hepatoprotective Effects of Bioflavonoid Luteolin Using Self-Nanoemulsifying Drug Delivery System
title_sort hepatoprotective effects of bioflavonoid luteolin using self-nanoemulsifying drug delivery system
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8703857/
https://www.ncbi.nlm.nih.gov/pubmed/34946581
http://dx.doi.org/10.3390/molecules26247497
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