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

Sci Rep. 2018 Dec 5;8(1):17640. doi: 10.1038/s41598-018-36162-0.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / administration & dosage*
  • Antioxidants / pharmacokinetics
  • Antioxidants / therapeutic use
  • Biological Availability
  • Cell Line, Tumor
  • Colonic Neoplasms / drug therapy
  • Colonic Neoplasms / pathology
  • Doxorubicin / administration & dosage*
  • Doxorubicin / pharmacokinetics
  • Doxorubicin / therapeutic use
  • Drug Carriers / chemistry*
  • Humans
  • Lecithins / chemistry*
  • Male
  • Mice, Inbred BALB C
  • Micelles*
  • Quercetin / administration & dosage*
  • Quercetin / pharmacokinetics
  • Quercetin / therapeutic use
  • Rats, Sprague-Dawley

Substances

  • Antioxidants
  • Drug Carriers
  • Lecithins
  • Micelles
  • Doxorubicin
  • Quercetin