Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma

Chenjun Ma, Tiantian Wei, Yingying Hua, Zhongjie Wang, Liefeng Zhang School of Food and Pharmaceutical Engineering, Nanjing Normal University, Nanjing, 210046, People’s Republic of ChinaCorrespondence: Liefeng Zhang Wenyuan Road 1#, Qixia District, Nanjing, 210046, People’s Republic of ChinaTel +86-...

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Autores principales:	Ma C, Wei T, Hua Y, Wang Z, Zhang L
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	nanoparticles target penetrating peptide tyroserleutide hepatocellular carcinoma cellular respiration rate Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/5ddf298505e74c5ba8f0ae888c947ec8
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spelling	oai:doaj.org-article:5ddf298505e74c5ba8f0ae888c947ec82021-12-02T16:51:47ZEffective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma1178-2013https://doaj.org/article/5ddf298505e74c5ba8f0ae888c947ec82021-07-01T00:00:00Zhttps://www.dovepress.com/effective-antitumor-of-orally-intestinal-targeting-penetrating-peptide-peer-reviewed-fulltext-article-IJNhttps://doaj.org/toc/1178-2013Chenjun Ma, Tiantian Wei, Yingying Hua, Zhongjie Wang, Liefeng Zhang School of Food and Pharmaceutical Engineering, Nanjing Normal University, Nanjing, 210046, People’s Republic of ChinaCorrespondence: Liefeng Zhang Wenyuan Road 1#, Qixia District, Nanjing, 210046, People’s Republic of ChinaTel +86-25-85898184Fax +86-25-85898184Email lfzhang@njnu.edu.cnPurpose: Hepatocellular carcinoma (HCC) is a common malignant tumor that seriously threatens human life and health. Currently, the majority of antitumor drugs are administered in an injectable manner, which can cause pain and side effects to patients. Objective of this study is to establish an effective oral drug delivery system for anti hepatoma drugs.Methods: In this study, intestinal targeting cell penetrating peptide (R6LRVG) was obtained by binding cell penetrating peptide (R6) with the polypeptide of LRVG (targeting intestinal epithelial cells). Next, R6LRVG-modified tyroserleutide-poly(lactic-co-glycolic acid) (PLGA) nanoparticles (YSL-PLGA/R6LRVG NPs) were prepared. After that, the nanoparticles were characterized and their stability was evaluated. The cellular uptake, in vitro bioactivity and in vivo antitumor activity of the nanoparticles were investigated. In addition, the mechanism, including the endocytic pathway and respiratory rate detection of mitochondria, was further investigated.Results: YSL-PLGA/R6LRVG NPs were successfully prepared. Characterization revealed YSL-PLGA/R6LRVG NPs to be globular particles with smooth surfaces and an average diameter of 222.6 nm. The entrapment efficiency and drug loading of tyroserleutide were 70.27% and 19.69%, respectively. Furthermore, the YSL-PLGA/R6LRVG NPs group exhibited the largest amount of YSL uptake. We also found that cell uptake of YSL-PLGA/R6LRVG NPs could be related to the endocytosis pathways mediated by reticulin and caveolae/lipid rafts. Additionally, the YSL-PLGA/R6LRVG NPs could interfere with mitochondrial function. In vivo experiments revealed that orally administered YSL-PLGA/R6LRVG NPs exerted excellent anticancer effects in tumor-bearing mice. Hematoxylin-eosin staining did not show any histological changes in the major organs.Conclusion: To summarize, YSL-PLGA/R6LRVG NPs could be a useful oral delivery system of YSL and may provide a new platform for the oral delivery of anticancer drugs.Keywords: nanoparticles, target penetrating peptide, tyroserleutide, hepatocellular carcinoma, cellular respiration rateMa CWei THua YWang ZZhang LDove Medical Pressarticlenanoparticlestarget penetrating peptidetyroserleutidehepatocellular carcinomacellular respiration rateMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 4495-4513 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	nanoparticles target penetrating peptide tyroserleutide hepatocellular carcinoma cellular respiration rate Medicine (General) R5-920
spellingShingle	nanoparticles target penetrating peptide tyroserleutide hepatocellular carcinoma cellular respiration rate Medicine (General) R5-920 Ma C Wei T Hua Y Wang Z Zhang L Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma
description	Chenjun Ma, Tiantian Wei, Yingying Hua, Zhongjie Wang, Liefeng Zhang School of Food and Pharmaceutical Engineering, Nanjing Normal University, Nanjing, 210046, People’s Republic of ChinaCorrespondence: Liefeng Zhang Wenyuan Road 1#, Qixia District, Nanjing, 210046, People’s Republic of ChinaTel +86-25-85898184Fax +86-25-85898184Email lfzhang@njnu.edu.cnPurpose: Hepatocellular carcinoma (HCC) is a common malignant tumor that seriously threatens human life and health. Currently, the majority of antitumor drugs are administered in an injectable manner, which can cause pain and side effects to patients. Objective of this study is to establish an effective oral drug delivery system for anti hepatoma drugs.Methods: In this study, intestinal targeting cell penetrating peptide (R6LRVG) was obtained by binding cell penetrating peptide (R6) with the polypeptide of LRVG (targeting intestinal epithelial cells). Next, R6LRVG-modified tyroserleutide-poly(lactic-co-glycolic acid) (PLGA) nanoparticles (YSL-PLGA/R6LRVG NPs) were prepared. After that, the nanoparticles were characterized and their stability was evaluated. The cellular uptake, in vitro bioactivity and in vivo antitumor activity of the nanoparticles were investigated. In addition, the mechanism, including the endocytic pathway and respiratory rate detection of mitochondria, was further investigated.Results: YSL-PLGA/R6LRVG NPs were successfully prepared. Characterization revealed YSL-PLGA/R6LRVG NPs to be globular particles with smooth surfaces and an average diameter of 222.6 nm. The entrapment efficiency and drug loading of tyroserleutide were 70.27% and 19.69%, respectively. Furthermore, the YSL-PLGA/R6LRVG NPs group exhibited the largest amount of YSL uptake. We also found that cell uptake of YSL-PLGA/R6LRVG NPs could be related to the endocytosis pathways mediated by reticulin and caveolae/lipid rafts. Additionally, the YSL-PLGA/R6LRVG NPs could interfere with mitochondrial function. In vivo experiments revealed that orally administered YSL-PLGA/R6LRVG NPs exerted excellent anticancer effects in tumor-bearing mice. Hematoxylin-eosin staining did not show any histological changes in the major organs.Conclusion: To summarize, YSL-PLGA/R6LRVG NPs could be a useful oral delivery system of YSL and may provide a new platform for the oral delivery of anticancer drugs.Keywords: nanoparticles, target penetrating peptide, tyroserleutide, hepatocellular carcinoma, cellular respiration rate
format	article
author	Ma C Wei T Hua Y Wang Z Zhang L
author_facet	Ma C Wei T Hua Y Wang Z Zhang L
author_sort	Ma C
title	Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma
title_short	Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma
title_full	Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma
title_fullStr	Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma
title_full_unstemmed	Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma
title_sort	effective antitumor of orally intestinal targeting penetrating peptide-loaded tyroserleutide/plga nanoparticles in hepatocellular carcinoma
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/5ddf298505e74c5ba8f0ae888c947ec8
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Effective Antitumor of Orally Intestinal Targeting Penetrating Peptide-Loaded Tyroserleutide/PLGA Nanoparticles in Hepatocellular Carcinoma

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