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Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment

[Image: see text] Luteolin (LT) is a natural polyphenol water-insoluble compound. LT-loaded nanovesicles (NVs) were prepared by using the solvent evaporation method. LT-NVs were prepared using cholesterol, phosphatidylcholine, span 60, and labrasol in a different composition. The prepared LT-NVs wer...

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Autores principales: Imam, Syed Sarim, Alshehri, Sultan, Altamimi, Mohammad A., Hussain, Afzal, Alyahya, Khaled Hamad, Mahdi, Wael A., Qamar, Wajhul
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8757359/
https://www.ncbi.nlm.nih.gov/pubmed/35036768
http://dx.doi.org/10.1021/acsomega.1c05628
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author Imam, Syed Sarim
Alshehri, Sultan
Altamimi, Mohammad A.
Hussain, Afzal
Alyahya, Khaled Hamad
Mahdi, Wael A.
Qamar, Wajhul
author_facet Imam, Syed Sarim
Alshehri, Sultan
Altamimi, Mohammad A.
Hussain, Afzal
Alyahya, Khaled Hamad
Mahdi, Wael A.
Qamar, Wajhul
author_sort Imam, Syed Sarim
collection PubMed
description [Image: see text] Luteolin (LT) is a natural polyphenol water-insoluble compound. LT-loaded nanovesicles (NVs) were prepared by using the solvent evaporation method. LT-NVs were prepared using cholesterol, phosphatidylcholine, span 60, and labrasol in a different composition. The prepared LT-NVs were evaluated for encapsulation efficiency, in vitro drug release, and permeation study. The optimized LT-NVs were further evaluated for antioxidant activity and cytotoxicity using the lung cancer cell line. LT-NVs showed nanometric size (less than 300 nm), an optimum polydispersibility index (less than 0.5), and a negative zeta potential value. The formulations also showed significant variability in the encapsulation efficiency (69.44 ± 0.52 to 83.75 ± 0.35%) depending upon the formulation composition. The in vitro and permeation study results revealed enhanced drug release as well as permeation profile. The formulation LT-NVs (F2) showed the maximum drug release of 88.28 ± 1.13%, while pure LT showed only 20.1 ± 1.21% in 12 h. The release data revealed significant variation (p < 0.001) in the release pattern. The permeation results also depicted significant (p < 0.001) enhancement in the permeation across the membrane. The enhanced permeation from LT-NVs was achieved due to the enhanced solubility of LT in the presence of the surfactant. The antioxidant activity results proved that LT-NVs showed greater activity compared to pure LT. The cytotoxicity study showed lesser IC(50) value from LT-NVs than the pure LT. Thus, it can be concluded that LT-NVs are a natural alternative to the synthetic drug in the treatment of lung cancer.
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spelling pubmed-87573592022-01-13 Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment Imam, Syed Sarim Alshehri, Sultan Altamimi, Mohammad A. Hussain, Afzal Alyahya, Khaled Hamad Mahdi, Wael A. Qamar, Wajhul ACS Omega [Image: see text] Luteolin (LT) is a natural polyphenol water-insoluble compound. LT-loaded nanovesicles (NVs) were prepared by using the solvent evaporation method. LT-NVs were prepared using cholesterol, phosphatidylcholine, span 60, and labrasol in a different composition. The prepared LT-NVs were evaluated for encapsulation efficiency, in vitro drug release, and permeation study. The optimized LT-NVs were further evaluated for antioxidant activity and cytotoxicity using the lung cancer cell line. LT-NVs showed nanometric size (less than 300 nm), an optimum polydispersibility index (less than 0.5), and a negative zeta potential value. The formulations also showed significant variability in the encapsulation efficiency (69.44 ± 0.52 to 83.75 ± 0.35%) depending upon the formulation composition. The in vitro and permeation study results revealed enhanced drug release as well as permeation profile. The formulation LT-NVs (F2) showed the maximum drug release of 88.28 ± 1.13%, while pure LT showed only 20.1 ± 1.21% in 12 h. The release data revealed significant variation (p < 0.001) in the release pattern. The permeation results also depicted significant (p < 0.001) enhancement in the permeation across the membrane. The enhanced permeation from LT-NVs was achieved due to the enhanced solubility of LT in the presence of the surfactant. The antioxidant activity results proved that LT-NVs showed greater activity compared to pure LT. The cytotoxicity study showed lesser IC(50) value from LT-NVs than the pure LT. Thus, it can be concluded that LT-NVs are a natural alternative to the synthetic drug in the treatment of lung cancer. American Chemical Society 2021-12-23 /pmc/articles/PMC8757359/ /pubmed/35036768 http://dx.doi.org/10.1021/acsomega.1c05628 Text en © 2021 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Imam, Syed Sarim
Alshehri, Sultan
Altamimi, Mohammad A.
Hussain, Afzal
Alyahya, Khaled Hamad
Mahdi, Wael A.
Qamar, Wajhul
Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment
title Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment
title_full Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment
title_fullStr Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment
title_full_unstemmed Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment
title_short Formulation and Evaluation of Luteolin-Loaded Nanovesicles: In Vitro Physicochemical Characterization and Viability Assessment
title_sort formulation and evaluation of luteolin-loaded nanovesicles: in vitro physicochemical characterization and viability assessment
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8757359/
https://www.ncbi.nlm.nih.gov/pubmed/35036768
http://dx.doi.org/10.1021/acsomega.1c05628
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