Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles

Kyoung Mee Kim,1,2 Hyun Kyung Lim,1,2 Sang Hee Shim,1,2 Joohee Jung1,2 1College of Pharmacy, 2Innovative Drug Center, Duksung Women’s University, Seoul, Republic of Korea Abstract: Chrysin is a flavone that is found in several plants and in honeycomb and possesses various biological acti...

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Autores principales: Kim KM, Lim HK, Shim SH, Jung J
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Publicado: Dove Medical Press 2017
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Acceso en línea:https://doaj.org/article/35ac6e52d24a415a943b767ed2b92eeb
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spelling oai:doaj.org-article:35ac6e52d24a415a943b767ed2b92eeb2021-12-02T01:50:20ZImproved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles1178-2013https://doaj.org/article/35ac6e52d24a415a943b767ed2b92eeb2017-03-01T00:00:00Zhttps://www.dovepress.com/improved-chemotherapeutic-efficacy-of-injectable-chrysin-encapsulated--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Kyoung Mee Kim,1,2 Hyun Kyung Lim,1,2 Sang Hee Shim,1,2 Joohee Jung1,2 1College of Pharmacy, 2Innovative Drug Center, Duksung Women’s University, Seoul, Republic of Korea Abstract: Chrysin is a flavone that is found in several plants and in honeycomb and possesses various biological activities. However, its low solubility means it has poor bioavailability, which must be resolved to enable its pharmaceutical applications. In the present study, chrysin was incorporated into methoxy poly(ethylene glycol)-β-polycaprolactone nanoparticles (chrysin-NPs) using the oil-in-water technique in order to overcome problems associated with chrysin. The properties of chrysin-NPs were analyzed, and their anticancer effects were investigated in vitro and in vivo. Chrysin-NPs were 77 nm sized (as determined by dynamic laser light scattering) and showed a monodisperse distribution. The zeta potential of chrysin-NPs was –2.22 mV, and they were spherically shaped by cryo-transmission electron microscopy (cryo-TEM). The loading efficiency of chrysin-NPs was 46.96%. Chrysin-NPs retained the cytotoxicity of chrysin in A549 cells. The therapeutic efficacies of chrysin-NPs were compared with those of chrysin in an A549-derived xenograft mouse model. Chrysin-NPs were intravenously injected at a 10 times lower dosage than chrysin 3 times per week (q2d×3/week). However, free chrysin was orally administrated 5 times per week (q1d×5/week). Chrysin-NP-treated group showed significant tumor growth delay, which was similar to that of chrysin-treated group, despite the considerably lower total dosage. These results suggest that the injectable chrysin-NPs enhance therapeutic efficacy in vivo and offer a beneficial formulation for chemotherapy. Keywords: chrysin, nanoparticle, chemotherapeutic efficacy, non-small-cell lung cancer, in vivo modelKim KMLim HKShim SHJung JDove Medical PressarticleChrysinNanoparticleChemotherapeutic efficacyNon-small cell lung cancerin vivo modelMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 1917-1925 (2017)
institution DOAJ
collection DOAJ
language EN
topic Chrysin
Nanoparticle
Chemotherapeutic efficacy
Non-small cell lung cancer
in vivo model
Medicine (General)
R5-920
spellingShingle Chrysin
Nanoparticle
Chemotherapeutic efficacy
Non-small cell lung cancer
in vivo model
Medicine (General)
R5-920
Kim KM
Lim HK
Shim SH
Jung J
Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles
description Kyoung Mee Kim,1,2 Hyun Kyung Lim,1,2 Sang Hee Shim,1,2 Joohee Jung1,2 1College of Pharmacy, 2Innovative Drug Center, Duksung Women’s University, Seoul, Republic of Korea Abstract: Chrysin is a flavone that is found in several plants and in honeycomb and possesses various biological activities. However, its low solubility means it has poor bioavailability, which must be resolved to enable its pharmaceutical applications. In the present study, chrysin was incorporated into methoxy poly(ethylene glycol)-β-polycaprolactone nanoparticles (chrysin-NPs) using the oil-in-water technique in order to overcome problems associated with chrysin. The properties of chrysin-NPs were analyzed, and their anticancer effects were investigated in vitro and in vivo. Chrysin-NPs were 77 nm sized (as determined by dynamic laser light scattering) and showed a monodisperse distribution. The zeta potential of chrysin-NPs was –2.22 mV, and they were spherically shaped by cryo-transmission electron microscopy (cryo-TEM). The loading efficiency of chrysin-NPs was 46.96%. Chrysin-NPs retained the cytotoxicity of chrysin in A549 cells. The therapeutic efficacies of chrysin-NPs were compared with those of chrysin in an A549-derived xenograft mouse model. Chrysin-NPs were intravenously injected at a 10 times lower dosage than chrysin 3 times per week (q2d×3/week). However, free chrysin was orally administrated 5 times per week (q1d×5/week). Chrysin-NP-treated group showed significant tumor growth delay, which was similar to that of chrysin-treated group, despite the considerably lower total dosage. These results suggest that the injectable chrysin-NPs enhance therapeutic efficacy in vivo and offer a beneficial formulation for chemotherapy. Keywords: chrysin, nanoparticle, chemotherapeutic efficacy, non-small-cell lung cancer, in vivo model
format article
author Kim KM
Lim HK
Shim SH
Jung J
author_facet Kim KM
Lim HK
Shim SH
Jung J
author_sort Kim KM
title Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles
title_short Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles
title_full Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles
title_fullStr Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles
title_full_unstemmed Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles
title_sort improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles
publisher Dove Medical Press
publishDate 2017
url https://doaj.org/article/35ac6e52d24a415a943b767ed2b92eeb
work_keys_str_mv AT kimkm improvedchemotherapeuticefficacyofinjectablechrysinencapsulatedbycopolymernanoparticles
AT limhk improvedchemotherapeuticefficacyofinjectablechrysinencapsulatedbycopolymernanoparticles
AT shimsh improvedchemotherapeuticefficacyofinjectablechrysinencapsulatedbycopolymernanoparticles
AT jungj improvedchemotherapeuticefficacyofinjectablechrysinencapsulatedbycopolymernanoparticles
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