Lecithin-Stabilized Polymeric Micelles (LsbPMs) for Delivering Quercetin: Pharmacokinetic Studies and Therapeutic Effects of Quercetin Alone and in Combination with Doxorubicin

Chia-En Chang, Chien-Ming Hsieh, Sheng-Chin Huang, Chia-Yu Su, Ming-Thau Sheu, Hsiu-O. Ho

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Abstract

In this study, lecithin-stabilized polymeric micelles (LsbPMs) were prepared to load quercetin (QUE) in order to improve its bioavailability and increase its antitumor activity. Its combination with doxorubicin (DOX) to minimize DOX-mediated cardiac toxicity and increase the antitumor activity of QUE-loaded LsbPMs was also examined. LsbPMs were prepared following a previously reported procedure. Results demonstrated that optimal QUE-loaded LsbPMs contained quercetin, D-α-tocopheryl polyethylene glycol succinate, and lecithin at a weight ratio of 6:40:80. Drug-release studies showed that QUE released from LsbPMs followed a controlled release pattern. A cytotoxicity assay revealed that QUE-loaded LsbPMs had significant anticancer activities against MCF-7, SKBR-3, and MDA-MB-231 human breast cancer cells and CT26 mouse colon cancer cells. In animal studies, intravenous administration of QUE-loaded LsbPMs resulted in efficient growth inhibition of CT26 colon cancer cells in a Balb/c mice model. In a pharmacokinetics study compared to free QUE, intravenous and oral administration of QUE-loaded LsbPMs was found to have significantly increased the relative bioavailability to 158% and 360%, respectively, and the absolute bioavailability to 5.13%. The effect of QUE-loaded LsbPMs in combination with DOX resulted in efficient growth inhibition of CT26 colon cancer cells and reduced cardiac toxicity in the Balb/c mice model.
Original languageEnglish
Article number17640
Pages (from-to)17640
JournalScientific Reports
Volume8
Issue number1
DOIs
Publication statusPublished - Dec 1 2018

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Lecithins
Quercetin
Micelles
Therapeutic Uses
Doxorubicin
Pharmacokinetics
Colonic Neoplasms
Biological Availability
Intravenous Administration
Growth
Oral Administration
Breast Neoplasms
Weights and Measures

ASJC Scopus subject areas

  • General

Cite this

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title = "Lecithin-Stabilized Polymeric Micelles (LsbPMs) for Delivering Quercetin: Pharmacokinetic Studies and Therapeutic Effects of Quercetin Alone and in Combination with Doxorubicin",
abstract = "In this study, lecithin-stabilized polymeric micelles (LsbPMs) were prepared to load quercetin (QUE) in order to improve its bioavailability and increase its antitumor activity. Its combination with doxorubicin (DOX) to minimize DOX-mediated cardiac toxicity and increase the antitumor activity of QUE-loaded LsbPMs was also examined. LsbPMs were prepared following a previously reported procedure. Results demonstrated that optimal QUE-loaded LsbPMs contained quercetin, D-α-tocopheryl polyethylene glycol succinate, and lecithin at a weight ratio of 6:40:80. Drug-release studies showed that QUE released from LsbPMs followed a controlled release pattern. A cytotoxicity assay revealed that QUE-loaded LsbPMs had significant anticancer activities against MCF-7, SKBR-3, and MDA-MB-231 human breast cancer cells and CT26 mouse colon cancer cells. In animal studies, intravenous administration of QUE-loaded LsbPMs resulted in efficient growth inhibition of CT26 colon cancer cells in a Balb/c mice model. In a pharmacokinetics study compared to free QUE, intravenous and oral administration of QUE-loaded LsbPMs was found to have significantly increased the relative bioavailability to 158{\%} and 360{\%}, respectively, and the absolute bioavailability to 5.13{\%}. The effect of QUE-loaded LsbPMs in combination with DOX resulted in efficient growth inhibition of CT26 colon cancer cells and reduced cardiac toxicity in the Balb/c mice model.",
author = "Chia-En Chang and Chien-Ming Hsieh and Sheng-Chin Huang and Chia-Yu Su and Ming-Thau Sheu and Hsiu-O. Ho",
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AU - Chang, Chia-En

AU - Hsieh, Chien-Ming

AU - Huang, Sheng-Chin

AU - Su, Chia-Yu

AU - Sheu, Ming-Thau

AU - Ho, Hsiu-O.

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