Abstract

Abstract

Quercetin (QT) is a flavonoid that exhibits anti-oxidant and chemo-preventive activity. This research work aimed to develop surface-modified bilosomes (BS) of QT. The BS was prepared by the solvent evaporation method and optimized by the Box-Behnken design. The optimized QT-BS (QT-BS3opt) displayed vesicle size (143.51 nm), PDI (0.256), zeta potential (−15.4 mV), and entrapment efficiency (89.52%). Further, the optimized QT-BS formulation was coated with chitosan (CS). The XRD diffractogram of CS-QT-BS3opt1 did not exhibit extensive peaks of QT, revealing that QT is properly encapsulated in the polymer matrix. The QT-BS3opt and CS-QT-BS3opt1 exhibited sustained-release (86.62 ± 3.23% and 69.32 ± 2.57%, respectively) up to 24 h with the Korsmeyer-Peppas kinetic model (R2 =0.9089). CS-QT-BS3opt1 exhibited significantly (P < .05) high flux, i.e. 4.20-fold more than pure QT dispersion and 1.27-fold higher than QT-BS3opt. CS-QT-BS3opt1 showed significantly greater bio-adhesion (76.43 ± 2.42%) than QT-BS3opt (20.82 ± 1.45%). The antioxidant activity showed that QT from CS-QT-BS3opt1 has more remarkable (P < .05) antioxidant activity at each concentration than pure QT. The CS-QT-BS3opt1 exhibited 1.61-fold higher cytotoxicity against MFC7 and 1.44-fold higher cytotoxicity against MDA-MB-231 than pure QT. The CS-QT-BS3opt1 displayed a significantly greater antimicrobial potential against E. coli than against S. aureus. From all these findings, it could be concluded that surface-modified QT-BS might be an effective approach for increasing the efficacy of QT in the treatment of certain ailments.

Details

Title
Development of surface modified bilosomes for the oral delivery of quercetin: optimization, characterization in-vitro antioxidant, antimicrobial, and cytotoxicity study
Author
Alruwaili, Nabil K 1 ; Ameeduzzafar Zafar 1 ; Omar Awad Alsaidan 1 ; Yasir, Mohd 2 ; Mostafa, Ehab M 3 ; Alnomasy, Sultan F 4 ; Rawaf, Alenazy 5 ; Alquraini, Ali 6 ; Alomar, Fadhel A 7 

1  Department of Pharmaceutics, College of Pharmacy, Jouf University , Sakaka , Al-Jouf , Saudi Arabia 
2  Department of Pharmacy, College of Health Sciences, Arsi University , Asella , Ethiopia 
3  Department of Pharmacognosy, College of Pharmacy, Jouf University , Sakaka , Al-Jouf , Saudi Arabia 
4  Department of Medical Laboratories Sciences, College of Applied Medical Sciences in Al-Quwayiyah, Shaqra University , Shaqraa , Saudi Arabia 
5  Department of Medical Laboratory, College of Applied Medical Sciences-Shaqra, Shaqra University , Shaqraa , Saudi Arabia 
6  Department of Pharmaceutical Chemistry, Faculty of Clinical Pharmacy, Al Baha University , Al Baha , Saudi Arabia 
7  Department of Pharmacology and Toxicology, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University , Dammam , Saudi Arabia 
Pages
3035-3050
Publication year
2022
Publication date
Dec 2022
Publisher
Taylor & Francis Ltd.
ISSN
10717544
e-ISSN
15210464
Source type
Scholarly Journal
Language of publication
English
DOI
https://doi.org/10.1080/10717544.2022.2122634
ProQuest document ID
2754997015
Copyright
© 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.. This work is licensed under the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/ (the "License"). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.