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3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer

BACKGROUND: 3,5,4′-trimethoxy-trans-stilbene (BTM) is a methylated derivative of resveratrol. To improve the pharmaceutical properties of BTM, BTM loaded PEG-PE micelles (BTM@PEG-PE) were fabricated and its anti-cancer efficacy against colon cancer was evaluated. METHODS: BTM@PEG-PE micelles were pr...

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Autores principales: Wu, Jun-Yong, Li, Yong-Jiang, Liu, Xin-Yi, Cai, Jia-Xin, Hu, Xiong-Bin, Wang, Jie-Min, Tang, Tian-Tian, Xiang, Da-Xiong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6749994/
https://www.ncbi.nlm.nih.gov/pubmed/31571860
http://dx.doi.org/10.2147/IJN.S221625
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author Wu, Jun-Yong
Li, Yong-Jiang
Liu, Xin-Yi
Cai, Jia-Xin
Hu, Xiong-Bin
Wang, Jie-Min
Tang, Tian-Tian
Xiang, Da-Xiong
author_facet Wu, Jun-Yong
Li, Yong-Jiang
Liu, Xin-Yi
Cai, Jia-Xin
Hu, Xiong-Bin
Wang, Jie-Min
Tang, Tian-Tian
Xiang, Da-Xiong
author_sort Wu, Jun-Yong
collection PubMed
description BACKGROUND: 3,5,4′-trimethoxy-trans-stilbene (BTM) is a methylated derivative of resveratrol. To improve the pharmaceutical properties of BTM, BTM loaded PEG-PE micelles (BTM@PEG-PE) were fabricated and its anti-cancer efficacy against colon cancer was evaluated. METHODS: BTM@PEG-PE micelles were prepared by the solvent evaporation method and were characterized by nuclear magnetic resonance (NMR), size, zeta potential, polymer disperse index (PDI) and transmission electron microscopy (TEM). Cellular uptake, cell viability assay, caspase-3 activity assay and flow cytometry were performed to evaluate the cell internalization and anti-cancer efficacy of BTM@PEG-PE micelles in vitro. Pharmacokinetic profiles of BTM and BTM@PEG-PE micelles were compared and in vivo anti-cancer therapeutic efficacy and safety of BTM@PEG-PE micelles on CT26 xenograft mice were evaluated. RESULTS: BTM was successfully embedded in the core of PEG-PE micelles, with a drug loading capacity of 5.62±0.80%. PEG-PE micelles facilitated BTM entering to the CT26 cells and BTM@PEG-PE micelles exerted enhanced anti-cancer efficacy against CT26 cells. BTM@PEG-PE micelles showed prolonged half-life and increased bioavailability. More importantly, BTM@PEG-PE micelles treatment suppressed tumor growth in tumor-bearing mice and prolonged survival with minimal damage to normal tissues. CONCLUSION: Altogether, the BTM@PEG-PE micelles might be a promising strategy to enhance the pharmacokinetic and pharmacodynamic potentials of BTM for colon cancer therapy.
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spelling pubmed-67499942019-09-30 3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer Wu, Jun-Yong Li, Yong-Jiang Liu, Xin-Yi Cai, Jia-Xin Hu, Xiong-Bin Wang, Jie-Min Tang, Tian-Tian Xiang, Da-Xiong Int J Nanomedicine Original Research BACKGROUND: 3,5,4′-trimethoxy-trans-stilbene (BTM) is a methylated derivative of resveratrol. To improve the pharmaceutical properties of BTM, BTM loaded PEG-PE micelles (BTM@PEG-PE) were fabricated and its anti-cancer efficacy against colon cancer was evaluated. METHODS: BTM@PEG-PE micelles were prepared by the solvent evaporation method and were characterized by nuclear magnetic resonance (NMR), size, zeta potential, polymer disperse index (PDI) and transmission electron microscopy (TEM). Cellular uptake, cell viability assay, caspase-3 activity assay and flow cytometry were performed to evaluate the cell internalization and anti-cancer efficacy of BTM@PEG-PE micelles in vitro. Pharmacokinetic profiles of BTM and BTM@PEG-PE micelles were compared and in vivo anti-cancer therapeutic efficacy and safety of BTM@PEG-PE micelles on CT26 xenograft mice were evaluated. RESULTS: BTM was successfully embedded in the core of PEG-PE micelles, with a drug loading capacity of 5.62±0.80%. PEG-PE micelles facilitated BTM entering to the CT26 cells and BTM@PEG-PE micelles exerted enhanced anti-cancer efficacy against CT26 cells. BTM@PEG-PE micelles showed prolonged half-life and increased bioavailability. More importantly, BTM@PEG-PE micelles treatment suppressed tumor growth in tumor-bearing mice and prolonged survival with minimal damage to normal tissues. CONCLUSION: Altogether, the BTM@PEG-PE micelles might be a promising strategy to enhance the pharmacokinetic and pharmacodynamic potentials of BTM for colon cancer therapy. Dove 2019-09-12 /pmc/articles/PMC6749994/ /pubmed/31571860 http://dx.doi.org/10.2147/IJN.S221625 Text en © 2019 Wu et al. http://creativecommons.org/licenses/by-nc/3.0/ This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php).
spellingShingle Original Research
Wu, Jun-Yong
Li, Yong-Jiang
Liu, Xin-Yi
Cai, Jia-Xin
Hu, Xiong-Bin
Wang, Jie-Min
Tang, Tian-Tian
Xiang, Da-Xiong
3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer
title 3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer
title_full 3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer
title_fullStr 3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer
title_full_unstemmed 3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer
title_short 3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer
title_sort 3,5,4′-trimethoxy-trans-stilbene loaded peg-pe micelles for the treatment of colon cancer
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6749994/
https://www.ncbi.nlm.nih.gov/pubmed/31571860
http://dx.doi.org/10.2147/IJN.S221625
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