Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies
Numerous neurological disorders have a pathophysiology that involves an increase in free radical production in the brain. Quercetin (QER) is a nutraceutical compound that shields the brain against oxidative stress-induced neurodegeneration. Nonetheless, its low oral bioavailability diminishes brain...
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MDPI AG
2023-06-01
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| 丛编: | Pharmaceutics |
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| 在线阅读: | https://www.mdpi.com/1999-4923/15/7/1805 |
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| author | Mohammed H. Elkomy Randa Mohammed Zaki Omar A. Alsaidan Mohammed Elmowafy Ameeduzzafar Zafar Khaled Shalaby Mohamed A. Abdelgawad Fatma I. Abo El-Ela Mostafa E. Rateb Ibrahim A. Naguib Hussein M. Eid |
| author_facet | Mohammed H. Elkomy Randa Mohammed Zaki Omar A. Alsaidan Mohammed Elmowafy Ameeduzzafar Zafar Khaled Shalaby Mohamed A. Abdelgawad Fatma I. Abo El-Ela Mostafa E. Rateb Ibrahim A. Naguib Hussein M. Eid |
| author_sort | Mohammed H. Elkomy |
| collection | DOAJ |
| description | Numerous neurological disorders have a pathophysiology that involves an increase in free radical production in the brain. Quercetin (QER) is a nutraceutical compound that shields the brain against oxidative stress-induced neurodegeneration. Nonetheless, its low oral bioavailability diminishes brain delivery. Therefore, the current study aimed to formulate QER-loaded transferosomal nanovesicles (QER-TFS) in situ gel for QER brain delivery via the intranasal route. This study explored the impacts of lipid amount, edge activator (EA) amount, and EA type on vesicle diameter, entrapment, and cumulative amount permeated through nasal mucosa (24 h). The optimum formulation was then integrated into a thermosensitive gel after its physical and morphological characteristics were assessed. Assessments of the optimized QER-TFS showed nanometric vesicles (171.4 ± 3.4 nm) with spherical shapes and adequate entrapment efficiency (78.2 ± 2.8%). The results of short-term stability and high zeta potential value (−32.6 ± 1.4 mV) of QER-TFS confirmed their high stability. Compared with the QER solution, the optimized QER-TFS in situ gel formulation exhibited sustained release behavior and augmented nasal mucosa permeability. CT scanning of rat brains demonstrated the buildup of gold nanoparticles (GNPs) in the brains of all treatment groups, with a greater level of GNPs noted in the rats given the transferosomal gel. Additionally, in vitro studies on PCS-200-014 cells revealed minimal cytotoxicity of QER-TFS in situ gel. Based on these results, the developed transferosomal nanovesicles may be a suitable nanocarrier for QER brain targeting through the intranasal route. |
| first_indexed | 2024-03-11T00:44:37Z |
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| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T00:44:37Z |
| publishDate | 2023-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-25da909f42b8458db6aeafa901b0e3432023-11-18T20:54:05ZengMDPI AGPharmaceutics1999-49232023-06-01157180510.3390/pharmaceutics15071805Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic StudiesMohammed H. Elkomy0Randa Mohammed Zaki1Omar A. Alsaidan2Mohammed Elmowafy3Ameeduzzafar Zafar4Khaled Shalaby5Mohamed A. Abdelgawad6Fatma I. Abo El-Ela7Mostafa E. Rateb8Ibrahim A. Naguib9Hussein M. Eid10Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka 72341, Saudi ArabiaDepartment of Pharmacology, Faculty of Veterinary Medicine, Beni-Suef University, Beni-Suef 62511, EgyptSchool of Computing, Engineering & Physical Sciences, University of the West of Scotland, Paisley PA1 2BE, UKDepartment of Pharmaceutical Chemistry, College of Pharmacy, Taif University, Taif 21944, Saudi ArabiaDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62511, EgyptNumerous neurological disorders have a pathophysiology that involves an increase in free radical production in the brain. Quercetin (QER) is a nutraceutical compound that shields the brain against oxidative stress-induced neurodegeneration. Nonetheless, its low oral bioavailability diminishes brain delivery. Therefore, the current study aimed to formulate QER-loaded transferosomal nanovesicles (QER-TFS) in situ gel for QER brain delivery via the intranasal route. This study explored the impacts of lipid amount, edge activator (EA) amount, and EA type on vesicle diameter, entrapment, and cumulative amount permeated through nasal mucosa (24 h). The optimum formulation was then integrated into a thermosensitive gel after its physical and morphological characteristics were assessed. Assessments of the optimized QER-TFS showed nanometric vesicles (171.4 ± 3.4 nm) with spherical shapes and adequate entrapment efficiency (78.2 ± 2.8%). The results of short-term stability and high zeta potential value (−32.6 ± 1.4 mV) of QER-TFS confirmed their high stability. Compared with the QER solution, the optimized QER-TFS in situ gel formulation exhibited sustained release behavior and augmented nasal mucosa permeability. CT scanning of rat brains demonstrated the buildup of gold nanoparticles (GNPs) in the brains of all treatment groups, with a greater level of GNPs noted in the rats given the transferosomal gel. Additionally, in vitro studies on PCS-200-014 cells revealed minimal cytotoxicity of QER-TFS in situ gel. Based on these results, the developed transferosomal nanovesicles may be a suitable nanocarrier for QER brain targeting through the intranasal route.https://www.mdpi.com/1999-4923/15/7/1805quercetintransferosomesbrain targetingCT scancytotoxicityintranasal |
| spellingShingle | Mohammed H. Elkomy Randa Mohammed Zaki Omar A. Alsaidan Mohammed Elmowafy Ameeduzzafar Zafar Khaled Shalaby Mohamed A. Abdelgawad Fatma I. Abo El-Ela Mostafa E. Rateb Ibrahim A. Naguib Hussein M. Eid Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies Pharmaceutics quercetin transferosomes brain targeting CT scan cytotoxicity intranasal |
| title | Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies |
| title_full | Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies |
| title_fullStr | Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies |
| title_full_unstemmed | Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies |
| title_short | Intranasal Nanotransferosomal Gel for Quercetin Brain Targeting: I. Optimization, Characterization, Brain Localization, and Cytotoxic Studies |
| title_sort | intranasal nanotransferosomal gel for quercetin brain targeting i optimization characterization brain localization and cytotoxic studies |
| topic | quercetin transferosomes brain targeting CT scan cytotoxicity intranasal |
| url | https://www.mdpi.com/1999-4923/15/7/1805 |
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