Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer

Bee-Jen Tan, Yuanjie Liu, Kai-Lun Chang, Bennie KW Lim, Gigi NC ChiuDepartment of Pharmacy, Faculty of Science, National University of Singapore, SingaporeBackground: Realizing the therapeutic benefits of quercetin is mostly hampered by its low water solubility and poor absorption. In light of the a...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Tan BJ, Liu Y, Chang KL, Lim BKW, Chiu GNC
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/9c24dca9565943d3b8e8976e6d8f64c0
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:9c24dca9565943d3b8e8976e6d8f64c0
record_format	dspace
spelling	oai:doaj.org-article:9c24dca9565943d3b8e8976e6d8f64c02021-12-02T01:13:55ZPerorally active nanomicellar formulation of quercetin in the treatment of lung cancer1176-91141178-2013https://doaj.org/article/9c24dca9565943d3b8e8976e6d8f64c02012-02-01T00:00:00Zhttp://www.dovepress.com/perorally-active-nanomicellar-formulation-of-quercetin-in-the-treatmen-a9222https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Bee-Jen Tan, Yuanjie Liu, Kai-Lun Chang, Bennie KW Lim, Gigi NC ChiuDepartment of Pharmacy, Faculty of Science, National University of Singapore, SingaporeBackground: Realizing the therapeutic benefits of quercetin is mostly hampered by its low water solubility and poor absorption. In light of the advantages of nanovehicles in the delivery of flavanoids, we aimed to deliver quercetin perorally with nanomicelles made from the diblock copolymer, polyethylene glycol (PEG)-derivatized phosphatidylethanolamine (PE).Methods: Quercetin-loaded nanomicelles were prepared by using the film casting method, and were evaluated in terms of drug incorporation efficiency, micelle size, interaction with Caco-2 cells, and anticancer activity in the A549 lung cancer cell line and murine xenograft model.Results: The incorporation efficiency into the nanomicelles was &ge;88.9% when the content of quercetin was up to 4% w/w, with sizes of 15.4&ndash;18.5 nm and polydispersity indices of &lt;0.250. Solubilization of quercetin by the nanomicelles increased its aqueous concentration by 110-fold. The quercetin nanomicelles were stable when tested in simulated gastric (pH 1.2) and intestinal (pH 7.4) fluids, and were non-toxic to the Caco-2 cells as reflected by reversible reduction in transepithelial electrical resistance and &le;25% lactose dehydrogenase release. The anticancer activity of quercetin could be significantly improved over the free drug through the nanomicellar formulation when tested using the A549 cancer cell line and murine xenograft model. The nanomicellar quercetin formulation was well tolerated by the tumor-bearing animals, with no significant weight loss observed at the end of the 10-week study period.Conclusion: A stable PEG-PE nanomicellar formulation of quercetin was developed with enhanced peroral anticancer activity and no apparent toxicity to the intestinal epithelium.Keywords: quercetin, polymeric micelles, PEG-PE, peroral drug delivery, lung cancerTan BJLiu YChang KLLim BKWChiu GNCDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 651-661 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Tan BJ Liu Y Chang KL Lim BKW Chiu GNC Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer
description	Bee-Jen Tan, Yuanjie Liu, Kai-Lun Chang, Bennie KW Lim, Gigi NC ChiuDepartment of Pharmacy, Faculty of Science, National University of Singapore, SingaporeBackground: Realizing the therapeutic benefits of quercetin is mostly hampered by its low water solubility and poor absorption. In light of the advantages of nanovehicles in the delivery of flavanoids, we aimed to deliver quercetin perorally with nanomicelles made from the diblock copolymer, polyethylene glycol (PEG)-derivatized phosphatidylethanolamine (PE).Methods: Quercetin-loaded nanomicelles were prepared by using the film casting method, and were evaluated in terms of drug incorporation efficiency, micelle size, interaction with Caco-2 cells, and anticancer activity in the A549 lung cancer cell line and murine xenograft model.Results: The incorporation efficiency into the nanomicelles was &ge;88.9% when the content of quercetin was up to 4% w/w, with sizes of 15.4&ndash;18.5 nm and polydispersity indices of &lt;0.250. Solubilization of quercetin by the nanomicelles increased its aqueous concentration by 110-fold. The quercetin nanomicelles were stable when tested in simulated gastric (pH 1.2) and intestinal (pH 7.4) fluids, and were non-toxic to the Caco-2 cells as reflected by reversible reduction in transepithelial electrical resistance and &le;25% lactose dehydrogenase release. The anticancer activity of quercetin could be significantly improved over the free drug through the nanomicellar formulation when tested using the A549 cancer cell line and murine xenograft model. The nanomicellar quercetin formulation was well tolerated by the tumor-bearing animals, with no significant weight loss observed at the end of the 10-week study period.Conclusion: A stable PEG-PE nanomicellar formulation of quercetin was developed with enhanced peroral anticancer activity and no apparent toxicity to the intestinal epithelium.Keywords: quercetin, polymeric micelles, PEG-PE, peroral drug delivery, lung cancer
format	article
author	Tan BJ Liu Y Chang KL Lim BKW Chiu GNC
author_facet	Tan BJ Liu Y Chang KL Lim BKW Chiu GNC
author_sort	Tan BJ
title	Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer
title_short	Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer
title_full	Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer
title_fullStr	Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer
title_full_unstemmed	Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer
title_sort	perorally active nanomicellar formulation of quercetin in the treatment of lung cancer
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/9c24dca9565943d3b8e8976e6d8f64c0
work_keys_str_mv	AT tanbj perorallyactivenanomicellarformulationofquercetininthetreatmentoflungcancer AT liuy perorallyactivenanomicellarformulationofquercetininthetreatmentoflungcancer AT changkl perorallyactivenanomicellarformulationofquercetininthetreatmentoflungcancer AT limbkw perorallyactivenanomicellarformulationofquercetininthetreatmentoflungcancer AT chiugnc perorallyactivenanomicellarformulationofquercetininthetreatmentoflungcancer
_version_	1718403215305736192

Perorally active nanomicellar formulation of quercetin in the treatment of lung cancer

Ejemplares similares