Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer

Jiaojiao Cao,1,* Jie Huang,1,* Shuangying Gui,1,2 Xiaoqin Chu1,2 1Department of Pharmaceutics, Anhui University of Chinese Medicine, Hefei, 230012, People’s Republic of China; 2Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, 230012, People’s Republic of Chin...

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Autores principales:	Cao J, Huang J, Gui S, Chu X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	biocompatibility liver cancer sn 5-fu Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6b9bcac0a58b48149bb7af8f99196126
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spelling	oai:doaj.org-article:6b9bcac0a58b48149bb7af8f991961262021-12-02T14:59:45ZPreparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer1178-2013https://doaj.org/article/6b9bcac0a58b48149bb7af8f991961262021-05-01T00:00:00Zhttps://www.dovepress.com/preparation-synergism-and-biocompatibility-of-in-situ-liquid-crystals--peer-reviewed-fulltext-article-IJNhttps://doaj.org/toc/1178-2013Jiaojiao Cao,1,* Jie Huang,1,* Shuangying Gui,1,2 Xiaoqin Chu1,2 1Department of Pharmaceutics, Anhui University of Chinese Medicine, Hefei, 230012, People’s Republic of China; 2Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, 230012, People’s Republic of China*These authors contributed equally to this workCorrespondence: Xiaoqin ChuMaster Instructor Tel +86 13856929921Fax +86 551-68129028Email chuxq420@163.comPurpose: Transarterial chemoembolization is the preferred treatment for patients with middle and advanced-stage hepatocellular carcinoma (HCC); however, most hepatic artery embolization agents have various disadvantages. The purpose of this study was to evaluate phytantriol-based liquid crystal injections for potential use in treatment of HCC.Methods: Using sinomenine (SN) and 5-fluorouracil (5-FU) as model drugs, three precursor in situ liquid crystal injections based on phytantriol (P1, P2, and P3) were prepared, and their in vitro biocompatibility, anticancer activity, and drug release investigated, to evaluate their feasibility for use in treatment of HCC. The properties of the precursor injections and subsequent cubic liquid crystal gels were observed by visual and polarizing microscopy, in an in vitro gelation experiment. Biocompatibility was evaluated by in vitro hemolysis, histocompatibility, and cytotoxicity assays.Results: Precursor injections were colorless liquids that formed transparent cubic liquid crystal gels on addition of excess water. The three precursor injections all caused slight hemolysis, without agglutination, and were mildly cytotoxic. Histocompatibility experiments showed that P1 had good histocompatibility, while P2 and P3 resulted in strong inflammatory responses, which subsequently resolved spontaneously. In vitro anti-cancer testing showed that SN and 5-FU inhibited HepG2 cells in a time- and concentration-dependent manner and had synergistic effects. Further, in vitro release assays indicated that all three preparations had sustained release effects, with cumulative release of > 80% within 48 h.Conclusion: These results indicate that SN and 5-FU have synergistic inhibitory effects on HepG2 cells, which has not previously been reported. Moreover, we describe a biocompatible precursor injection, useful as a drug carrier for the treatment of liver cancer, which can achieve targeting, sustained release, synergistic chemotherapy, and embolization. These data indicate that precursor injections containing SN and 5-FU have great potential for use in therapy for liver cancer.Keywords: carcinoma, hepatocellular, drug carriers, delayed-action preparations, chemoembolization, therapeutic, SN, 5-FUCao JHuang JGui SChu XDove Medical Pressarticlebiocompatibilityliver cancersn5-fuMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 3725-3739 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	biocompatibility liver cancer sn 5-fu Medicine (General) R5-920
spellingShingle	biocompatibility liver cancer sn 5-fu Medicine (General) R5-920 Cao J Huang J Gui S Chu X Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer
description	Jiaojiao Cao,1,* Jie Huang,1,* Shuangying Gui,1,2 Xiaoqin Chu1,2 1Department of Pharmaceutics, Anhui University of Chinese Medicine, Hefei, 230012, People’s Republic of China; 2Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, 230012, People’s Republic of China*These authors contributed equally to this workCorrespondence: Xiaoqin ChuMaster Instructor Tel +86 13856929921Fax +86 551-68129028Email chuxq420@163.comPurpose: Transarterial chemoembolization is the preferred treatment for patients with middle and advanced-stage hepatocellular carcinoma (HCC); however, most hepatic artery embolization agents have various disadvantages. The purpose of this study was to evaluate phytantriol-based liquid crystal injections for potential use in treatment of HCC.Methods: Using sinomenine (SN) and 5-fluorouracil (5-FU) as model drugs, three precursor in situ liquid crystal injections based on phytantriol (P1, P2, and P3) were prepared, and their in vitro biocompatibility, anticancer activity, and drug release investigated, to evaluate their feasibility for use in treatment of HCC. The properties of the precursor injections and subsequent cubic liquid crystal gels were observed by visual and polarizing microscopy, in an in vitro gelation experiment. Biocompatibility was evaluated by in vitro hemolysis, histocompatibility, and cytotoxicity assays.Results: Precursor injections were colorless liquids that formed transparent cubic liquid crystal gels on addition of excess water. The three precursor injections all caused slight hemolysis, without agglutination, and were mildly cytotoxic. Histocompatibility experiments showed that P1 had good histocompatibility, while P2 and P3 resulted in strong inflammatory responses, which subsequently resolved spontaneously. In vitro anti-cancer testing showed that SN and 5-FU inhibited HepG2 cells in a time- and concentration-dependent manner and had synergistic effects. Further, in vitro release assays indicated that all three preparations had sustained release effects, with cumulative release of > 80% within 48 h.Conclusion: These results indicate that SN and 5-FU have synergistic inhibitory effects on HepG2 cells, which has not previously been reported. Moreover, we describe a biocompatible precursor injection, useful as a drug carrier for the treatment of liver cancer, which can achieve targeting, sustained release, synergistic chemotherapy, and embolization. These data indicate that precursor injections containing SN and 5-FU have great potential for use in therapy for liver cancer.Keywords: carcinoma, hepatocellular, drug carriers, delayed-action preparations, chemoembolization, therapeutic, SN, 5-FU
format	article
author	Cao J Huang J Gui S Chu X
author_facet	Cao J Huang J Gui S Chu X
author_sort	Cao J
title	Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer
title_short	Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer
title_full	Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer
title_fullStr	Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer
title_full_unstemmed	Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer
title_sort	preparation, synergism, and biocompatibility of in situ liquid crystals loaded with sinomenine and 5-fluorouracil for treatment of liver cancer
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/6b9bcac0a58b48149bb7af8f99196126
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Preparation, Synergism, and Biocompatibility of in situ Liquid Crystals Loaded with Sinomenine and 5-Fluorouracil for Treatment of Liver Cancer

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