Preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin
Jin-Feng Qiu,1 Xiang Gao,1,2 Bi-Lan Wang,1 Xia-Wei Wei,1 Ma-Ling Gou,1 Ke Men,1 Xing-Yu Liu,1 Gang Guo,1 Zhi-Yong Qian,1 Mei-Juan Huang1 1Department of Thoracic Oncology, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital and Medical School, Sichuan University, Chengdu, People...
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Dove Medical Press
2013
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oai:doaj.org-article:71b830a791a04cb4a8e5525d4b1c4d432021-12-02T02:10:29ZPreparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin1176-91141178-2013https://doaj.org/article/71b830a791a04cb4a8e5525d4b1c4d432013-08-01T00:00:00Zhttp://www.dovepress.com/preparation-and-characterization-of-monomethoxy-polyethylene-glycol-po-a14015https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Jin-Feng Qiu,1 Xiang Gao,1,2 Bi-Lan Wang,1 Xia-Wei Wei,1 Ma-Ling Gou,1 Ke Men,1 Xing-Yu Liu,1 Gang Guo,1 Zhi-Yong Qian,1 Mei-Juan Huang1 1Department of Thoracic Oncology, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital and Medical School, Sichuan University, Chengdu, People’s Republic of China; 2Medical School and Department of Pathophysiology, College of Preclinical and Forensic Medical Sciences, Sichuan University, Chengdu, People’s Republic of China Abstract: Luteolin (Lu) is one of the flavonoids with anticancer activity, but its poor water solubility limits its use clinically. In this work, we used monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles to encapsulate Lu by a self-assembly method, creating a water-soluble Lu/MPEG-PCL micelle. These micelles had a mean particle size of 38.6 ± 0.6 nm (polydispersity index = 0.16 ± 0.02), encapsulation efficiency of 98.32% ± 1.12%, and drug loading of 3.93% ± 0.25%. Lu/MPEG-PCL micelles could slowly release Lu in vitro. Encapsulation of Lu in MPEG-PCL micelles improved the half-life (t½; 152.25 ± 49.92 versus [vs] 7.16 ± 1.23 minutes, P = 0.007), area under the curve (0–t) (2914.05 ± 445.17 vs 502.65 ± 140.12 mg/L/minute, P = 0.001), area under the curve (0–∞) (2989.03 ± 433.22 vs 503.81 ± 141.41 mg/L/minute, P = 0.001), and peak concentration (92.70 ± 11.61 vs 38.98 ± 7.73 mg/L, P = 0.003) of Lu when the drug was intravenously administered at a dose of 30 mg/kg in rats. Also, Lu/MPEG-PCL micelles maintained the cytotoxicity of Lu on 4T1 breast cancer cells (IC50 = 6.4 ± 2.30 µg/mL) and C-26 colon carcinoma cells (IC50 = 12.62 ± 2.17 µg/mL) in vitro. These data suggested that encapsulation of Lu into MPEG-PCL micelles created an aqueous formulation of Lu with potential anticancer effect. Keywords: luteolin, micelle, MPEG-PCL, cancer therapyQiu JFGao XWang BLWei XWGou MLMen KLiu XYGuo GQian ZYHuang MJDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 3061-3069 (2013) |
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Medicine (General) R5-920 |
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Medicine (General) R5-920 Qiu JF Gao X Wang BL Wei XW Gou ML Men K Liu XY Guo G Qian ZY Huang MJ Preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin |
| description |
Jin-Feng Qiu,1 Xiang Gao,1,2 Bi-Lan Wang,1 Xia-Wei Wei,1 Ma-Ling Gou,1 Ke Men,1 Xing-Yu Liu,1 Gang Guo,1 Zhi-Yong Qian,1 Mei-Juan Huang1 1Department of Thoracic Oncology, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital and Medical School, Sichuan University, Chengdu, People’s Republic of China; 2Medical School and Department of Pathophysiology, College of Preclinical and Forensic Medical Sciences, Sichuan University, Chengdu, People’s Republic of China Abstract: Luteolin (Lu) is one of the flavonoids with anticancer activity, but its poor water solubility limits its use clinically. In this work, we used monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles to encapsulate Lu by a self-assembly method, creating a water-soluble Lu/MPEG-PCL micelle. These micelles had a mean particle size of 38.6 ± 0.6 nm (polydispersity index = 0.16 ± 0.02), encapsulation efficiency of 98.32% ± 1.12%, and drug loading of 3.93% ± 0.25%. Lu/MPEG-PCL micelles could slowly release Lu in vitro. Encapsulation of Lu in MPEG-PCL micelles improved the half-life (t½; 152.25 ± 49.92 versus [vs] 7.16 ± 1.23 minutes, P = 0.007), area under the curve (0–t) (2914.05 ± 445.17 vs 502.65 ± 140.12 mg/L/minute, P = 0.001), area under the curve (0–∞) (2989.03 ± 433.22 vs 503.81 ± 141.41 mg/L/minute, P = 0.001), and peak concentration (92.70 ± 11.61 vs 38.98 ± 7.73 mg/L, P = 0.003) of Lu when the drug was intravenously administered at a dose of 30 mg/kg in rats. Also, Lu/MPEG-PCL micelles maintained the cytotoxicity of Lu on 4T1 breast cancer cells (IC50 = 6.4 ± 2.30 µg/mL) and C-26 colon carcinoma cells (IC50 = 12.62 ± 2.17 µg/mL) in vitro. These data suggested that encapsulation of Lu into MPEG-PCL micelles created an aqueous formulation of Lu with potential anticancer effect. Keywords: luteolin, micelle, MPEG-PCL, cancer therapy |
| format |
article |
| author |
Qiu JF Gao X Wang BL Wei XW Gou ML Men K Liu XY Guo G Qian ZY Huang MJ |
| author_facet |
Qiu JF Gao X Wang BL Wei XW Gou ML Men K Liu XY Guo G Qian ZY Huang MJ |
| author_sort |
Qiu JF |
| title |
Preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin |
| title_short |
Preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin |
| title_full |
Preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin |
| title_fullStr |
Preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin |
| title_full_unstemmed |
Preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin |
| title_sort |
preparation and characterization of monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles for the solubilization and in vivo delivery of luteolin |
| publisher |
Dove Medical Press |
| publishDate |
2013 |
| url |
https://doaj.org/article/71b830a791a04cb4a8e5525d4b1c4d43 |
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