Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma

The molecularly targeted agent anlotinib offers a novel therapeutic strategy against advanced hepatocellular carcinoma (HCC). With this study, we aimed to solve the technical problem of anlotinib being insoluble in injectable solutions; we also aimed to assess the antitumor activity of anlotinib on...

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Autores principales:	Mei Luo, Huiwei Sun, Qiyu Jiang, Yantao Chai, Congshu Li, Bin Yang, Zhixian Hong
Formato:	article
Lenguaje:	EN
Publicado:	Frontiers Media S.A. 2021
Materias:	advanced hepatocellular carcinoma molecularly targeted agents anlotinib nanoscale crystal injection antitumor activation Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/042bbc3c19444915afb2ab4e118883db
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spelling	oai:doaj.org-article:042bbc3c19444915afb2ab4e118883db2021-12-02T10:14:15ZNovel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma2234-943X10.3389/fonc.2021.777356https://doaj.org/article/042bbc3c19444915afb2ab4e118883db2021-12-01T00:00:00Zhttps://www.frontiersin.org/articles/10.3389/fonc.2021.777356/fullhttps://doaj.org/toc/2234-943XThe molecularly targeted agent anlotinib offers a novel therapeutic strategy against advanced hepatocellular carcinoma (HCC). With this study, we aimed to solve the technical problem of anlotinib being insoluble in injectable solutions; we also aimed to assess the antitumor activity of anlotinib on hepatocellular carcinoma cells. We prepared an anlotinib nanocrystal injection by wet grinding, and we optimized the prescription process using a transmission electron microscope (TEM) and a laser particle size analyzer (LPSA). The release of anlotinib from the injected nanocrystals was evaluated using LC-MS/MS in vitro, and the drug’s anti-tumor effects were assessed in a nude mice tumor model. The anlotinib nanocrystals had a uniform particle size distribution (the average nanoparticle size was ~200 nm). The preparation of anlotinib into nanocrystals did not change the original crystal structure. The intravenous injection of anlotinib nanocrystals achieved anti-tumor activity at very low doses compared to those required for oral administration of an anlotinib suspension: anlotinib nanocrystals at a dose of 50 μg/kg inhibited the subcutaneous growth of the HCC cell line MHCC97-H; whereas the dose of anlotinib suspension required for an equivalent effect was 1 mg/kg. Therefore, our novel anlotinib nanocrystal injection preparation provides an option for achieving a safe and effective molecularly targeted therapy against advanced HCC.Mei LuoHuiwei SunQiyu JiangYantao ChaiCongshu LiBin YangZhixian HongFrontiers Media S.A.articleadvanced hepatocellular carcinomamolecularly targeted agentsanlotinibnanoscale crystal injectionantitumor activationNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENFrontiers in Oncology, Vol 11 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	advanced hepatocellular carcinoma molecularly targeted agents anlotinib nanoscale crystal injection antitumor activation Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	advanced hepatocellular carcinoma molecularly targeted agents anlotinib nanoscale crystal injection antitumor activation Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Mei Luo Huiwei Sun Qiyu Jiang Yantao Chai Congshu Li Bin Yang Zhixian Hong Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma
description	The molecularly targeted agent anlotinib offers a novel therapeutic strategy against advanced hepatocellular carcinoma (HCC). With this study, we aimed to solve the technical problem of anlotinib being insoluble in injectable solutions; we also aimed to assess the antitumor activity of anlotinib on hepatocellular carcinoma cells. We prepared an anlotinib nanocrystal injection by wet grinding, and we optimized the prescription process using a transmission electron microscope (TEM) and a laser particle size analyzer (LPSA). The release of anlotinib from the injected nanocrystals was evaluated using LC-MS/MS in vitro, and the drug’s anti-tumor effects were assessed in a nude mice tumor model. The anlotinib nanocrystals had a uniform particle size distribution (the average nanoparticle size was ~200 nm). The preparation of anlotinib into nanocrystals did not change the original crystal structure. The intravenous injection of anlotinib nanocrystals achieved anti-tumor activity at very low doses compared to those required for oral administration of an anlotinib suspension: anlotinib nanocrystals at a dose of 50 μg/kg inhibited the subcutaneous growth of the HCC cell line MHCC97-H; whereas the dose of anlotinib suspension required for an equivalent effect was 1 mg/kg. Therefore, our novel anlotinib nanocrystal injection preparation provides an option for achieving a safe and effective molecularly targeted therapy against advanced HCC.
format	article
author	Mei Luo Huiwei Sun Qiyu Jiang Yantao Chai Congshu Li Bin Yang Zhixian Hong
author_facet	Mei Luo Huiwei Sun Qiyu Jiang Yantao Chai Congshu Li Bin Yang Zhixian Hong
author_sort	Mei Luo
title	Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma
title_short	Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma
title_full	Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma
title_fullStr	Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma
title_full_unstemmed	Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma
title_sort	novel nanocrystal injection of insoluble drug anlotinib and its antitumor effects on hepatocellular carcinoma
publisher	Frontiers Media S.A.
publishDate	2021
url	https://doaj.org/article/042bbc3c19444915afb2ab4e118883db
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Novel Nanocrystal Injection of Insoluble Drug Anlotinib and Its Antitumor Effects on Hepatocellular Carcinoma

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