Open Access

Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells

  • Authors:
    • Jun Hu
    • Junjie Wang
    • Gang Wang
    • Zhongjun Yao
    • Xiaoqian Dang
  • View Affiliations

  • Published online on: January 14, 2016     https://doi.org/10.3892/ijmm.2016.2458
  • Pages: 690-702
  • Copyright: © Hu et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

In the present study, a new type of DSPE-PEG2000 polymeric liposome for the brain-targeted delivery of poorly water-soluble anticancer drugs was successfully prepared and characterized. The nanoparticles were formed by the self-assembly of an amphiphilic polymer consisting of hydrophilic 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (DSPE‑PEG2000). These nanoliposomes served as a safe delivery platform for the simultaneous delivery of quercetin (QUE) and temozolomide (TMZ) to rat brains. The 2-in-1 PEG2000‑DSPE nanoliposomes containing QUE and TMZ (QUE/TMZ-NLs) were rapidly taken up by the U87 glioma cells in vitro, whereas at the same concentrations, the amounts of the free drugs taken up were minimal. The QUE/TMZ-NLs showed an enhanced potency in the U87 cells and the TMZ-resistant U87 cells (U87/TR cells), possibly due to the high intracellular drug concentration and the subsequent drug release. In vivo biodistribution experiments revealed a significant accumulation of QUE/TMZ-NLs in the brain, with significantly increased plasma concentrations of QUE and TMZ, as well as delayed clearance in our rat model of glioma. The results were not so significant for the QUE-loaded nanoliposomes (QUE-NLs) and free TMZ. The findings of our study establish the DSPE‑PEG2000 polymeric liposome as a novel and effective nanocarrier for enhancing drug delivery to brain tumors.
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March-2016
Volume 37 Issue 3

Print ISSN: 1107-3756
Online ISSN:1791-244X

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Spandidos Publications style
Hu J, Wang J, Wang G, Yao Z and Dang X: Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells. Int J Mol Med 37: 690-702, 2016
APA
Hu, J., Wang, J., Wang, G., Yao, Z., & Dang, X. (2016). Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells. International Journal of Molecular Medicine, 37, 690-702. https://doi.org/10.3892/ijmm.2016.2458
MLA
Hu, J., Wang, J., Wang, G., Yao, Z., Dang, X."Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells". International Journal of Molecular Medicine 37.3 (2016): 690-702.
Chicago
Hu, J., Wang, J., Wang, G., Yao, Z., Dang, X."Pharmacokinetics and antitumor efficacy of DSPE-PEG2000 polymeric liposomes loaded with quercetin and temozolomide: Analysis of their effectiveness in enhancing the chemosensitization of drug-resistant glioma cells". International Journal of Molecular Medicine 37, no. 3 (2016): 690-702. https://doi.org/10.3892/ijmm.2016.2458