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

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Author(s): Tan BJ | Liu Y | Chang KL | Lim BKW | Chiu GNC

Journal: International Journal of Nanomedicine
ISSN 1176-9114

Volume: 2012;
Issue: default;
Start page: 651;
Date: 2012;
Original page

ABSTRACT
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 ≥88.9% when the content of quercetin was up to 4% w/w, with sizes of 15.4–18.5 nm and polydispersity indices of

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