3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer
Jun-Yong Wu,1–3* Yong-Jiang Li,1–3* Xin-Yi Liu,1–3 Jia-Xin Cai,1–3 Xiong-Bin Hu,1–3 Jie-Min Wang,1–3 Tian-Tian Tang,1–3 Da-Xiong Xiang1–3 1Department of Pharmacy, The Second Xiangya Hospital, Central South University, Ch...
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Dove Medical Press
2019
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oai:doaj.org-article:317f186bde7846c2bb19ef1cab48c87b2021-12-02T09:56:51Z3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer1178-2013https://doaj.org/article/317f186bde7846c2bb19ef1cab48c87b2019-09-01T00:00:00Zhttps://www.dovepress.com/354prime-trimethoxy-trans-stilbene-loaded-peg-pe-micelles-for-the-trea-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jun-Yong Wu,1–3* Yong-Jiang Li,1–3* Xin-Yi Liu,1–3 Jia-Xin Cai,1–3 Xiong-Bin Hu,1–3 Jie-Min Wang,1–3 Tian-Tian Tang,1–3 Da-Xiong Xiang1–3 1Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha 410011, Hunan, People’s Republic of China; 2Institute of Clinical Pharmacy, Central South University, Changsha 410011, Hunan, People’s Republic of China; 3Hunan Provincial Engineering Research Center of Translational Medicine and Innovative Drug, Changsha, Hunan, People’s Republic of China*These authors contributed equally to this workCorrespondence: Da-Xiong XiangDepartment of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha 410011, Hunan, People’s Republic of ChinaEmail xiangdaxiong@csu.edu.cnBackground: 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.Keywords: 3,5,4′-trimethoxy-trans-stilbene, bioavailability, colon cancer, drug delivery, micellesWu JYLi YJLiu XYCai JXHu XBWang JMTang TTXiang DXDove Medical Pressarticle354′-trimethoxy-trans-stilbenebioavailabilitycolon cancerdrug deliverymicellesMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 7489-7502 (2019) |
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3 5 4′-trimethoxy-trans-stilbene bioavailability colon cancer drug delivery micelles Medicine (General) R5-920 |
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3 5 4′-trimethoxy-trans-stilbene bioavailability colon cancer drug delivery micelles Medicine (General) R5-920 Wu JY Li YJ Liu XY Cai JX Hu XB Wang JM Tang TT Xiang DX 3,5,4′-trimethoxy-trans-stilbene loaded PEG-PE micelles for the treatment of colon cancer |
| description |
Jun-Yong Wu,1–3* Yong-Jiang Li,1–3* Xin-Yi Liu,1–3 Jia-Xin Cai,1–3 Xiong-Bin Hu,1–3 Jie-Min Wang,1–3 Tian-Tian Tang,1–3 Da-Xiong Xiang1–3 1Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha 410011, Hunan, People’s Republic of China; 2Institute of Clinical Pharmacy, Central South University, Changsha 410011, Hunan, People’s Republic of China; 3Hunan Provincial Engineering Research Center of Translational Medicine and Innovative Drug, Changsha, Hunan, People’s Republic of China*These authors contributed equally to this workCorrespondence: Da-Xiong XiangDepartment of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha 410011, Hunan, People’s Republic of ChinaEmail xiangdaxiong@csu.edu.cnBackground: 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.Keywords: 3,5,4′-trimethoxy-trans-stilbene, bioavailability, colon cancer, drug delivery, micelles |
| format |
article |
| author |
Wu JY Li YJ Liu XY Cai JX Hu XB Wang JM Tang TT Xiang DX |
| author_facet |
Wu JY Li YJ Liu XY Cai JX Hu XB Wang JM Tang TT Xiang DX |
| author_sort |
Wu JY |
| title |
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_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_sort |
3,5,4′-trimethoxy-trans-stilbene loaded peg-pe micelles for the treatment of colon cancer |
| publisher |
Dove Medical Press |
| publishDate |
2019 |
| url |
https://doaj.org/article/317f186bde7846c2bb19ef1cab48c87b |
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