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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Dove Medical Press
2017
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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) |
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Chrysin Nanoparticle Chemotherapeutic efficacy Non-small cell lung cancer in vivo model Medicine (General) R5-920 |
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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 |
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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 |
_version_ |
1718402827983781888 |