Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo

Yanan Dong,1–3 Rongzhan Fu,1–3 Jing Yang,1–3 Pei Ma,1–3 Lihua Liang,2 Yu Mi,1–3 Daidi Fan1–31Shaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University, Xi’an, Shaanxi 710069, P...

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Autores principales: Dong Y, Fu R, Yang J, Ma P, Liang L, Mi Y, Fan D
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Publicado: Dove Medical Press 2019
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spelling oai:doaj.org-article:80463e4845664741992923ee22c2d37e2021-12-02T09:27:11ZFolic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo1178-2013https://doaj.org/article/80463e4845664741992923ee22c2d37e2019-08-01T00:00:00Zhttps://www.dovepress.com/folic-acid-modified-ginsenoside-rg5-loaded-bovine-serum-albumin-nanopa-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Yanan Dong,1–3 Rongzhan Fu,1–3 Jing Yang,1–3 Pei Ma,1–3 Lihua Liang,2 Yu Mi,1–3 Daidi Fan1–31Shaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University, Xi’an, Shaanxi 710069, People’s Republic of China; 2Shaanxi R&D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University, Xi’an, Shaanxi 710069, People’s Republic of China; 3Biotech & Biomed Research Institute, Northwest University, Xi’an, Shaanxi 710069, People’s Republic of ChinaCorrespondence: Yu Mi; Daidi FanShaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University, 229 North Taibai Road, Xi’an, Shaanxi 710069, People’s Republic of ChinaEmail mi_yu@nwu.edu.cn; fandaidi@nwu.edu.cnBackground and purpose: Ginsenoside Rg5 (Rg5), a triterpene saponin, extracted from the natural herbal plant ginseng, is one of the most potent anticancer drugs against various carcinoma cells. However, the therapeutic potential of Rg5 is limited by its low solubility in water, poor bioavailability, and nontargeted delivery. Therefore, we prepared folic acid (FA)-modified bovine serum albumin (BSA) nanoparticles (FA-Rg5-BSA NPs) to improve the therapeutic efficacy and tumor targetability of Rg5.Methods: Various aspects of the FA-Rg5-BSA NPs were characterized, including size, polydispersity, zeta potential, morphology, entrapment efficiency (EE), drug loading (DL), in vitro drug release, thermal stability, in vitro cytotoxicity, cell apoptosis, cellular uptake, in vivo antitumor effects and in vivo biodistribution imaging.Results: The FA-Rg5-BSA NPs showed a particle size of 201.4 nm with a polydispersity index of 0.081, uniform spherical shape, and drug loading of 12.64±4.02%. The aqueous solution of FA-Rg5-BSA NPs had favorable stability for 8 weeks at 4°C. The FA-Rg5-BSA NPs dissolved under acidic conditions. Moreover, the Rg5-BSA NPs and FA-Rg5-BSA NPs had advanced anticancer activity compared with Rg5 in MCF-7 cells, while poor cytotoxicity was observed in L929 cells. The FA-Rg5-BSA NPs facilitated cellular uptake and induced apoptosis in MCF-7 cells. In addition, in an MCF-7 xenograft mouse model, the in vivo antitumor evaluation revealed that FA-Rg5-BSA NPs were more effective in inhibiting tumor growth than Rg5 and Rg5-BSA NPs. The in vivo real-time bioimaging study showed that the FA-Rg5-BSA NPs exhibited superior tumor accumulation ability.Conclusion: The results suggested that FA-Rg5-BSA NPs could serve as a promising system to improve the antitumor effect of Rg5.Keywords: ginsenoside Rg5, drug delivery, nanoparticles, antitumor activity, human MCF-7 breast cancer cellsDong YFu RYang JMa PLiang LMi YFan DDove Medical Pressarticleginsenoside Rg5drug deliverynanoparticlesantitumor activityhuman MCF-7 breast cancer cellsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 6971-6988 (2019)
institution DOAJ
collection DOAJ
language EN
topic ginsenoside Rg5
