Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy

Raj Kumar Thapa,1 Ju Yeon Choi,1 Bijay Kumar Poudel,1 Han-Gon Choi,2 Chul Soon Yong,1 Jong Oh Kim1 1College of Pharmacy, Yeungnam University, Gyeongsan, Gyeongsanbuk-do, South Korea; 2College of Pharmacy, Hanyang University, Ansan, South Korea Abstract: Cancer is one of the leading causes of death...

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Autores principales: Thapa RK, Choi JY, Poudel BK, Choi HG, Yong CS, Kim JO
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Publicado: Dove Medical Press 2016
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spelling oai:doaj.org-article:8550e0672e0144b38d01e563f6a68c542021-12-02T01:49:55ZReceptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy1178-2013https://doaj.org/article/8550e0672e0144b38d01e563f6a68c542016-06-01T00:00:00Zhttps://www.dovepress.com/receptor-targeted-drug-loaded-functionalized-graphene-oxides-for-chemo-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Raj Kumar Thapa,1 Ju Yeon Choi,1 Bijay Kumar Poudel,1 Han-Gon Choi,2 Chul Soon Yong,1 Jong Oh Kim1 1College of Pharmacy, Yeungnam University, Gyeongsan, Gyeongsanbuk-do, South Korea; 2College of Pharmacy, Hanyang University, Ansan, South Korea Abstract: Cancer is one of the leading causes of death worldwide. Although different chemotherapeutic agents have been developed to treat cancers, their use can be limited by low cellular uptake, drug resistance, and side effects. Hence, targeted drug delivery systems are continually being developed in order to improve the efficacy of chemotherapeutic agents. The main aim of this study was to prepare folic acid (FA)-conjugated polyvinyl pyrrolidone-functionalized graphene oxides (GO) (FA-GO) for targeted delivery of sorafenib (SF). GO were prepared using a modified Hummer’s method and subsequently altered to prepare FA-GO and SF-loaded FA-GO (FA-GO/SF). Characterization of GO derivatives was done using ultraviolet/visible spectroscopy, Fourier transform infrared spectroscopy, X-ray diffraction, atomic force microscopy, zeta potential measurements, and determination of in vitro drug release. Hemolytic toxicity, in vitro cytotoxicity, cellular uptake, and apoptotic effects of FA-GO/SF were also investigated. The results revealed that GO was successfully synthesized and that further transformation to FA-GO improved the stability and SF drug-loading capacity. In addition, the enhanced SF release under acidic conditions suggested possible benefits for cancer treatment. Conjugation of FA within the FA-GO/SF delivery system enabled targeted delivery of SF to cancer cells expressing high levels of FA receptors, thus increasing the cellular uptake and apoptotic effects of SF. Furthermore, the photothermal effect achieved by exposure of GO to near-infrared irradiation enhanced the anticancer effects of FA-GO/SF. Taken together, FA-GO/SF is a potential carrier for targeted delivery of chemotherapeutic agents in cancer. Keywords: graphene oxide, folic acid, sorafenib, targeted drug delivery, near-infraredThapa RKChoi JYPoudel BKChoi HGYong CSKim JODove Medical PressarticleGraphene oxidefolic acidsorafenibtargeted drug deliverynear-infraredMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 2799-2813 (2016)
institution DOAJ
collection DOAJ
language EN
topic Graphene oxide
folic acid
sorafenib
targeted drug delivery
near-infrared
Medicine (General)
R5-920
spellingShingle Graphene oxide
folic acid
sorafenib
targeted drug delivery
near-infrared
Medicine (General)
R5-920
Thapa RK
Choi JY
Poudel BK
Choi HG
Yong CS
Kim JO
Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
description Raj Kumar Thapa,1 Ju Yeon Choi,1 Bijay Kumar Poudel,1 Han-Gon Choi,2 Chul Soon Yong,1 Jong Oh Kim1 1College of Pharmacy, Yeungnam University, Gyeongsan, Gyeongsanbuk-do, South Korea; 2College of Pharmacy, Hanyang University, Ansan, South Korea Abstract: Cancer is one of the leading causes of death worldwide. Although different chemotherapeutic agents have been developed to treat cancers, their use can be limited by low cellular uptake, drug resistance, and side effects. Hence, targeted drug delivery systems are continually being developed in order to improve the efficacy of chemotherapeutic agents. The main aim of this study was to prepare folic acid (FA)-conjugated polyvinyl pyrrolidone-functionalized graphene oxides (GO) (FA-GO) for targeted delivery of sorafenib (SF). GO were prepared using a modified Hummer’s method and subsequently altered to prepare FA-GO and SF-loaded FA-GO (FA-GO/SF). Characterization of GO derivatives was done using ultraviolet/visible spectroscopy, Fourier transform infrared spectroscopy, X-ray diffraction, atomic force microscopy, zeta potential measurements, and determination of in vitro drug release. Hemolytic toxicity, in vitro cytotoxicity, cellular uptake, and apoptotic effects of FA-GO/SF were also investigated. The results revealed that GO was successfully synthesized and that further transformation to FA-GO improved the stability and SF drug-loading capacity. In addition, the enhanced SF release under acidic conditions suggested possible benefits for cancer treatment. Conjugation of FA within the FA-GO/SF delivery system enabled targeted delivery of SF to cancer cells expressing high levels of FA receptors, thus increasing the cellular uptake and apoptotic effects of SF. Furthermore, the photothermal effect achieved by exposure of GO to near-infrared irradiation enhanced the anticancer effects of FA-GO/SF. Taken together, FA-GO/SF is a potential carrier for targeted delivery of chemotherapeutic agents in cancer. Keywords: graphene oxide, folic acid, sorafenib, targeted drug delivery, near-infrared
format article
author Thapa RK
Choi JY
Poudel BK
Choi HG
Yong CS
Kim JO
author_facet Thapa RK
Choi JY
Poudel BK
Choi HG
Yong CS
Kim JO
author_sort Thapa RK
title Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
title_short Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
title_full Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
title_fullStr Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
title_full_unstemmed Receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
title_sort receptor-targeted, drug-loaded, functionalized graphene oxides for chemotherapy and photothermal therapy
publisher Dove Medical Press
publishDate 2016
url https://doaj.org/article/8550e0672e0144b38d01e563f6a68c54
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AT poudelbk receptortargeteddrugloadedfunctionalizedgrapheneoxidesforchemotherapyandphotothermaltherapy
AT choihg receptortargeteddrugloadedfunctionalizedgrapheneoxidesforchemotherapyandphotothermaltherapy
AT yongcs receptortargeteddrugloadedfunctionalizedgrapheneoxidesforchemotherapyandphotothermaltherapy
AT kimjo receptortargeteddrugloadedfunctionalizedgrapheneoxidesforchemotherapyandphotothermaltherapy
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