drug delivery
nanoparticles
antitumor activity
human MCF-7 breast cancer cells
Medicine (General)
R5-920
spellingShingle ginsenoside Rg5
drug delivery
nanoparticles
antitumor activity
human MCF-7 breast cancer cells
Medicine (General)
R5-920
Dong Y
Fu R
Yang J
Ma P
Liang L
Mi Y
Fan D
Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo
description Yanan Dong,1–3 Rongzhan Fu,1–3 Jing Yang,1–3 Pei Ma,1–3 Lihua Liang,2 Yu Mi,1–3 Daidi Fan1–31Shaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University, Xi’an, Shaanxi 710069, People’s Republic of China; 2Shaanxi R&D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University, Xi’an, Shaanxi 710069, People’s Republic of China; 3Biotech & Biomed Research Institute, Northwest University, Xi’an, Shaanxi 710069, People’s Republic of ChinaCorrespondence: Yu Mi; Daidi FanShaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University, 229 North Taibai Road, Xi’an, Shaanxi 710069, People’s Republic of ChinaEmail mi_yu@nwu.edu.cn; fandaidi@nwu.edu.cnBackground and purpose: Ginsenoside Rg5 (Rg5), a triterpene saponin, extracted from the natural herbal plant ginseng, is one of the most potent anticancer drugs against various carcinoma cells. However, the therapeutic potential of Rg5 is limited by its low solubility in water, poor bioavailability, and nontargeted delivery. Therefore, we prepared folic acid (FA)-modified bovine serum albumin (BSA) nanoparticles (FA-Rg5-BSA NPs) to improve the therapeutic efficacy and tumor targetability of Rg5.Methods: Various aspects of the FA-Rg5-BSA NPs were characterized, including size, polydispersity, zeta potential, morphology, entrapment efficiency (EE), drug loading (DL), in vitro drug release, thermal stability, in vitro cytotoxicity, cell apoptosis, cellular uptake, in vivo antitumor effects and in vivo biodistribution imaging.Results: The FA-Rg5-BSA NPs showed a particle size of 201.4 nm with a polydispersity index of 0.081, uniform spherical shape, and drug loading of 12.64±4.02%. The aqueous solution of FA-Rg5-BSA NPs had favorable stability for 8 weeks at 4°C. The FA-Rg5-BSA NPs dissolved under acidic conditions. Moreover, the Rg5-BSA NPs and FA-Rg5-BSA NPs had advanced anticancer activity compared with Rg5 in MCF-7 cells, while poor cytotoxicity was observed in L929 cells. The FA-Rg5-BSA NPs facilitated cellular uptake and induced apoptosis in MCF-7 cells. In addition, in an MCF-7 xenograft mouse model, the in vivo antitumor evaluation revealed that FA-Rg5-BSA NPs were more effective in inhibiting tumor growth than Rg5 and Rg5-BSA NPs. The in vivo real-time bioimaging study showed that the FA-Rg5-BSA NPs exhibited superior tumor accumulation ability.Conclusion: The results suggested that FA-Rg5-BSA NPs could serve as a promising system to improve the antitumor effect of Rg5.Keywords: ginsenoside Rg5, drug delivery, nanoparticles, antitumor activity, human MCF-7 breast cancer cells
format article
author Dong Y
Fu R
Yang J
Ma P
Liang L
Mi Y
Fan D
author_facet Dong Y
Fu R
Yang J
Ma P
Liang L
Mi Y
Fan D
author_sort Dong Y
title Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo
title_short Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo
title_full Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo
title_fullStr Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo
title_full_unstemmed Folic acid-modified ginsenoside Rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo
title_sort folic acid-modified ginsenoside rg5-loaded bovine serum albumin nanoparticles for targeted cancer therapy in vitro and in vivo
publisher Dove Medical Press
publishDate 2019
url https://doaj.org/article/80463e4845664741992923ee22c2d37e
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